20th Annual Drug Discovery Summit - Oxford Global · 34% Senoir Manager / Scientist or Lab Head...

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Ingo Hartung Bayer Denise Barrault NPSC Lauren Drowley UCB Pharma Emilio Merlo Pich Takeda Carl Petersson Merck KGaA Teemu Junttila Genentech KEY SPEAKERS INCLUDE Conference Brochure DELEGATES FROM LEADING PHARMA, BIOTECH & ACADEMIC COMPANIES 350+ INTERACTIVE STREAMS ON THE LATEST INNOVATIONS 10 PRESENTATIONS, CASE STUDIES AND DISCUSSIONS 100+ R&D SERIES EU 20th Annual Drug Discovery Summit 7th Annual Discovery Chemistry & Drug Design Congress Bispecifics in Discovery & Development Congress Neuroscience in Discovery & Development Congress + Pre-Event Drug Discovery Workshop 10 - 12 June 2019 | Berlin, Germany Join the Conversation #RNDSeries19 | #DDSEU19

Transcript of 20th Annual Drug Discovery Summit - Oxford Global · 34% Senoir Manager / Scientist or Lab Head...

Ingo Hartung Bayer

Denise Barrault NPSC

Lauren Drowley UCB Pharma

Emilio Merlo Pich Takeda

Carl Petersson Merck KGaA

Teemu Junttila Genentech

KEY SPEAKERS INCLUDE

Conference Brochure

DELEGATES FROM LEADING PHARMA, BIOTECH & ACADEMIC

COMPANIES

350+INTERACTIVE STREAMS ON THE LATEST INNOVATIONS

10PRESENTATIONS, CASE

STUDIES AND DISCUSSIONS

100+

R&D SERIES EU

20th Annual Drug Discovery Summit7th Annual Discovery Chemistry & Drug Design Congress

Bispecifics in Discovery & Development CongressNeuroscience in Discovery & Development Congress

+ Pre-Event Drug Discovery Workshop

10 - 12 June 2019 | Berlin, Germany

Join the Conversation #RNDSeries19 | #DDSEU19

2018’s Congress in Review

81%14%

5%

34% Senoir Manager /Scientist or Lab Head

50% Director & ProfessorPharma & Biotech

16% Commercial or BD

A T T E N D E E P R O F I L E

12% Academic & Healthcare

32%

56%

Vendor Companies

SECTOR FUNCTION

81% UK & Europe

14% USA

5% Rest of World

GEOGRAPHY

SPEAKERS75

EXHIBITORSSPONSORS AND

35300ATTENDEES

81%14%

5%

34% Senoir Manager /Scientist or Lab Head

50% Director & ProfessorPharma & Biotech

16% Commercial or BD

A T T E N D E E P R O F I L E

12% Academic & Healthcare

32%

56%

Vendor Companies

SECTOR FUNCTION

81% UK & Europe

14% USA

5% Rest of World

GEOGRAPHY

SPEAKERS75

EXHIBITORSSPONSORS AND

35300ATTENDEES

81%14%

5%

34% Senoir Manager /Scientist or Lab Head

50% Director & ProfessorPharma & Biotech

16% Commercial or BD

A T T E N D E E P R O F I L E

12% Academic & Healthcare

32%

56%

Vendor Companies

SECTOR FUNCTION

81% UK & Europe

14% USA

5% Rest of World

GEOGRAPHY

SPEAKERS75

EXHIBITORSSPONSORS AND

35300ATTENDEES

81%14%

5%

34% Senoir Manager /Scientist or Lab Head

50% Director & ProfessorPharma & Biotech

16% Commercial or BD

A T T E N D E E P R O F I L E

12% Academic & Healthcare

32%

56%

Vendor Companies

SECTOR FUNCTION

81% UK & Europe

14% USA

5% Rest of World

GEOGRAPHY

SPEAKERS75

EXHIBITORSSPONSORS AND

35300ATTENDEES

Welcome

Oxford Global’s R&D Europe Series features four outstanding programmes: the 20th Annual Drug Discovery Summit and 7th Annual Discovery Chemistry & Drug Design Congress, Bispecifics in Discovery & Development Congress and Neuroscience in Discovery and Development Congress. Uniting 350 drug discovery attendees from global pharmaceutical organisations, top biotech companies and internationally renowned academic institutions, this series provides a valuable opportunity for leaders to transform and lead the future of drug discovery and development.

20th Annual Drug Discovery Summit and 7th Annual Discovery Chemistry & Drug Design: The congresses will focus on facing the complexity of drug discovery and development head on, looking at improving target identification, validation and optimisation as well as hit exploration and discovery within biologics, small molecules and critical therapeutic areas such as oncology. New for 2019, the congress will be showcasing three critical focus sessions in the areas of AI/ML, DNA-encoded libraries and protein degradation in drug discovery and development.

Bispecifics in Discovery & Development Congress: Gain valuable insights into the most innovative bispecific antibody drug discovery strategies and platforms with key leaders in the field. Hear about maximising clinical performance through effective translation studies and discuss biomarker analysis in clinical development. Further consideration will also be given to safety, aggregation, immunogenicity and CMC considerations.

Neuroscience in Discovery and Development Congress: Explore the latest strategies and technologies impacting the neuroscience field; from identifying and validating molecular targets to patient stratification and diagnostics. Further talks include an overview of biomarkers in neuroscience and the use of CRISPR screening.

I liked that there was a broad variety of topics regarding early drug discovery at this conference.

- Head of Investigational Toxicology, Vice President, Bayer AG

There was a good number of attendees, not too many, not too few. There was strong selection of different companies and a great number of potential clients. I also thought there was a good mix of big companies and smaller ones. Long coffee breaks allowed time to discuss

- Scientific Project Manager, Discngine“ “

Don’t Miss Our Complimentary Webinars and Workshops

Wednesday 13th March 2019 at 10:00am GMT / 11:00am CET Functional Genomics Strategies At AstraZeneca hosted by Davide Gianni, Associate Director, AstraZeneca

Tuesday 23rd April 2019 at 2:00pm BST / 3:00pm CEST Effect of Removing Cholinergic Input On Auditory Sensory Processing hosted by Victoria Bajo Lorenzana, Associate Professor of Neuroscience, University of Oxford

Tuesday 5th March 2019 at 10:00am GMT / 11:00am CET Nanofitin-Antibody Fusion As A Novel Multispecific Platform: Providing Extra Specificities While Maintaining Developability hosted by Mathieu Cinier, Scientific Director, Affologic

Drug Discovery and Discovery Chemistry &

Drug DesignClick here to view Agenda

6PAGE

15PAGE Bispecifics in Discovery

& Development

Click here to view Agenda19PAGE Neuroscience in

Discovery & Development

Click here to view Agenda

Monday 10th June 2019 at 12:30pm CEST Structure-Based Drug Design, Docking and SAR Analysis Chemical Computing Group Pre-Congress Workshop

Click here to register your interest in upcoming webinars, or download past webinars from our Resources page

Click here for more details on the workshop

WHO IS ATTENDING?

For the full attendee list please contact [email protected] companies and many more

WHO IS SPONSORING?

For sponsorship enquiries, please contact [email protected]

350+ VPs, Directors & Senior Managers from pharmaceutical organisations, biotech companies and academic institutions in the following fields:

Formal and informal meeting opportunities offer delegates the chance to meet with leading service providers and discuss key solutions including:

● Small Molecule Drug Discovery

● Target Selection / Validation

● Protein Therapeutics ● Antibody Engineering ● Biomarker Development ●CMC ● Cell Line Development ● Therapeutic Discovery

●Neuroengineering

● Bispecific Antibody Discovery

● Neuroscience Discovery ● Stem Cell Platform Technologies ● Cell Line Development ● Translational Neuro Imaging

●Neuroinformatics

● Preclinical Biology

● CNS Discovery

● Translational Neurobiology

● Protein/Antibody Engineering

● Computational Neuroscience

● Large Molecule Drug Discovery

● Lead Optimisation ● Drug Design ●Modelling

● Medicinal / Discovery Chemistry

● Oncology

● Modelling and Simulation ● Target Validation

● Lead Optimisation ● Assay Development

● Phenotypic Screening

● AI / Machine Learning

● DNA Encoded Libraries

● Protein Degradation

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The 20th Annual Drug Discovery Summit and co-located 7th Annual Discovery Chemistry & Drug Design Congress feature 6 interactive streams, which include over 65 presentations, case studies and panel discussions focused on the key issues in drug discovery and medicinal chemistry today:

DRUG DISCOVERY: AGENDA AT A GLANCE

CO-LOCATED EVENT: 7TH ANNUAL DISCOVERY CHEMISTRY & DRUG DESIGN CONGRESS

CO-LOCATED EVENT: 7TH ANNUAL DISCOVERY CHEMISTRY & DRUG DESIGN CONGRESS

DAY ONE: 11 JUNE DAY TWO: 12 JUNE

1

2 2

3 3

DRUG DISCOVERY INNOVATION AND STRATEGIES

PHENOTYPIC SCREENING IN DRUG DISCOVERY AND HIGH CONTENT SCREENING TOOLS

DISCOVERY CHEMISTRY, MEDICINAL AND COMPUTATIONAL CHEMISTRY

MEDICINAL CHEMISTRY AND DRUG DESIGN: NOVEL APPROACHES

CRISPR/Cas 9 Therapeutics

New Modalities For Challenging Targets

• Proteins, Antibodies and Peptides

Innovative Tools and Technologies for Drug Discovery

Open Innovation Through Partnerships:

• Public-Private Collaborations

• Drug Discovery Partnerships / Collaboration Models

Protein Degradation In Drug Discovery & Drug Design

Target Discovery and Phenotypic Screening

Novel Approaches for Phenotypic Screening

• Pooled CRISPR and Phenotypic Screens

Updates in High-Throughput Screening

Next Generation High-Content Screening

Computational Chemistry Approaches in Drug Discovery

Case Study: Binding Affinity Estimating in Drug Design

High-Throughput Chemistry Approaches

Peptide Discovery and Development

• Oral peptide-based macrocycles

• Peptidomimetics in discovery chemistry

• HDAC Inhibitor discovery

Protein-Protein Interactions as Drug Targets

Targeting RNA – Modifying Enzymes

Case Studies in Fragment-Based Discovery

Novel Tools and Assays to Determine Compound Behaviour

INNOVATION IN GENOME AND CELL BASED DRUG DISCOVERY, SCREENING, IMAGING & TARGET DISCOVERY

1 BIOLOGICS AND SMALL MOLECULE DRUG TARGET DISCOVERY FOR IMMUNO-THERAPY, AUTOIMMUNE DISEASES AND ONCOLOGY

Drug-Target Kinetics In Drug Discovery

Updates in Cancer Target Validation

Epigenetics in Oncology and Immuno-Oncology

Cancer Metabolism Targets

Antibodies for Oncology and Immuno-Therapy

Antibody and T-Cell Discovery

Peptides for Tumour Targeting

Modelling and Organ-On-A-Chip

Functional Genomics in Drug Discovery

• Single Cell CRISPR Techniques

Gene Editing For Drug Discovery

• CRISPR

Novel Platforms For Gene Based Drug Discovery

Epigenetic Drug Discovery

PANEL DISCUSSION: The Real Measurable Outcomes of AI / ML in Drug Discovery & Design

Focused Session: AI and ML in Drug Discovery• Application and Case Studies of AI in Drug Discovery• AI in Clinical Development• Opportunities and Challenges of AI / ML in Drug Discovery

Focused Session: AI in Medicinal Chemistry & Drug Design• ML & Toxicity Prediction / Hit-to-Lead Optimisation / Deep

Learning in Medicinal Chemistry

Focused Session: DNA Encoded Libraries in Drug Discovery• Updates in Small Molecule Drug Discovery• Protein-Protein Interactions and DNA Encoded Libraries• Encoded Peptide Libraries for Drug Discovery• Application of Encoded Self-Assembly Chemical Libraries

DAY 1, STREAM 1

DAY 1, STREAM 2PHENOTYPIC SCREENING IN DRUG DISCOVERY AND HIGH CONTENT SCREENING TOOLS

DAY 1, STREAM 3 DISCOVERY CHEMISTRY: MEDICINAL AND COMPUTATIONAL CHEMISTRY

DRUG DISCOVERY: SPEAKERS BY STREAM

DAVIDE GIANNI

Associate Director AstraZeneca

CARL PETERSSON

Scientific Director Drug Disposition Merck KGaA

DENISE BARRAULT

Executive Director NPSC

RICHARD LEWIS

Global Head CADD Novartis

JEAN-PHILIPPE STEPHANDirector SERVIER Center of Excellence Pharmacological Screening, Compound Management and Biobanking Institut de Recherches SERVIER

GOVINDA BHISETTIPrincipal Investigator and Head of Computation Chemistry Biogen

NILS JAKOB VEST HANSEN

Chief Executive Officer Vipergen ApS

CLARA CHRIST

Head of Computational Molecular Design Bayer AG

ALEX BATCHELOR

Chief Executive Officer Orbit Discovery

ERIC GOEDKENPrincipal Scientist, Discovery Dermatology & FibrosisAbbVie

BRANDON ALLGOOD

Chief Technology Officer Numerate, Inc

WILLEM VAN HOORN

Chief Decision Scientist Exscientia Ltd

PATRICK JIMONETDirector, External Innovation in Drug Discovery Sanofi

YOLANDA CHONG

Senior Vice President, Biology Recursion Pharmaceuticals

CHRISTIAN TYRCHAN

Teamleader Computational Chemistry AstraZeneca

JOHANNES OTTLDirector Novartis Institutes for BioMedical Research, Chemical Biology & Therapeutics, Chemical Genetics

GARRICK SMITH

Project Manager Nuevolution

FLORENT SAMAIN

Research Scientist Philochem

MARTIN REDHEAD

Group Leader Molecular Pharmacology UCB

PATRICK STEIGEMANN

Senior Scientist Bayer

SUGUNA RACHAKONDA

Senior Director, Product Development Cleveland Clinic

SARAH BROCKBANK

Lead Scientist - Virtual R&D Medicines Discovery Catapult

GREG MILLER

Principal Data Scientist BERG Health

GISBERT SCHNEIDER

Professor ETH Zürich

MATTHIAS RAREYProfessor University of Hamburg / Center for Bioinformatics

DAY 2, STREAM 2INNOVATION IN GENOME AND CELL BASED DRUG DISCOVERY, SCREENING, IMAGING & TARGET DISCOVERY

SYLVIA BOJ

Scientific Director Hubrecht Organoid Technology

JENNA BRADLEY

Senior Research Scientist AstraZeneca

MICHAEL DIDRIKSEN

Senior Director Lundbeck

MANFRED JUNG

Professor Freiburg University

LAUREN DROWLEY

Director, Head Functional Genomics UCB Pharma

ARNE HANSENProfessor University Medical Center Hamburg-Eppendorf (UKE)

DAVID BRIERLEY

Team Leader GlaxoSmithKline

DRUG DISCOVERY: SPEAKERS BY STREAM

DRUG DISCOVERY INNOVATION AND STRATEGIES DAY 2, STREAM 1BIOLOGICS AND SMALL MOLECULE DRUG TARGET DISCOVERY FOR IMMUNO-THERAPY, AUTOIMMUNE DISEASES AND ONCOLOGY

AFJAL MIAHInvestigator, Medicinal Chemistry, Protein Degradation GlaxoSmithKline

YUSUKE TOMINARIChief Executive Officer / Chief Scientific Officer FIMECS, Inc.

MIKE SCHOPPERLE

Chief Executive Officer CureMeta

GEMMA MUDD

Senior Scientist Bicycle Therapeutics

FRANCES NEAL

Scientist 1 AstraZeneca

INGO HARTUNG

Vice President of Medicinal Chemistry Bayer

ELIZABETH DE LANGEProfessor Predictive Pharmacology LACDR - Division of Systems Biomedicine and Pharmacology

TAMARA MAES

Chief Scientific Officer Oryzon Genomics

FRED JACOBS

Chief Executive Officer and Co-Founder TYG Oncology

TAMARA REYES ROBLES

Senior Scientist MSD

JACOB STUCKEY

Senior Scientist Constellation Pharmaceuticals

PHILIP LIENAU

Senior Research PK Scientist Bayer

ERIK NORDLINGPrincipal Scientist, Biomedical Science & Portfolio Innovation Sobi

DAY 2, STREAM 3 MEDICINAL CHEMISTRY AND DRUG DESIGN: NOVEL APPROACHES

JOSE A. MARTINEZ PEREZPrincipal Research Scientist, Discovery Research & Technologies Eli Lilly

JAMES O’CONNELL

Director, Structural Biology UCB

CHRISTIAN ADAM OLSENProfessor, Center for Biopharmaceuticals and Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences University of Copenhagen

WESLEY BLACKABY

Vice President of Chemistry Storm Therapeutics

ANDREW ROUGHTON

Vice President Discovery & Operations Encycle Therapeutics

ANDREAS RITZÉN

Senior Principal Scientist Leo Pharma A/S

HUIFEN CHENSenior Scientist, Computational Drug Design Genentech, Inc.

ZARA SANDS

Principal Scientist UCB BioPharma

THOMAS EVANGELIDISResearch ScientistInstitute of Organic Chemistry & Biochemistry of the Czech Academy of Sciences

MIKE DYSON

Chief Technology Officer IONTAS Ltd

COMPLIMENTARY PRE-CONGRESS WORKSHOP

Date: June 10th 2019

Venue: Maritim proAte Hotel, Friedrichstr. 151, 10117 Berlin

Aim of the Workshop

Aid the progression of drug discovery projects computationally, in the presence or absence of protein-ligand structural information.

Workshop Summary

Structure-based drug design, aided by computational methods, is now well established as a key discipline in the discovery of new medicines. The workshop will illustrate a range of computational techniques for SBDD, covering some related areas such as docking, and analysis of SAR data in case protein-ligand crystal structural information is not available, through demonstration using the MOE software. Trial copies of MOE can be provided by contacting [email protected]

Chemical Computing GroupComplimentary Pre-Congress Workshop

Structure-Based Drug Design, Docking and

SAR Analysis

Sponsored by

To sign up for this complimentary workshop, be sure to select it when making your booking.Contact [email protected] for more details.

13:30-

14:00

15:15-

15:45

12:30-

13:30

14:00-

15:15

15:45-

17:00

WORKSHOP PROGRAMME

Presentation: Targeting Specifi c Interactions to Improve EGFR-Ligand BindingThe epidermal growth factor receptor (EGFR) is implicated in many cancers, and its kinase activity is the target of commercial anti-cancer agents such as Tarceva and Iressa. However, despite their eff ectiveness, EGFR kinase inhibitors often show only moderate anti-proliferative activity against certain tumor types in the clinic. This inspired the investigation of dual action therapeutic agents directed not only at EGFR kinase but also at divergent targets such as Src kinase or DNA, with the purpose of producing single compounds termed “combi-molecules”, with greater potency than the single-mode EGFR inhibitor. A structure-based drug design modeling program, combined with PDB data-mining and protein structural fi ngerprints was used to help identify and characterize inhibitor design motifs for the development of combi-molecules. The resulting combi-molecules showed EGFR inhibitory potency in the low micromolar to nM range as well as DNA cross-linking activity.

Workshop: Structure-Based Drug DesignMolecular Surfaces and Maps / Ligand Interactions / Conformational Searching / Ligand Optimization / Ligand Selectivity / Protein Alignments and Superposition

Workshop: Protein-Ligand Docking and SAR AnalysisDocking / Fragment-based Design / Scaff old Replacement / R-Group Screening / Project Search / Protein-Ligand Interaction Fingerprints / MOEsaic / MMP Analysis

Registration and Lunch

Refreshment Break

R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY ONE: 11 JUNE

07:30-

08:20Registration: Conference Floor 1 Foyer

R&D SERIES EU

08:20 Conference Room: Hall II Oxford Global Welcome Address

08:25 Chairperson’s Opening Address: MIKE DYSON, Chief Technology Offi cer, IONTAS Ltd

08:30-

09:00

Co-Located Keynote Address: Communicating Prospective Accuracy Of Human PK PD Predictions; Impact In Discovery And Early Development Of Small Molecules• Increasing accuracy and integration of PK and PD along the value chain• Point prediction Vs density plots; impact on decision making• Impact of dose predictions on optimization strategies

CARL PETERSSON, Scientifi c Director Drug Disposition,Merck KGaA

DRUG DISCOVERY SUMMIT DISCOVERY CHEMISTRY& DRUG DESIGN CONGRESS

DRUG DISCOVERY INNOVATION AND STRATEGIES

PHENOTYPIC SCREENING IN DRUG DISCOVERY AND HIGH CONTENT SCREENING TOOLS

DISCOVERY CHEMISTRY: MEDICINAL AND COMPUTATIONAL CHEMISTRY

Conference Room: Hall II Conference Room: Salon 2 Conference Room: Salon 4

Stream Chair: MIKE DYSON, Chief Technology Offi cer,IONTAS Ltd

Stream Chair: JEAN-PHILIPPE STEPHAN, Director SERVIER Center of Excellence Pharmacological Screening, Compound Management and Biobanking, Institut de Recherches SERVIER

Stream Chair: KEVIN FOOTE, Vice President, Head of Drug Discovery Services Europe, Pharmaron

09:00-

09:30

Stream Keynote Address: Generation Of Large Mammalian Display Libraries For Isolating Novel Therapeutic Antibodies With Desirable Development Characteristics

Stream Keynote Address: An Integrated Approach To Target Discovery Through Phenotypic Screening

Stream Keynote Address: From Seven Million To Four: Identifying Novel Covalent Binders For KRASG12C

• Large libraries containing a single antibody gene/cell constructed in mammalian cells using directed integration of antibody genes by CRISPR/Cas9 and TALE nucleases

• 10s millions of monoclonal stable cell lines displaying IgG formatted antibodies on their surface from which novel binders can be isolated

• Select antibodies with improved solubility during antibody discovery

• Much evidence indicates that Target Discovery is a critical step to reduce attrition rate in drug discovery due to lack of clinical effi cacy

• The vision of the functional genomics group in Astrazeneca is to leverage experience in high content imaging and CRISPR/Cas9 technology to deliver novel target hypothesis through phenotypic screening

• I will discuss a few examples of the integrated approach we have taken to identify novel vulnerabilities that aff ect the stability of known tumour drivers

• Binding free energy calculations are now routinely used as they are accurate and fast enough to show substantial impact

• We will present the average accuracy obtained over a multitude of research projects and point out examples of the expanded applicability domain seen in recent years

• We show how a multistep workfl ow allowed the discovery of novel, selective, low single digit uM KRASG12C inhibitors with an unprecedented binding mode

MIKE DYSON, Chief Technology Offi cer,IONTAS Ltd

DAVIDE GIANNI, Associate Director,AstraZeneca

CLARA CHRIST, Head of Computational Molecular Design,Bayer AG

09:30-

10:00

Looking Toward Multiple Modalities Against Targets & Pathways - The Leading Edge Of Drug Discovery

Unbiased Mode Of Action Deconvolution Using CETSA® MS, A Case Study With Thalidomide

Biology Oriented Library Design

What is CETSA® MS? How and when to apply thermal proteome profi ling illustrated by case study examples.

• Analyticon‘ Chemical Ecosystem • Fragments from Nature • Virtual Library • Structural Biology • Structure based Library Design • Integrated Drug Discovery

JAYASHREE AIYAR, Vice President Biology,Syngene International

MICHAEL DABROWSKI, Chief Executive Offi cer,Pelago Bioscience

LARS OLE HAUSTEDT, Director Projects & Innovation,AnalytiCon Discovery GmbH

10:00-

11:20

Exhibition Area: Hall IMorning Coff ee & Refreshments, One To One Meetings x4, Poster Presentation Sessions

11:20-

11:50

Workshop: Improving The Quality And Reproducibility Of Data In Drug DiscoveryCo-leaders of this workshop, Bertrand Raynal (Insitut Pasteur) and Natalia Markova (Malvern Panalytical) will share experiences highlighting the importance of ensuring sample quality and observing good experimental practices for the generation of meaningful and reliable binding and structural data in drug discovery projects. Interactive presentations will be followed by a panel discussion.

Pooled CRISPR Genomic And Small Molecule Phenotypic Screens Targeting Keratinocyte Signaling

Can Computer-Aided Drug Design Impact Chemistry?

• I will outline our approach and compare/contrast the fi ndings from these two orthogonal methods

• This provides an example of successful screening in primary cells using a pooled CRISPR format

• I will highlight a target with novel involvement in the IL-17 pathway that we have identifi ed in this manner

There is no doubt that CADD has impacted the drug discovery process with key contributions to several marketed drugs. The question is whether in silico models are woven into the daily decision making of medicinal chemists, or is experimental data always sought? With the rebirth of AI, the infl uence of models on decision making becomes even more relevant.

NATALIA MARKOVA, Segment Marketing Manager,Malvern PanalyticalBERTRAND RAYNAL, Senior Experimental Offi cer,Institut Pasteur

ERIC GOEDKEN, Principal Scientist, Discovery Dermatology & Fibrosis,AbbVie

RICHARD LEWIS, Global Head CADD,Novartis

STREAM

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11:50-

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Workshop: Improving The Quality And Reproducibility Of Data In Drug Discovery (Continued)

Strategies Towards Target ID In Phenotypic Drug DiscoveryRecent developments in PDD at Evotec, including

• Cell painting

• CRISPR screening

• Relevant cellular systemsCo-leaders of this workshop, Bertrand Raynal (Insitut Pasteur) and Natalia Markova (Malvern Panalytical) will share experiences highlighting the importance of ensuring sample quality and observing good experimental practices for the generation of meaningful and reliable binding and structural data in drug discovery projects.

Interactive presentations will be followed by a panel discussion.

Presentation 1: Implementing A Standardized Protein Sample Quality Control (QC) Service

BERTRAND RAYNAL, Senior Experimental Offi cer,Institut Pasteur

Presentation 2: Sample And Data Quality In Interaction And Structural Analysis – Two Sides Of The Same Coin

NATALIA MARKOVA, Principal Scientist – MicroCal, Malvern Panalytical

Panel Discussion

NATALIA MARKOVA, Principal Scientist – MicroCal, Malvern Panalytical

BERTRAND RAYNAL, Senior Experimental Offi cer,Institut Pasteur

INA STERNBERGER, Senior Vice President In Vitro Biology,Evotec

PHENOTYPIC SCREENING IN DRUG DISCOVERY AND HIGH CONTENT SCREENING TOOLS

DISCOVERY CHEMISTRY: MEDICINAL AND COMPUTATIONAL CHEMISTRY

Conference Room: Salon 2 Conference Room: Salon 4

12:20-

12:50

Transcriptome Profi ling And Functional Screening To Identify Genes Driving Biological Responses And Disease Progression

Teaching A Robot To Get High: Automated Multi-Objective Drug Design Using Cyclica’s Ligand Design™ Platform

• Labeling individual cells with unique barcodes detectable by both NGS and RNA sequencing provides a way to identify cell subpopulations and track fractions of cells experiencing phenotypic changes such as activation or diff erentiation

• Transduced populations can then be analyzed by NGS to identify subsets of cells with specifi c traits or phenotypic responses

• NGS analysis of targeted multiplex RT-PCR from cell samples, down to single-cell levels, enables parallel analysis of diff erences in gene activation

• Emerging in silico drug design technologies aim to substitute individual processes in the established, target-centric paradigm. At Cyclica, we believe that modern machine learning approaches have the potential to redefi ne drug discovery by factoring in increasingly holistic models of living systems. Looking beyond single targets provides new opportunities to create eff ective medicines

• By combining powerful methods for molecule generation, ADMET prediction, and high-throughput ligand-protein interaction prediction through MatchMaker™, we have created the Ligand Design™ platform: a tool for building new molecules with desirable polypharmacological profi les and physicochemical/ADMET properties

• In this talk, we are excited to introduce the Ligand Design™ platform. We will explore the methods and approaches used during the process of generating new molecules with the system, and illustrate the generation of novel psychoactive compounds as a specifi c applied example

PAUL DIEHL, Chief Operating Offi cer,Cellecta, Inc.

ANDREW E. BRERETON, Scientist and Drug Design Team Lead,Cyclica Inc.

12:50-

13:50

Exhibition Area: Hall ILunch, One To One Meetings x2, Poster Presentation Sessions

Stream Chair: Martin Redhead, Group Leader Molecular Pharmacology, UCB

Stream Chair: JEAN-PHILIPPE STEPHAN, Director SERVIER Center of Excellence Pharmacological Screening, Compound Management and Biobanking, Institut de Recherches SERVIER

Stream Chair: KEVIN FOOTE, Vice President, Head of Drug Discovery Services Europe, Pharmaron

13:50-

14:20

Advanced 3D Cell Culture Assays For High-Throughput, High-Content Screening In Drug Discovery: Selected Case Reports

Improving Translation Through AI Modeling Of ADME/Tox

• Setup of a robust system for high-throughput, high-content screening of 3D cell culture models using automated workfl ows

• Selected case reports for the use of 3D spheroids in oncology and pharmacological target deconvolution

• Short reports on 3D HCS for invasive diseases and polycystic kidney disease

• Discuss the current state-of-the-art modeling of ADME and toxicity

• Examine some of the challenges/wins in applying AI modeling to ADME and toxicity

• Explore case studies involving the use of these models to solve key challenges

PATRICK STEIGEMANN, Senior Scientist,Bayer

BRANDON ALLGOOD, Chief Technology Offi cer,Numerate, Inc

14:20-

14:50

Allosteric fA As Reagents And Therapeutics

Moving High-Content Screening Into The Fourth Dimension

Introducing The Centaur ChemistTM

The increase in structural information collected on drug targets has allowed for the prosecution of increasingly complex targets, previously considered ‘undrugable’. During this period antibodies have also found commercial success in tackling targets previously intractable to small molecules. Most commercial therapeutic antibodies work by binding to the ligand binding site of their target, and hence are competitive orthosteric molecules. Antibodies are also able to stabilise the conformation of the protein they bind to and have found success aiding crystallographic eff orts. Most antibodies stabilise the most common conformation of the protein (its lowest energy state), but some rare antibodies can capture and stabilise unusual conformations of the protein. If these rare conformations have a biologically relevant eff ect, and the antibody binds outside of the ligand binding domain of the target, the antibody may be described as allosteric. This talk will detail methods of discovering allosteric antibodies, and employ two case studies to detail how they may be used to accelerate traditional small molecule drug discovery or be leveraged as therapeutics.

In recent years, questions about the sustainability of the current drug discovery process have triggered a revival of interest in phenotypic drug discovery approaches. This trend has clearly been amplifi ed by the emergence of multiple cell-based assay technologies enabling a higher degree of translatability between in vitro conditions and physio-pathological situations, including induced pluripotent stem cells, three-dimensional models, co-culture and organ-on-a-chip systems, complemented by advances in gene editing technologies. Progress in High-Content Screening technology contributed to the recent excitement for phenotypic drug discovery approaches, bringing image-capture and processing, and data-analysis, to a level of content and throughput fully compatible with large scale drug discovery eff orts. This presentation will highlight the eff orts currently undertaken at Servier to move High-Content Screening into the fourth dimension, taking advantage of various technological developments including deep neuronal network approaches.

JEAN-PHILIPPE STEPHAN, Director SERVIER Center of Excellence Pharmacological Screening, Compound Management and Biobanking,Institut de Recherches SERVIER

The optimisation trajectory of hit to lead to candidate is the most expensive part of drug discovery. Exscientia’s drug discovery platform brings that cost down signifi cantly by combining the strengths of AI compound design and human strategic thinking into the Centaur ChemistTM. A high level overview of the technology is presented and results are shown from successful collaborations that resulted in the delivery of clinical candidates in less than a year.

MARTIN REDHEAD, Group Leader Molecular Pharmacology,UCB

WILLEM VAN HOORN, Chief Decision Scientist,Exscientia Ltd

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R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY ONE: 11 JUNE

DRUG DISCOVERY INNOVATION AND STRATEGIES

PHENOTYPIC SCREENING IN DRUG DISCOVERY AND HIGH CONTENTSCREENING TOOLS

Conference Room: Hall II Conference Room: Salon 2

STREAM

1

STREAM

2

Delegates are welcome to attend the co-located presentations

14:50-

15:20

ZeCardio & ZeGenesis: Innovative Zebrafi sh Platforms For Cardiovascular Assessments And Generation of CRISPR/Cas9 Models

Accelerate Drug Discovery With Organ-On-A-Chip: The Mimetas Playbook

In Silico Lead Optimization Via Rapid Exploration Of Synthetically Tractable Chemical Space With Combined Free Energy And Machine Learning Approaches

• The powerful zebrafi sh model• Diff erent capabilities and activities of ZeClinics• Description of ZeCardio platform for the evaluation of

cardiovascular Tox, Target Validation and CV disease modelling

• Description of ZeGenesis platform for the generation and phenotyping of CRISPR/Cas 9 genetic models

• How Mimetas is revolutionizing the drug discovery pipeline

• How you can speed-up the preclinical phase while saving money using organ-on-a-chip

• How to predictably create 3D tissue models that produce reliable results

• Improving or maintaining the potency of lead compounds, while simultaneously optimizing multiple other properties required for safety and biological effi cacy, is a primary objective of lead optimization in small molecule drug discovery. A series of computational techniques have recently become available to aid in these tasks. We will discuss how predictive free energy calculations, synthesis-aware compound enumeration and next-generation machine learning techniques can rapidly accelerate the identifi cation, under realistic conditions, of chemical matter that fulfi lls appropriate property constraints

• Specifi cally, we will recount how the Pathfi nder enumeration workfl ow, FEP+ binding free energy calculations and DeepChem machine learning models have been combined to rapidly generate and profi le a library of novel compounds, based on commercially available building blocks, to explore both R-group and core-hopping modifi cations of an initial CDK2 inhibitor. The entire workfl ow provides a library of high-affi nity, novel CDK2 inhibitors at a high enough throughput to positively impact pharmaceutical industry project timelines. Surprisingly, only a small fraction of the suggested cores had existing matches in BindingDB, despite featuring typical kinase hinge binding features and being achievable by straightforward synthesis. This indicates that exhaustive mining of easily accessible chemical space is typically not done in drug discovery today, even in a highly explored target class like kinases

• Overall, it appears that the combination of the complementary computational techniques of binding free energy calculations, machine learning and compound enumeration off ers huge synergistic eff ects. We will present evidence that a true de novo computational design solution benefi ting from these advances is now feasible

DAVIDE RUBBINI, R&D CNS Scientist,ZeClinics

PAUL VULTO, Chief Executive Offi cer,MIMETAS

THOMAS STEINBRECHER, Director, Applications Science, Europe, Schrödinger

15:20-

16:20

Exhibition Area: Hall IAfternoon Coff ee & Refreshments, One To One Meetings x3, Poster Presentation Sessions

16:20-

16:50

High Throughput Selection Of Peptides With Biological Function

Can AI Help Us In Drug Discovery? Machine Learning Models For ADME Optimisation

• Peptide therapeutics combine the benefi ts of small molecules and larger biologics

• Identifying peptides when no natural peptide exists requires display technology

• Next generation display can be used to fi nd novel, functional hits

• Using next generation display to screen GPCRs and T-cell receptors

• How AI is currently being applied?• What predictive tools do we need to build? • What data sets do we need?

• A machine learning prediction model for P-gp effl ux ratio of small molecules is implemented for compound design

• Feature selection prior to model building helped to improve model performance

• Cross-validation Cohen kappa score is used to assess model performance

• Support Vector Machine (SVM) performed best for prediction of P-gp substrates for our datasets

ALEX BATCHELOR, Chief Executive Offi cer,Orbit Discovery

YOLANDA CHONG, Senior Vice President, Biology,Recursion Pharmaceuticals

GOVINDA BHISETTI, Principal Investigator and Head of Computation Chemistry,Biogen

16:50-

17:20

Exploring Strong Inter-Species Diff erences In Tissue Distribution – Case Study With A Basic Lipophilic Compound

Streamlining Clinical Development Through Artifi cial Intelligence

Considerations And Challenges Of Applying Deep Learning In Drug Discovery

• Strong species diff erences in preclinical in vivo PK often impairs human PK prediction

• Discussion of approaches to generate mechanistic understanding of distribution diff erences

• Presentation of novel assays and tools to improve understanding of the compound behavior

• AI technologies have the potential to challenge the ineffi cient status quo of Clinical Development

• Targeting the current challenges of data analysis technologies, Berg developed a data-driven and data-agnostic AI technology that can be applied from Drug Development to Health IT

• We will discuss use cases where Berg AI technology, bAIcis®, was successively implemented in the discovery of new Drug Targets and Clinical Trials optimization

A brief discussion about:• Considerations and application domain of deep learning

(DL) for medicinal chemistry questions• Challenges in the application of DL in prospective drug

design projects• Some learnings from within AstraZeneca

PHILIP LIENAU, Senior Research PK Scientist,Bayer

GREG MILLER, Principal Data Scientist, BERG Health

CHRISTIAN TYRCHAN, Team Leader Computational Chemistry,AstraZeneca

DRUG DISCOVERY INNOVATION AND STRATEGIES

PHENOTYPIC SCREENING IN DRUG DISCOVERY AND HIGH CONTENT SCREENING TOOLS

DISCOVERY CHEMISTRY: MEDICINAL AND COMPUTATIONAL CHEMISTRY

Conference Room: Hall II Conference Room: Salon 2 Conference Room: Salon 4

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R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY ONE: 11 JUNE

Stream Chair: Martin Redhead, Group Leader Molecular Pharmacology, UCB

Stream Chair: JEAN-PHILIPPE STEPHAN, Director SERVIER Center of Excellence Pharmacological Screening, Compound Management and Biobanking, Institut de Recherches SERVIER

Stream Chair: JOHANNES OTTL, Director, Novartis Institutes for BioMedical Research, Chemical Biology & Therapeutics, Chemical Genetics

17:20-

17:50

Accelerating Academic Drug Discovery Through Public-Private Partnerships

Designing Molecules With Machine Intelligence

Development Of Small Molecule Inhibitors Of IL-17A/IL-17AF Identifi ed From DNA Encoded Libraries

• Many discoveries in life sciences have academic origins. However, these discoveries get lost in translations due to challenges academic innovators face

• Proof-of-concept centers through public-private partnerships can help to accelerate the transition of discoveries into commercially viable therapeutics, examples of such partnerships will be discussed

• Bringing industry expertise and rigor, skin-in the game from stake holders and education/skills development for the academic innovators can make this possible

• Applications of constructive machine learning to de novo small molecule and peptide design

• Scaff old hopping from natural products to synthetic compounds with artifi cial intelligence

• Reaction-based compound design with neural networks

• Designing DNA encoded Libraries• Identifi cation of IL-17A Blockers • Structural Insights of IL-17A/A Binding • Biophysical Validation of IL-17A Blockers• Characterisation of Key IL-17A Blockers • Proof of concept studies using IL-17A Blockers

SUGUNA RACHAKONDA, Senior Director, Product Development, Cleveland Clinic

GISBERT SCHNEIDER, Professor,ETH Zürich

GARRICK SMITH, Project Manager,Nuevolution

17:50-

18:20

Transforming Early Innovation Into Therapeutic Solutions; The SEED Model

Data-Driven Structure-Based Drug Discovery

Advances In DNA-Encoded Library Technology Platforms: YoctoReactor And Binder Trap Enrichment

• Innovative biology, modalities, technologies and business models are critical components of drug discovery in 2019; examples of implementation at Sanofi will be presented

• De-risking early innovation from academia/biotech with drug discovery partners is the basis of the SEED model

• SEED concept, project portfolio and examples will be commented

• Protein structure-based design off ers a unique way of creating innovative bioactive compounds. Data quality estimation and automated processing tools are the prerequisites for machine-learning based approaches

• The growing amount of structures available can off er new opportunities of gaining knowledge for compound design. Novel database concepts with easy-to-use interfaces are the key for enabling medicinal chemists to mine this data

• Machine learning methods grep every signal correlating with the desired output in training data. New validation strategies are required to estimate the true value of novel approaches

• Nanomolar inhibitor of complex multi-subunit protein structure

• High fi delity DNA-encoded library synthesis• Homogenous screening assay • Low false positive rate

PATRICK JIMONET, Director, External Innovation in Drug Discovery, Sanofi

MATTHIAS RAREY, Professor,University of Hamburg / Center for Bioinformatics

NILS JAKOB VEST HANSEN, Chief Executive Offi cer,Vipergen ApS

18:20-

18:50

A Novel Human Intrinsically Disordered Protein Domain To Improve The Drug-Like Properties Of A Lysosomal Enzyme

Panel Discussion: The Real Measurable Outcomes Of AI/ML In Drug Discovery And Drug Design

Encoded Library Technologies As Integrated Lead Finding Platforms For Drug Discovery

• Sobi has created a platform to improve the drug-like properties of biotherapeutics by creating fusion proteins with a human intrinsically disordered protein domain (rh-IDPD)

• Lysosomal enzymes benefi t from the fusion with the rh-IDPD by decreased receptor engagement that alters the distribution of the enzyme and improves the plasma half-life

Panel Moderator: YOLANDA CHONG, Senior Vice President, Biology, Recursion Pharmaceuticals

Panellists Include:

BRANDON ALLGOOD, Chief Technology Offi cer, Numerate, Inc

RICHARD LEWIS, Global Head CADD, Novartis

The scope of targets investigated in pharmaceutical research is continuously moving into uncharted territory. Consequently, fi nding suitable chemical matter with current compound collections is proving increasingly diffi cult. Encoded library technologies enable the rapid exploration of large chemical space for the identifi cation of ligands for such targets. These binders facilitate drug discovery projects both as tools for target validation, structural elucidation and assay development as well as starting points for medicinal chemistry. Novartis internalized two complementing encoded library platforms to accelerate the initiation of its drug discovery programs. For the identifi cation of low-molecular weight ligands, we apply DNA-encoded libraries. In addition, encoded peptide libraries are employed to identify cyclic peptides. This review discusses how we apply these two platforms in our research and why we consider it benefi cial to run both pipelines in-house.

ERIK NORDLING, Principal Scientist, Biomedical Science & Portfolio Innovation,Swedish Orphan Biovitrum AB

JOHANNES OTTL, Director,Novartis Institutes for BioMedical Research, Chemical Biology & Therapeutics, Chemical Genetics

18:50-

19:20

Medicines Discovery Catapult: A New Model For Collaborative R&D

High Content Phenotypic Screening Increases The Translational Impact Of Academic Biological Research

Encoded Self-Assembling Chemical (ESAC) Libraries

• The aim of Medicines Discovery Catapult is to work collaboratively with all sectors of the UK medicines discovery industry, helping SME biotechs, academics and innovators to access the knowledge, data, technologies and networks they need to progress their R&D programmes faster and more cost-eff ectively

• In this talk I will describe how we develop new collaborative business models to enable life science entrepreneurs deliver their projects through external networks of best-in-class R&D partners and service providers

• I will make reference to Outsourcing And Partnerships In Drug Discovery; Novel Collaboration Business Models; Public-Private Collaborations

• Modern High Content Phenotypic Screening (HCS) exploits exciting new developments in cell-based models of human diseases and new assay screening technologies. By reproducing complex characteristics of healthy and diseased human cells in vitro, HCS off ers a route to discover drugs that act on the diseased cells specifi cally and promises a higher probability of translational success compared to contemporary reductionist drug discovery strategies

• The academic and clinical research communities have much to off er HCS including development of new disease-relevant assays, novel cell and tissue-based screening technologies and complex mechanism-of-action and target deconvolution approaches

• We present exemplars of HCS programmes that demonstrate the therapeutic value of novel disease relevant phenotypic screening assays sourced from the academic community www.npsc.ac.uk

• DNA-Encoded chemical libraries are used for the discovery of ligands against protein targets of interest

• As an application, DNA-encoded chemistry improves chemotherapy with the discovery of ultra-high binding affi nity ligands for effi cient targeting (e.g. tumor targeting)

• Opportunities for cancer imaging, drug delivery

SARAH BROCKBANK, Lead Scientist - Virtual R&D,Medicines Discovery Catapult

DENISE BARRAULT, Executive Director,NPSC

FLORENT SAMAIN, Research Scientist,Philochem

19:20Exhibition Area: Hall I

Networking Drinks & End Of Day One

R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY ONE: 11 JUNE

DRUG DISCOVERY INNOVATION AND STRATEGIES

PHENOTYPIC SCREENING IN DRUG DISCOVERY AND HIGH CONTENT SCREENING TOOLS

DISCOVERY CHEMISTRY: MEDICINAL AND COMPUTATIONAL CHEMISTRY

Conference Room: Hall II Conference Room: Salon 2 Conference Room: Salon 4

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R&D SERIES EUTHINK TANK ROUNDTABLE DISCUSSIONS AND BREAKFAST

Conference Room: Hall II

08:00

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08:30

DRUG DISCOVERY SUMMIT DISCOVERY CHEMISTRY& DRUG DESIGN CONGRESS

BIOLOGICS AND SMALL MOLECULE DRUG TARGET DISCOVERY FOR IMMUNO-THERAPY, AUTOIMMUNE DISEASE AND ONCOLOGY

INNOVATION IN GENOME AND CELL BASED DRUG DISCOVERY, SCREENING, IMAGING & TARGET DISCOVERY

MEDICINAL CHEMISTRY AND DRUG DESIGN: NOVEL APPROACHES

Conference Room: Hall II Conference Room: Salon 2 Conference Room: Salon 4

Stream Chair: RUUD JORNA, Regional Business Manager LTG, Luminex Corporation

Stream Chair: TAMARA MAES, Chief Scientifi c Offi cer, Oryzon Genomics

Stream Chair: MARKUS KOSSNER, Scientifi c Services Manager, Chemical Computing Group

08:30-

09:00

Keynote Address: Leveraging Synthetic Modality Innovations To Probe Key Nodes In Cancer & Immune Cells

Keynote Address: Development Of LSD1 Inhibitors, From Bench To Bedside

Keynote Address: Oral Peptide-Based Macrocycle Antagonists Of Integrin α4β7 For The Treatment Of Infl ammatory Bowel Disease

• Impact of synthetic modalities in cancer drug discovery• Using chemical probes in cancer target validation:

Generating value instead of noise• Quality criteria for chemical probes & open innovation

approaches• Importance of combining diverse lead fi nding

technologies to identify valid starting points• Case studies: probing epigenetic reader ATAD2, PPI Ras/

SOS & metabolic immune switch AhR

• Mechanism of LSD1 inhibition • Biological impact of LSD1 inhibition• Therapeutic activities of LSD1 inhibition

• T cell traffi cking to the gut initiates mucosal infl ammation in the intestine, a hallmark of Infl ammatory Bowel Disease (IBD). Legacy and current agents for IBD have provided clinicians with eff ective treatment options comprised largely of biologics, including vedolizumab (Entyvio®), a monocolonal antibody targeting integrin α4β7

• Orally available agents that can mitigate shortcomings in low colon perfusion, loss of response or extra-intestinal adverse events would provide attractive alternatives

• Encycle Therapeutics conducted a discovery campaign starting from linear peptide ligands of integrin α4β7 and applied proprietary macrocyclization chemistry to create novel antagonists

• Several compounds exhibit a balanced gut-plasma exposure profi le, exclusion of α4β7+ memory T helper cells from gut-associated lymphoid tissues and persistent suppression of disease mechanisms

• Key features of the medicinal chemistry optimization will be presented

INGO HARTUNG, Vice President of Medicinal Chemistry,Bayer

TAMARA MAES, Chief Scientifi c Offi cer,Oryzon Genomics

ANDREW ROUGHTON, Vice President Discovery & Operations,Encycle Therapeutics

09:00-

09:30

Stream Keynote Address: Development Of Antibody-Drug-Conjugates To Novel Embryonic Targets In Cancer

Stream Keynote Address: The View From Industry: How Can Genetics Inform Drug Development?

Stream Keynote Address: The Challenges Of Prosecuting RNA-Modifying Enzymes As Drug Discovery Targets

• Metastatic and aggressive cancers caused by cellular reprogramming to generate primitive malignant cells with embryonic properties

• CureMeta develops novel high specifi c and high affi nity antibodies to embryonic targets not expressed in normal tissues but re-expressed in cancers

• CureMeta develops novel therapeutic antibody-drug-conjugates to treat patients with aggressive and metastatic cancers

• Identifi cation of novel drug targets• Strengthen construct validity of models and assays• Facilitate segmentation of patient populations• It is key to translate genetic variance to biological

consequence

RNA epigenetics is an unexplored and exciting fi eld for drug discovery. While post-transcriptional RNA modifi cations have been known for over 30 years, their mechanism and functional consequences have only recently begun to emerge. Tackling new classes of enzymes such as RNA methyltransferases generates challenges in assay development, screening and downstream hit to lead progression. This talk will describe some of the challenges we have faced in prosecuting our RNA methyltransferase programmes and the techniques we have developed to meet them.

MIKE SCHOPPERLE, Chief Executive Offi cer,CureMeta

MICHAEL DIDRIKSEN, Senior Director,Lundbeck

WESLEY BLACKABY, Vice President of Chemistry,Storm Therapeutics

Table 3: Innovation In Screening

Moderator: ERIC GOEDKEN, Principal Scientist, Discovery Dermatology & Fibrosis, AbbVie

Table 1: Broadening The Chemical Space Of DNA Encoded LibrariesModerator: JOHANNES OTTL, Director, Novartis Institutes for BioMedical Research, Chemical Biology & Therapeutics, Chemical Genetics

Table 2: New Approaches To Therapeutic Discovery In Oncology

Moderator: JAMES PRUDENT, President & Chief Executive Offi cer, Centrose

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R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY TWO: 12 JUNE

R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY TWO: 12 JUNE

BIOLOGICS AND SMALL MOLECULE DRUG TARGET DISCOVERY FOR IMMUNO-THERAPY, AUTOIMMUNE DISEASE AND ONCOLOGY

INNOVATION IN GENOME AND CELL BASED DRUG DISCOVERY, SCREENING, IMAGING & TARGET DISCOVERY

MEDICINAL CHEMISTRY AND DRUG DESIGN: NOVEL APPROACHES

Conference Room: Hall II Conference Room: Salon 2 Conference Room: Salon 4

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09:30-

10:00

Enabling Data Workfl ows Across External Collaborations And Partnerships

Make It Cyclic: A Paradigm For The Discovery Of Selective Kinases Inhibitors “Nanocyclix”

• All partners in a research collaboration must be able to share data and participate in cross-organization workfl ows

• A scientifi c collaboration and data exchange environment is critical to ensure these partnerships are successful & effi cient

Cyclization in drug discovery is a growing paradigm. We have developed an Integrated Drug Discovery platform Nanocyclix to synthesize small libraries of macrocycles and design specifi c molecules through SBDD to identify new kinases inhibitor. Nanocyclix molecule are in the drug-like space and display nM potencies and good selectivity across the kinome. Nanocyclix paradigm will be exemplifi ed at the level of H2L and beyond in Oncology and Immuno-infl ammation to illustrate the value and potential of the cyclization approach.• Integrated Drug Discovery • Medicinal chemistry technology Nanocyclix based on

macrocyclization of small Lead-like molecules • Kinase-focused library designed to identify attractive and

selective kinases inhibitor • Macrocyclization paradigm of known hinge binder scaff olds

resulting in tighter binding site recognition, potency and selectivity towards the ATP site.

• Examples of Nanocyclix in several indications ranging from Oncology to Immuno-infl ammation, and Imaging

ROB BROWN, Vice President, Global Informatics,Dotmatics

ALEXIS DENIS, Director Discovery Medicinal Chemistry,Oncodesign

10:00-

11:20

Exhibition Area: Hall IMorning Coff ee & Refreshments, One To One Meetings x4, Poster Presentation Sessions

11:20-

11:50

PROTAC: An Innovative New Modality In Drug Discovery

Functional Genomics In Drug Discovery: Applications And Potential

Fragment-Based Discovery Of Selective JAK1 Inhibitors

• Proteolysis targeting chimeras (PROTACs) are hetero-bifunctional small molecules. which simultaneously bind target proteins and E3 ubiquitin ligases forming a ternary complex. This induced spatial proximity results in ubiquitination of the target protein, leading to its recognition and subsequent degradation by the ubiquitin proteasome system

• PROTACs off er several potential advantages over small molecule inhibitors, including the potential for reduced dose as a result of their catalytic mechanism of action, extended duration of action arising from the rate of protein re-synthesis, and additional pharmacology through complete removal of the protein

• One of the challenges of the PROTAC technology is in the identifi cation and validation of suitable targets that can deliver truly diff erentiated medicines. In this talk, we will present case studies from our recent eff orts on developing PROTACs for RIPK2, and demonstration of diff erentiated biological eff ects of PCAF PROTACs over small molecule inhibition

• Applications in novel target identifi cation and validation• Using functional genomics to improve disease

understanding• Future developments and directions

We report the discovery of a series of JAK1-selective kinase inhibitors with high potency, excellent JAK family subtype selectivity and promising in vitro and in vivo pharmacokinetic properties. A fragment screening hit with moderate potency and selectivity was elaborated into a lead compound by two stages of fragment growth. First, we optimized a lipophilic moiety appended to the fragment core. We then introduced and optimized a polar substituent to modulate solubility and lipophilicity while adding affi nity and selectivity for JAK1.

AFJAL MIAH, Investigator, Medicinal Chemistry, Protein Degradation,GlaxoSmithKline

LAUREN DROWLEY, Director, Head Functional Genomics,UCB Pharma

ANDREAS RITZÉN, Senior Principal Scientist,Leo Pharma A/S

11:50-

12:20

Investigating Key Steps In PROTAC-Mediated Cellular Protein Degradation

Fragment Library Design; Quantitative Analysis Of Molecular Shape And Functionality

PROTACs induce selective protein degradation by chemically linking a protein target with an the E3 ubiquitin ligase component, initiating degradation of the protein target via the ubiquitin-proteosome system (UPS). Interrogating the key steps required for eff ective PROTAC-mediated target protein degradation remains a challenge, particularly in cells.In this talk, we will present the NanoLuc® platform technology suitable for live cell studies to answer the key questions in PROTAC research: • Is my target protein degraded?• Does my PROTAC enter the cell and bind to the target

protein or E3 component?• Does my PROTAC form a ternary complex with its target

and the E3 recruiter?• Is my target protein ubiquitinated?• Is my target protein traffi cked to the proteasome?

This presentation introduced the development of a new parameter that guides considerations of vector space within the fragment library design process. This quantitative parameter measures the vector space coverage of the key functionalities (e.g. HBD’s, HBA’s, lipophilic groups) within a fragment library. Optimally designed libraries achieve the broadest coverage of vector space from the smallest number of compounds.

This is an open innovation project between Liverpool ChiroChem, The University of Liverpool and Abbvie. The results are to be published in a high-impact cheminformatics journal, making ‘Vector Effi ciency’ a freely accessible parameter to be easily adopted by the medicinal chemistry community using widely available computational software.

RICHARD SOMBERG, Director Pharma Biotech,Promega Corp.

PAUL COLBON, Chief Executive Offi cer,Liverpool ChiroChem

Delegates are welcome to attend the co-located presentations

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY TWO: 12 JUNE

BIOLOGICS AND SMALL MOLECULE DRUG TARGET DISCOVERY FOR IMMUNO-THERAPY, AUTOIMMUNE DISEASE AND ONCOLOGY

INNOVATION IN GENOME AND CELL BASED DRUG DISCOVERY, SCREENING, IMAGING & TARGET DISCOVERY

MEDICINAL CHEMISTRY AND DRUG DESIGN: NOVEL APPROACHES

Conference Room: Hall II Conference Room: Salon 2 Conference Room: Salon 4

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12:20-

12:50

Case Study Of Targeted Protein Degradation For Immune-Oncology Program, IRAK-M Degrader

Human Engineered Heart Tissue – An Innovate Model For Preclinical Cardiac Assessment

Fragment-Based Drug Discovery At Lilly - Bridging Fragment And Lead Chemical Spaces

• IRAK-M degraders based on proprietary XIAP binders showed in vivo effi cacy in mouse syngeneic model

• Lead optimization from lead degrader compounds was completed within 1 year based on platform technology RaPPIDS(TM)

• Generation and automated contractility analysis of human human EHT

• Maturation of hiPSC-CM in human EHT model• Examples to characterise inotropic, pro-arrhythmic and

cardiotoxic compounds

• Starting FBDD at Lilly Fragment Hits Expansion• Strategies The Bridge library• A concept for Expansion Lilly Fragment Hit Expansion

procedure: Rialto examples of Rialto applications

YUSUKE TOMINARI, Chief Executive Offi cer / Chief Scientifi c Offi cer,FIMECS, Inc.

ARNE HANSEN, Professor,University Medical Center Hamburg-Eppendorf (UKE)

JOSE A. MARTINEZ PEREZ, Principal Research Scientist, Discovery Research & Technologies,Eli Lilly

12:50-

13:50

Exhibition AreaLunch, One To One Meetings, Poster Presentation Sessions

Stream Chair: RUUD JORNA, Regional Business Manager LTG, Luminex Corporation

Stream Chair: TAMARA MAES, Chief Scientifi c Offi cer, Oryzon Genomics

Stream Chair: GUIDO KIRSTEN, Principal Scientist, Chemical Computing Group

13:50-

14:20

Methods For Kinetic Assessment Of High Affi nity EZH2 Inhibitors: Identifi cation Of A 2nd Generation Of EZH2i With Improved Biological Activity And Extremely Long Residence Times

Patient-Derived Organoids For Development And Discovery Of Oncology And Immuno-Oncology Drugs

Unique Insights Into GPCR Allosteric Modulators Through The Application Of Orthogonal Techniques Spanning Multiple Timescales

• Development of biochemical assays to quantify high affinity, long residence time interactions

• EZH2i modifications leading to high affinity, long residence time antagonists

• Cellular and in vivo characterization of 2nd Generation EZH2 inhibitors

• HUB Organoid technology is based on the identifi cation of adult stem cells in many human tissues

• Patient-derived organoids are suitable for performing large scale screens

• We have now developed a novel system that allows the co-culture of organoids with immune cells to study the eff ect of immune modulating drugs

Many G-protein coupled receptors crystal structures have been solved in recent years. Such structures can be exploited to support drug discovery endeavors. However, they can be of limited utility if one is interested in studying ligands that bind to a state or pocket that is not captured in the available target structure(s). In this talk I will present how we are using advanced molecular dynamics simulations, in combination with orthogonal experimental techniques, to map conformational landscapes and allosteric binding sites for GPCR targets of therapeutic relevance. This has enabled us to elucidate novel insights into the modulation of GPCR targets by allosteric compounds.

JACOB STUCKEY, Senior Scientist, Constellation Pharmaceuticals

SYLVIA BOJ, Scientifi c Director,Hubrecht Organoid Technology

ZARA SANDS, Principal Scientist, Medicinal Chemistry,UCB BioPharma

14:20-

14:50

Identifying Biologics With Specifi c Mechanisms Of Action

Advances In CRISPR For Target Validation And Cellular Model Development

• There are many important properties to consider when isolating and selecting leads in early antibody drug discovery. These include; function, potency, specifi city, selectivity, affi nity and developability. Assays and screening cascades can be designed at the project outset to triage thousands of antibodies for these desired properties

• While screening for function early is paramount, it is also important to understand the mechanism of action through which an antibody drug mediates its functional eff ects (e.g. competitive, non-competitive, allosteric), to ensure that maximal target suppression can be achieved in vivo

• Using case studies, this presentation will highlight strategies and learnings in identifying antibody biologics with the desired mechanism of action

• Use of CRISPR for improved Target Validation • CRISPR editing in primary immune cells

FRANCES NEAL, Scientist 1,AstraZeneca

JENNA BRADLEY, Senior Research Scientist,AstraZeneca

14:50-

15:20

Exhibition Area: Hall IAfternoon Coff ee & Refreshments, Poster Presentation Sessions

15:20-

15:50

The Next Giant Steps In Immuno-Oncology Targeted Action Of Epigenetic Drugs From Softdrugs And Prodrugs

Tackling Protein-Protein Interactions (PPIs) Through Stabilisation Of Desired Conformations of Target Proteins. The Discovery Of Small Molecule Inhibitors Of TNF

• Active Checkpoint Control Immunotherapy is better than Nobel Prize winning passive checkpoint inhibition

• Naturally induced polyclonal antibodies are superior to Nobel Prize winning monoclonal antibodies that invariably lead to anti-drug antibodies against the foreign mAb and allow tumour escape

• We take the brakes off better and put down the accelerator better and in a safer and more eff ective manner with only one product instead of combining checkpoint inhibiting and coreceptor upregulating monoclonal antibodies

• Inhibitors of epigenetic targets (histone deacetylases and demethylases)

• Application of soft-drug and prodrug principles to epigenetic inhibitors

• Many proteins are dynamic and readily switch between both signalling and non-signalling conformations

• Here we report the discovery of orally available small molecule inhibitors of TNF that stabilise a naturally sampled, non-signalling conformer of the protein by binding to an allosteric, cryptic site

• These compounds may provide alternatives to the highly successful biologics against TNF in diseases such as RA, Crohn’s and psoriasis

• Stabilisation of inactive conformers may prove to be a general method of drugging protein interfaces using traditional non-peptide based medicinal chemistry

FRED JACOBS, Chief Executive Offi cer and Co-Founder,TYG Oncology

MANFRED JUNG, Professor,Freiburg University

JAMES O’CONNELL, Director, Structural Biology,UCB

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Drug Discovery and Discovery Chemistry & Drug Design DAY TWO: 12 JUNE

15:50-

16:20

Highly Potent And Selective Tumour Targeting Bicyclic Peptides: A Novel Approach To Cancer Therapy

High-Throughput Functional Genomics Using Single Cell Approaches

deepScaff Opt: Ligand Scaff old Optimization Guided By Artifi cial Intelligence

• Bicycle Therapeutics are pioneering the development of bicyclic peptides, or Bicycles® — a new class of versatile, chemically synthesised medicines

• Bicycle Toxin Conjugates link a potent toxin payload to a Bicycle designed to bind to a tumour surface antigen

• This targeted approach rapidly delivers payloads into solid tumours, with extensive tissue penetration, a short duration of systemic exposure and liver-sparing rapid renal elimination. These properties limit the body’s exposure to toxin to control any damage to normal tissue

• SC CRISPR coupled to transcriptional readouts: a novel approach for functional genomics and target ID

• SC approaches to delineate mechanisms behind lineage fate decisions in myeloid iPSC cell models

• SC approaches for deconvolution of ‘black box’ phenotypic screens

• Overview of deepScaff Opt algorithm for highly accurate, 1-sec fast binding affi nity prediction with minimal human input

• deepScaff Opt, which uses only ligand 2D-structure, achieved top performance in the latest D3R Challenges, surpassing the vast majority of 3D- and 2D-methods

• deepScaff Opt evidently outperforms the widely used Free Energy Perturbation method for scaff old optimization

• Preview of our new (i) corrected quantum chemical free energy method for ligand binding and affi nity prediction, (2) protein structure determination algorithm from only two 4D-NMR spectra

GEMMA MUDD, Senior Scientist,Bicycle Therapeutics

DAVID BRIERLEY, Team Leader,GlaxoSmithKline

THOMAS EVANGELIDIS, Research Scientist, Institute of Organic Chemistry & Biochemistry of the Czech Academy of Sciences

BIOLOGICS AND SMALL MOLECULE DRUG TARGET DISCOVERY FOR IMMUNO-THERAPY, AUTOIMMUNE DISEASE AND ONCOLOGY

MEDICINAL CHEMISTRY AND DRUG DESIGN: NOVEL APPROACHES

Conference Room: Hall II Conference Room: Salon 4

16:20-

16:50

Target Engagement In Vivo - The Role Of Drug-Target Binding Kinetics In The In Vivo Context

The Convoluted Journey Of An ERK2 Fragment Series (With A HTS Detour)

The presentation will deal with examples on how and when the association rate constant (Kon) and dissociation rate constant (koff ) value may infl uence: • The duration of target occupancy in vivo• The selectivity for the therapeutic target compared to a secondary target in vivo• Will determine binding kinetics of drug in the presence of an endogenous ligand in vivo

ERK1/2 represent an essential downstream node in the Ras/Raf/MEK/ERK (MAPK) signal transduction pathway, and have attracted signifi cant interest as a potential anticancer target. Both fragment and high-throughput screening were carried out in parallel to discover novel ERK1/2 inhibitors. In this presentation I will discuss the journey of a fragment-based series along with how learnings from the fragment series were incorporated into the HTS-derived series which led to a clinical candidate GDC-0994.

ELIZABETH DE LANGE, Professor Predictive Pharmacology,LACDR - Division of Systems Biomedicine and Pharmacology

HUIFEN CHEN, Senior Scientist, Computational Drug Design,Genentech, Inc.

16:50-

17:20

Profi ling Of Immunomodulatory Receptor Protein Interactions Via Photoactivation-Based Proximity Labeling Of The Cell Surface

Histone Deacetylase (HDAC) Enzymes And Macrocyclic Peptides

• Proximity labeling is an emerging powerful method to profi le protein-protein interactions at the cell surface

• We will present a novel, small molecule-based photoproximity labeling method termed PROPEL that allows protein labeling in a temporal, spatially-controlled manner and is applicable to any cell type

• Human HDAC enzymes cleave diverse acyl-lysine modifi cations• Macrocyclic peptides constitute a class of modular HDAC inhibitors• HDAC inhibitors exhibit their eff ect with diff erent kinetics

TAMARA REYES ROBLES, Senior Scientist,MSD

CHRISTIAN ADAM OLSEN, Professor, Center for Biopharmaceuticals and Department for Drug Design and Pharmacology, Faculty of Health and Medical Sciences,University of Copenhagen

17:20 End Of Conference

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BIOLOGICS AND SMALL MOLECULE DRUG TARGET DISCOVERY FOR IMMUNO-THERAPY, AUTOIMMUNE DISEASE AND ONCOLOGY

INNOVATION IN GENOME AND CELL BASED DRUG DISCOVERY, SCREENING, IMAGING & TARGET DISCOVERY

MEDICINAL CHEMISTRY AND DRUG DESIGN: NOVEL APPROACHES

Conference Room: Hall II Conference Room: Salon 2 Conference Room: Salon 4

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New for 2019, the Bispecifics in Discovery & Development Congress features 2 interactive streams, which include over 20 presentations, case studies and panel discussions focused on the key issues in the industry today:

BISPECIFICS: AGENDA AT A GLANCE BISPECIFICS: AGENDA AT A GLANCE

DAY ONE: 11 JUNE

BISPECIFIC DISCOVERY, THERAPEUTIC DEVELOPMENT AND DEVELOPABILITY CONSIDERATIONS

PRECLINICAL DEVELOPMENT, TRANSLATION AND CLINICAL DEVELOPMENT IN BISPECIFIC ANTIBODIES

Targeting Solid or Liquid Tumors - Novel Discovery and Platforms

T-Cell Re-direction and T-Cell-engaging Molecules

Antibody design in Bispecifics – Antibody Engineering

Validating Novel Applications

Enhancing Product Developability

Tri-Specific and Multispecific – Future Opportunities and Therapeutic Potential

Panel Discussion – Designing More Than One Specificity

• Choosing the Platform - Exosome and Nanobody Platforms

Immunogencity, Aggregation, Safety and Toxicity Considerations

Implementing Developability Processes and Maximize Clinical Performance

Biomarker Analysis and Translation

Clinical Development of Bispecific

• Bispecific Antibodies and Antibody-Drug Conjugates

• Bispecifics and Multi-Specifics

Case studies of Bispecific Clinical Development in Different Therapeutic Areas

• Immuno-Oncology, Metabolic Diseases and Infectious Diseases, Autoimmune Disease

Taking Bispecific to the Clinic

Panel Discussion – Clinical Development of Bispecific In Liquid And Solid Tumors

DAY TWO: 12 JUNE

DAY 1BISPECIFICS DISCOVERY, THERAPEUTIC DEVELOPMENT AND DEVELOPABILITY CONSIDERATIONS

DAY 2PRECLINICAL DEVELOPMENT, TRANSLATION AND CLINICAL DEVELOPMENT IN BISPECIFIC ANTIBODIES

JOHN DELANEY

Executive Director, Research Amgen

BENNO RATTEL

Executive Director Research Amgen Research (Munich) GmbH

MARTIN BADERHead of Biochemical and Analytical Research Roche

JAMES BALKOVEC

Senior Research Advisor Cidara Therapeutics, Inc

BRYAN GLASER

Vice President of Research Invenra Inc.

NATHAN TRINKLEIN

Chief Technology Officer Discovery Teneobio

EUGENE ZHUKOVSKY

Chief Scientific Officer Biomunex

ANTONIN DE FOUGEROLLES

Chief Executive Officer Evox Therapeutics

SIMON PLYTE

Vice President Immuno-Oncology Merus

TEEMU JUNTTILA

Senior Scientist, Translational Oncology Genentech

CHRISTOPHE BLANCHETOT

Director Discovery Argenx BVBA

MIHRIBAN TUNA

Senior Vice President, Drug Discovery F-Star

MATHIEU CINIER

Scientific Director Affilogic

MATTHIAS BROCK

Group Leader Pharmacology Numab

KRZYSZTOF MASTERNAK

Head of Biology Novimmune

NINA E. WEISSER

Principal Scientist Zymeworks Inc.

07:30-

08:20Registration: Conference Floor 1 Foyer

R&D SERIES EU

08:20 Conference Room: Hall II Oxford Global Welcome Address

08:25 Chairperson’s Opening Address: MIKE DYSON, Chief Technology Offi cer, IONTAS Ltd

08:30-

09:00

Co-Located Keynote Address: Communicating Prospective Accuracy Of Human PK PD Predictions; Impact In Discovery And Early Development Of Small Molecules• Increasing accuracy and integration of PK and PD along the value chain• Point prediction Vs density plots; impact on decision making• Impact of dose predictions on optimization strategies

CARL PETERSSON, Scientifi c Director Drug Disposition,Merck KGaA

BISPECIFICS IN DISCOVERY & DEVELOPMENT CONGRESS

NOVEL STRATEGIES & TECHNOLOGIES FOR BISPECIFIC DRUG DISCOVERY

Conference Room: Salon 3

09:00-

09:30

Stream Keynote Address: The Future of Biologic Therapeutics and Their Unique Challenges

• Bispecifi c T-Cell Engagers – Discovery• Bispecifi c T-Cell Engagers - Industrialization

JOHN DELANEY, Executive Director, Research,Amgen

09:30-

10:00

Capturing Bispecifi c Antibody-Induced Modulation of the Tumor Microenvironment Using A Personalized Ex Vivo Histoculture Approach• Mitra Biotech has developed and clinically validated our fully human ex vivo platform

technology (CANscript™)• CANscript ™ uses fresh patient material (tumor, autologous ligands and PBMCs) to

explore the mechanism of action by employing customizable endpoint assays• This talk will focus on how we use CANscript to explore the eff ect of bispecifi c antibodies

and checkpoint inhibitors alone and in combination with SOC as well as oncolytic virus to answer development-critical questions

STEFAN JELLBAUER, Technical Liaison for Translational Applications,Mitra Biotech

10:00-

11:20

Exhibition Area: Hall IMorning Coff ee & Refreshments, One To One Meetings x4, Poster Presentation Sessions

11:20-

11:50

T-Cell Re-Direction Using Bispecifi c Antibodies• Discovery of new CD3 antibodies with novel function• Development of T-cell engaging bispecifi c antibodies

NATHAN TRINKLEIN, Chief Technology Offi cer,Teneobio

11:50-

12:20

12:20-

12:50

12:50-

13:50

Exhibition Area: Hall ILunch, One To One Meetings x2, Poster Presentation Sessions

13:50-

14:20

Bispecifi c Discovery And Development Platform• Generating First In Class Programme In Immuno-Oncology

SIMON PLYTE, Vice President Immuno-Oncology,Merus

Stream Chair: NATHAN TRINKLEIN, Chief Technology Offi cer, Teneobio

Delegates are welcome to attend the co-located presentations

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Bispecifics in Discovery & Development DAY ONE: 11 JUNE

14:20-

14:50

Panel Discussion - Designing More Than One Specifi city • Choosing the platform – exosome and nanobody platforms

Panel Moderator: ANTONIN DE FOUGEROLLES, Chief Executive Offi cer, Evox Therapeutics

Panellists Include:

NATHAN TRINKLEIN, Chief Technology Offi cer, Teneobio

JOHN DELANEY, Executive Director, Research, Amgen

CHRISTOPHE BLANCHETOT, Director Discovery, Argenx BVBA

MATHIEU CINIER, Scientifi c Director, Affi logic

14:50-

15:20

15:20-

16:20

Exhibition Area: Hall IAfternoon Coff ee & Refreshments, One To One Meetings x3, Poster Presentation Sessions

16:20-

16:50

Analytical Strategies For The Development Of Bispecifi c Antibodies• In-silico tools and experimental tools to assess developability • In-depth characterization of side products for bispecifi c antibodies such as T cell bispecifi cs• Functional characterization of bispecifi c antibodies during early development

MARTIN BADER, Head of Biochemical and Analytical Research,Roche

16:50-

17:20

Development Of Argenx Bispecifi c Antibodies• Specifi city• Functionality

CHRISTOPHE BLANCHETOT, Director Discovery,Argenx BVBA

17:20-

17:50

Exosome Therapeutics: A New Way To Design And Deliver Multi-Specifi c Biologics• Exosomes represents the body’s natural vesicular delivery system for proteins and nucleic acids• Evox is engineering exosomes to enable a new format of multi-specifi c biologics• Engineered exosomes also enable biologics to access hard to reach areas, such as crossing the blood brain barrier or functional delivery into the cell cytoplasm

ANTONIN DE FOUGEROLLES, Chief Executive Offi cer,Evox Therapeutics

17:50-

18:20

Multispecifi c And Multivalent Antibodies As OX40 Agonists Discovery• Introduction to the Invenra ARCHER™ technology for empirical discovery and optimization of affi nity, epitope, and architecture to generate a second generation OX40 agonist• Exploration of the in vitro characterization the Invenra lead OX40 agonist on immune cell populations• Discussion of preclinical studies using the Invenra Lead OX40 agonist

BRYAN GLASER, Vice President of Research,Invenra Inc.

18:20-

18:50

Nanofi tin-Based Multispecifi cs Platform: More Targets, Same Developability• Highlights on the Nanofi tin technology: size, modularity, stability• Use of the Nanofi tin scaff old for engineering multispecifi c molecules• Use of the Nanofi tin scaff old for the empowerment of antibodies: multispecifi city and modulation of the PK

MATHIEU CINIER, Scientifi c Director,Affi logic

18:50-

19:20

A Novel Multi-Specifi c Antibody Targeting PD-L1-Overexpressing Cancers That Stimulates Antigen-Committed CD8+ T Cells Through Concomitant Engagement Of 4-1BB• Design and development of an innovative PD-L1x4-1BBxHSA multi-specifi c antibody that exclusively induces 4-1BB signaling in the proximity of PD-L1 expressing cells and thereby directs its activity

to PD-L1 expressing tumor tissue• Greater capacity of PD-L1x4-1BB antibody to activate T cells when compared to the combination of anti-PD-L1 and anti-4-1BB IgGs ex vivo and in a humanized HCC827 xenograft mouse model• Tolerability and increased serum half-life of PD-L1x4-1BB antibody mediated by serum albumin binding domain in cynomolgus monkey

MATTHIAS BROCK, Group Leader Pharmacology,Numab

19:20Exhibition Area: Hall I

Networking Drinks & End Of Day One

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Bispecifics in Discovery & Development DAY ONE: 11 JUNE

NOVEL STRATEGIES & TECHNOLOGIES FOR BISPECIFIC DRUG DISCOVERY

Conference Room: Salon 3

R&D SERIES EU 2019THINK TANK ROUNDTABLE DISCUSSIONS AND BREAKFAST

Conference Room: Hall II

08:00

-

08:30

08:30-

09:00

Co-Located Keynote Address: Leveraging Synthetic Modality Innovations To Probe Key Nodes In Cancer & Immune Cells• Impact of synthetic modalities in cancer drug discovery• Using chemical probes in cancer target validation: Generating value instead of noise• Quality criteria for chemical probes & open innovation approaches• Importance of combining diverse lead fi nding technologies to identify valid starting points• Case studies: probing epigenetic reader ATAD2, PPI Ras/SOS & metabolic immune switch AhR

INGO HARTUNG, Vice President of Medicinal Chemistry,Bayer

BISPECIFICS IN DISCOVERY & DEVELOPMENT CONGRESSPRECLINICAL DEVELOPMENT, TRANSLATION AND CLINICAL DEVELOPMENT INBISPECIFIC ANTIBODIES

Conference Room: Salon 3

09:00-

09:30

Stream Keynote Address: Clinical Translation Of Nonclinical Assessment Of T Cell Engaging BiTE® Antibody Constructs

• T-cell engagers, commonly referred to as BiTE® antibody constructs, consist of two fl exibly-linked single-chain variable (scFv) regions, one directed against a tumor-associated antigen (TAA) and the other targeting CD3

• BiTE® antibody constructs provide an off the shelf therapy that activates a patient’s own immune system and redirects T cells to kill tumor cells by transiently linking tumor cells with resting polyclonal T-cells for induction of a surface target antigen-dependent re-directed lysis of tumor cells

• This BiTE® mechanism of action is distinct from other immunotherapies• A panel of in vitro assays is employed to characterize novel BiTE® molecules nonclinically that successfully predicted in vivo hallmarks of BiTE® activity as well as clinical anticancer activity• For new BiTE® antibody constructs, the selection of a safe starting dose and clinical safety biomarkers is based on a detailed target liability and pharmacological assessment, repeat-dose

toxicity studies in cynomolgus monkeys and an in vitro MABEL determination

BENNO RATTEL, Executive Director Research,Amgen Research (Munich) GmbH

09:30-

10:00

Tumor-Specifi c Carbohydrate Antigens As Preferable Targets For Novel Bispecifi c Immunotherapeutics Targeting Solid Tumors• Carbohydrates on the surface of cancer cells represent preferable targets for bispecifi cs due to their unique tumor-specifi city with lack or inaccessibility on normal tissues and broad

indication coverage• We demonstrate that carbohydrates are valuable targets for diff erent bispecifi c approaches by creating a carbohydrate-targeted IL-15-based immunocytokine and a bispecifi c T cell engager• Both molecules are able to stimulate an array of eff ector cell responses in vitro and in vivo and are suitable agents for mono or combinatorial therapy of solid tumors

JOHANNA RÜHMANN, Senior Director, Internal Project Strategy & Cooperation,Glycotope GmbH

10:00-

11:20

Exhibition Area: Hall IMorning Coff ee & Refreshments, One To One Meetings x4, Poster Presentation Sessions

11:20-

11:50

Introducing Bixab: Bispecifi c Antibody Platform For Cancer Therapy In Developing Clinical Leads• BiXAb® are “Plug-and-Play” bispecifi c antibodies• Excellent drug-like properties: manufacturability, stability, and no aggregation propensity• Two showcases: BMX-002 and BMX-101 target solid tumors and hematological malignancies

EUGENE ZHUKOVSKY, Chief Scientifi c Offi cer,Biomunex

11:50-

12:20

12:20-

12:50

Optimization Of Preclinical Safety And Effi cacy Of Anti-HER2/CD3 TDB• Adverse eff ects limiting the applicability of T cell re-directing bispecifi c antibodies• Impact of HER2 and CD3 affi nity on anti-tumor effi cacy and pre-clinical safety will be described• Several strategies to optimize therapeutic index will be discussed

TEEMU JUNTTILA, Senior Scientist, Translational Oncology,Genentech

12:50-

13:50

Exhibition Area: Hall ILunch, One To One Meetings x2, Poster Presentation Sessions

Table 3: Innovation In Screening

Moderator: ERIC GOEDKEN, Principal Scientist, Discovery Dermatology & Fibrosis, AbbVie

Table 1: Broadening The Chemical Space Of DNA Encoded Libraries

Moderator: JOHANNES OTTL, Director, Novartis Institutes for BioMedical Research, Chemical Biology & Therapeutics, Chemical Genetics

Table 2: New Approaches To Therapeutic Discovery In Oncology

Moderator: JAMES PRUDENT, President & Chief Executive Offi cer, Centrose

Stream Chair: EUGENE ZHUKOVSKY, Chief Scientifi c Offi cer, Biomunex

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Bispecifics in Discovery & Development DAY TWO: 12 JUNE

R&D Series EU 2019 - Bispecifics in Discovery & Development DAY TWO: 12 JUNE

PRECLINICAL DEVELOPMENT, TRANSLATION AND CLINICAL DEVELOPMENT IN BISPECIFIC ANTIBODIES

Conference Room: Salon 3

13:50-

14:20

Cloudbreak: A Novel Approach To Immunotherapeutics Targeting Infectious Diseases

• Cloudbreak bispecifi c conjugates consist of a Targeting Moiety (TM) covalently linked to an Eff ector Moiety (EM). The TM binds to and neutralizes the targeted pathogen while the EM engages the immune system to provide enhanced effi cacy

• Cloudbreak small molecule and Fc conjugates eff ective against fungal, bacterial and viral infections will be presented

JAMES BALKOVEC, Senior Research Advisor,Cidara Therapeutics, Inc

14:20-

14:50

Guided Inhibition With Bispecifi c Antibodies: CD47 Case Study• CD47 is a ubiquitously expressed immune checkpoint and a “marker of self” downregulating phagocytosis• Guided inhibition of CD47 in tumour cells can be achieved with bispecifi c antibodies targeting a tumour-associated antigen (TAA) with a high-affi nity anti-TAA arm (the “guide”). The lower-

affi nity “eff ector” arm is capable of blocking CD47 upon co-engagement of TAA on tumour cells, but not on TAA-negative healthy cells• CD47/TAA bispecifi c antibodies show potent anti-tumour activity in vitro and in vivo, associated with resistance to CD47-mediated “antigen sink” and favourable safety and pharmacokinetic

profi les in non-human primate studies

KRZYSZTOF MASTERNAK, Head of Biology,NovImmune

14:50-

15:20

Exhibition Area: Hall IAfternoon Coff ee & Refreshments, Poster Presentation Sessions

15:20-

15:50

Agonist Bispecifi c Antibodies Delivering The Next Immuno-Oncology Breakthrough• Targeting T-cells via TNFRSF costimulatory pathways has the potential to strongly activate the immune system due to broad expression across multiple immune cells• FcγR-mediated crosslinking is often required for optimal activity, limiting clinical effi cacy, due to low affi nity of Fc:FcyR interactions and ADCC-mediated T-cell depletion• We present novel bispecifi c programmes that do not bind to FcyR, but instead crosslink their two targets, resulting in a potent and controlled T-cell activation

MIHRIBAN TUNA, Senior Vice President, Drug Discovery,F-Star

15:50-

16:20

Preclinical And Clinical Development of ZW25, A Novel HER2-Targeted Biparatopic Antibody• Highlights of ZW25’s unique and diff erentiating mechanisms of action• Updated clinical results underscoring ZW25’s anti-tumor activity and tolerability in a variety of HER2-expressing cancers

NINA E. WEISSER, Principal Scientist,Zymeworks Inc.

16:20 End of Congress

New for 2019, the Neuroscience in Discovery & Development Congress features 2 interactive streams, which include over 20 presentations, case studies and panel discussions focused on the key issues in the industry today:

NEUROSCIENCE: AGENDA AT A GLANCE NEUROSCIENCE: AGENDA AT A GLANCE

DAY ONE: 11 JUNE

DRUG DISCOVERY STRATEGIES, TOOLS AND TECHNOLOGIES IN CNS

TRANSLATION, STRATIFICATION AND PRECISION MEDICINE

Target Identification and Validation Approaches

Advancements and Emerging Trends in the Application of Technology to Develop Neurological Treatments

Cutting Edge Technologies in Animal and Translational Modelling for CNS Drug Discovery

iPS Cells for Disease Modeling and Drug Discovery - Neuro Stem Cells for Drug Discovery

Stem Cell Technology to Fuel Drug Discovery for Neurodegenerative Diseases

Imaging Technologies

The Role of Biomarkers in Drug Discovery of Neurodegenerative Disorders e.g. Alzheimer’s, ALS, Parkinson’s

Patient Stratification & Advanced Brain Monitoring

Translational Neuropsychiatry

Neuroscience-Based Precision Medicine, Including Diagnosis and Treatment of Brain Mechanisms in Genetics / Epigenetics

DAY TWO: 12 JUNE

DAY 2 TRANSLATION, STRATIFICATION AND PRECISION MEDICINE

MORITZ VON HEIMENDAHL

Principle Scientist Boehringer Ingelheim Pharma GmbH & Co. KG

THOMAS MISKOLead Scientist & Senior Scientific Director, Translational Neuroscience AbbVie Neuroscience Development

ROLAND HEYM

Lab Head In Neuroscience Discovery AbbVie

DAY 1 DRUG DISCOVERY STRATEGIES, TOOLS AND TECHNOLOGIES IN CNS

STEFAN HAUSER

Head of Stem Cell Laboratory German Center for Neurodegenerative Diseases

CARLO CUSULIN

Senior Scientist, Lead Discovery F. Hoffmann-La Roche

VINEETA TRIPATHI

Principal Scientist Ipsen

PRADEEP NATHANVice President Clinical Development & Head of Experimental Medicine (Neuroscience), Professor of Neuroscience (Monash University), Affiliated Lecturer (University of Cambridge) Heptares Therapeutics Ltd

VICTORIA BAJO LORENZANA

Associate Professor of Neuroscience University of Oxford

HOLGER MONENSCHEINDirector, Medicinal Chemistry, Neuroscience Drug Discovery Unit Takeda

MAGNUS IVARSSON

Vice President, Head of Discovery Rodin Therapeutics

MARKUS SCHADE

Scientific Director Grünenthal GmbH

CEDRIC POINSARD

Chief Executive Officer Genochem

07:30-

08:20Registration: Conference Floor 1 Foyer

R&D SERIES EU

08:20 Conference Room: Hall II Oxford Global Welcome Address

08:25 Chairperson’s Opening Address: MIKE DYSON, Chief Technology Offi cer, IONTAS Ltd

08:30-

09:00

Co-Located Keynote Address: Communicating Prospective Accuracy Of Human PK PD Predictions; Impact In Discovery And Early Development Of Small Molecules• Increasing accuracy and integration of PK and PD along the value chain• Point prediction Vs density plots; impact on decision making• Impact of dose predictions on optimization strategies

CARL PETERSSON, Scientifi c Director Drug Disposition,Merck KGaA

NEUROSCIENCE IN DISCOVERY & DEVELOPMENT CONGRESS

DRUG DISCOVERY STRATEGIES, TOOLS AND TECHNOLOGIES IN CNS

Conference Room: Salon 6

Stream Chair: MARKUS BUTZ-OSTENDORF, Innovation Manager Brain Science, Biomax Informatics AG, Planegg

09:00-

09:30

Stream Keynote Address: Identifi cation And Validation Of Cell-Type Selective GPCRs As Drug Targets In The CNS• Toxicity is still one of the major reasons for clinical and preclinical attrition• While on-target toxicity is diffi cult to address, off target toxicity can be managed via selectivity, either of the drug itself, or by selecting targets with high regional specifi city• Takeda’s bac-TRAP technology, which enables the profi ling of target expression patterns from individual cell types in the CNS, has guided the selection of 3 GPCRs as drug targets for very

specifi c circuit modulation without engaging other unwanted pharmacology• All 3 case studies will be discussed

HOLGER MONENSCHEIN, Director, Medicinal Chemistry, Neuroscience Drug Discovery Unit,Takeda

09:30-

10:00

NeuroXM Brain Science Suite - The One Stop Shop For NeuroscientistsThe NeuroXM Suite is a novel product by Biomax Informatics, Planegg, Germany, launched end 2018, to Integrate, harmonize, analyze and report all brain-related data from molecular to neuroimaging data. With its capabilities and features, NeuroXM Suite supports the whole pharmaceutical developmental process from target fi nding, safety and risk minimization of new drug candidates up to monitoring clinical trials of each phase. The NeuroXM Suite supports the discovery of new neuropharmaca by analyzing the local action of drug candidates with information from gene expression maps (from Allen Human and Mouse Brain Atlases or even in-house single-cell data), Reactome pathways, disease ontologies and literature references. It further helps predict the systemic eff ects of a compound from its local physiological action by integrating connectome data measured by DTI, rs-fMR, td-fMRI or even EEG. The integration of human brain data with model organism brain data allows for a range of essential analyses, such as query homologue genes; visualize diff erential expression; analyze connectivity patterns of brain areas with high expression; as well as analyze diff erential connectivity in mouse and humans. The NeuroXM one stop shop for neuroscientists off ers a clear value proposition for all in neuroscience researching pharmaceutical companies as supports target fi nding by making all public and in-house information on a potential new drug target available. It predicts safety of new drugs by better localizing binding sites of new compounds, predicts the systemic eff ects of new compounds in very early stages of drug development, and predicts the eff ect of new compounds in humans from fi ndings in mice to save costs long before entering clinical trials.

MARKUS BUTZ-OSTENDORF, Innovation Manager Brain Science,Biomax Informatics AG, Planegg

10:00-

11:20

Exhibition AreaMorning Coff ee & Refreshments, One to One Meetings x3, Poster Presentation Sessions

11:20-

11:50

Modelling Rare Neurological Disorders By Using Induced Pluripotent Stem Cells• Disease modelling using iPSC-derived neurons• Rare neurological disorders (Hereditary spastic paraplegia)• Preclinical treatment strategies

STEFAN HAUSER, Head of Stem Cell Laboratory,German Center for Neurodegenerative Diseases

11:50-

12:20

12:20-

12:50

12:50-

13:50

Exhibition Area: Hall ILunch, One To One Meetings x2, Poster Presentation Sessions

Delegates are welcome to attend the co-located presentations

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Neuroscience in Discovery & Development DAY ONE: 11 JUNE

13:50-

14:20

Translational Biomarkers For Measuring Synaptic Density In Neurogenerative Diseases

Biomarkers are readouts to determine the eff ect of a novel drug discovery target. It has been specifi cally challenging to identify accessible biomarkers refl ecting CNS effi cacy or target engagement. SV2A PET ligand is a novel imaging tool that can measure synaptic density and track changes over time.

MAGNUS IVARSSON, Vice President, Head of Discovery,Rodin Therapeutics

14:20-

14:50

Leveraging Stem Cell Technology To Fuel Drug Discovery For Neurodegenerative Diseases• Use of iPS technology to model diff erent aspects of Alzheimer’s disease, spanning from hypothesis generation to lead optimization• Transcriptional eff ects of Aβ changes in vitro and in vivo• Tau aggregation model and screening of small molecules to reduce it• Microglia model

CARLO CUSULIN, Senior Scientist, Lead Discovery,F. Hoff mann-La Roche

14:50-

15:20

15:20-

16:20

Exhibition Area: Hall IAfternoon Coff ee & Refreshments, One To One Meetings x3, Poster Presentation Sessions

16:20-

16:50

Panel Discussion: The Role Of Informatics In Neuroscience Drug Discovery

Panel Moderator: MARKUS BUTZ-OSTENDORF, Innovation Manager Brain Science, Biomax Informatics AG, Planegg

Panellists Include:VINEETA TRIPATHI, Principal Scientist, Ipsen BIoinnovation Ltd. Oxford, UKVICTORIA BAJO LORENZANA, Associate Professor of Neuroscience, University of Oxford

16:50-

17:20

Eff ect Of Removing Cholinergic Input On Auditory Sensory Processing• Acetylcholine (Ach) is essential for a normal sound localization behavior under normal hearing conditions and unilateral conductive hearing loss • Reduced cholinergic release in the auditory cortex does not infl uence the spatial sensitivity of neurons but prevent adaptation to changes in the localization cues• ACh may play an important but not yet confi rmed role in tinnitus triggering and its chronifi cation

VICTORIA BAJO LORENZANA, Associate Professor of Neuroscience,University of Oxford

17:20-

17:50

Chimeras Of Anthrax Toxin And Botulinum Neurotoxin As Novel Analgesic Proteins• We found that the anthrax toxin receptor, ANTXR2, is expressed in nociceptor neurons, but not other nervous tissues or cell types• Anthrax toxin binds to ANTXR2 via Protective Antigen (PA), which binds and translocates Lethal Factor (LF) or Edema Factor (EF) into the cytoplasm. Botulinum neurotoxins (BoNT)

proteolytically cleave SNARE proteins to inhibit neurotransmitter release• We have produced Anthrax toxin–BoNT chimeras to assess their analgesic potential• Chimeric proteins combining anthrax toxin receptor binding activity and BoNT SNARE cleavage provide a platform to develop therapeutic proteins for the treatment of pain

VINEETA TRIPATHI, Principal Scientist,Ipsen Bioinnovation Ltd. Oxford, UK

17:50-

18:20

The Use Of Functional Imaging In Drug Development: From Target Engagement To Proof Of Concept

Functional imaging methods such as functional magnetic resonance imaging (fMRI) have been widely used to gain greater understanding of brain circuitry abnormalities in CNS disorders and their underlying neurochemical basis. It is also increasingly used in early clinical drug development as a biomarker to demonstrate target engagement and provide an early indication of effi cacy on brain systems relevant to clinical outcome. Studies that have used fMRI in early clinical development including studies conducted by the author on the development of a mu-opioid receptor antagonist GSK1521498 for disorders of compulsive consumption suggest that fMRI is a promising biomarker to demonstrate; 1) target engagement, 2) dose response eff ects and 3) diff erential or synergistic eff ects, on relevant brain circuitry. There is also some evidence that early drug eff ects on brain activity can predict clinical effi cacy, although more studies are needed to examine this across diff erent outcome measures. Together, these observations suggest that functional imaging methods like fMRI are sensitive biomarkers of abnormal regional or brain networks activity in CNS disorders and can add value in early clinical development to examine key drug discovery questions related to target engagement, diff erential effi cacy, dose response relationships and prediction of behavioural and clinical relevant changes. However, in order for fMRI to be used as a decision making biomarker in drug development requires further validation and demonstration of its ability to predict clinically relevant drug eff ects across diff erent outcome measures.

PRADEEP NATHAN, Vice President Clinical Development & Head of Experimental Medicine (Neuroscience), Sosei Heptares and Professor of Neuroscience, Monash University and Affi liated Lecturer, University of Cambridge

18:20-

18:50

18:50-

19:20

19:20Exhibition Area: Hall I

Networking Drinks & End Of Day One

Delegates are welcome to attend the co-located presentations

Delegates are welcome to attend the co-located presentations

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Neuroscience in Discovery & Development DAY ONE: 11 JUNE

DRUG DISCOVERY STRATEGIES, TOOLS AND TECHNOLOGIES IN CNS

Conference Room: Salon 6

R&D SERIES EU 2019THINK TANK ROUNDTABLE DISCUSSIONS AND BREAKFAST

Conference Room: Hall II

08:00-

08:30

Co-Located Keynote Address: Leveraging Synthetic Modality Innovations To Probe Key Nodes In Cancer & Immune Cells

08:30-

09:00

• Impact of synthetic modalities in cancer drug discovery• Using chemical probes in cancer target validation: Generating value instead of noise• Quality criteria for chemical probes & open innovation approaches• Importance of combining diverse lead fi nding technologies to identify valid starting points• Case studies: probing epigenetic reader ATAD2, PPI Ras/SOS & metabolic immune switch AhR

INGO HARTUNG, Vice President of Medicinal Chemistry,Bayer

09:00-

09:30

Stream Keynote Address: Development Of Antibody-Drug-Conjugates To Novel Embryonic Targets In Cancer• Metastatic and aggressive cancers caused by cellular reprogramming to generate primitive malignant cells with embryonic properties• CureMeta develops novel high specifi c and high affi nity antibodies to embryonic targets not expressed in normal tissues but re-expressed in cancers• CureMeta develops novel therapeutic antibody-drug-conjugates to treat patients with aggressive and metastatic cancers

MIKE SCHOPPERLE, Chief Executive Offi cer,CureMeta

09:30-

10:00

Enabling Data Workfl ows Across External Collaborations And Partnerships• All partners in a research collaboration must be able to share data and participate in cross-organization workfl ows• A scientifi c collaboration and data exchange environment is critical to ensure these partnerships are successful & effi cient

ROB BROWN, Vice President, Global Informatics,Dotmatics

10:00-

11:20

Exhibition Area: Hall IMorning Coff ee & Refreshments, One To One Meetings x4, Poster Presentation Sessions

NEUROSCIENCE IN DISCOVERY & DEVELOPMENT CONGRESS

TRANSLATION, STRATIFICATION AND PRECISION MEDICINE

Conference Room: Salon 6

Stream Chair: THOMAS MISKO, Lead Scientist & Senior Scientifi c Director, Translational NeuroscienceAbbVie Neuroscience Development

11:20-

11:50

Stream Keynote Address: Fragment-Based Drug Discovery For Neuroscience Targets• First-line analgesics for moderate to severe pain have CNS modes-of-action• Case study of fragment-based discovery of novel NCEs for a chronic low back pain target• Presentation of target-inhibitor crystal structures and MedChem optimization

MARKUS SCHADE, Scientifi c Director, Grünenthal GmbH

11:50-

12:20

12:20-

12:50

Blood Biomarkers In Neurological Disorders: Utility In Disease Progression And Patient Response In The Clinic• The Challenge of Identifying Biomarkers for Patient Selection, Stratifi cation and Therapeutic Response• Blood as the Nexus of CNS Disease Progression and Therapeutic Response

THOMAS MISKO, Lead Scientist & Senior Scientifi c Director, Translational NeuroscienceAbbVie Neuroscience Development

12:50-

13:50

Exhibition Area: Hall ILunch, One To One Meetings x2, Poster Presentation Sessions

Table 3: Innovation In Screening

Moderator: ERIC GOEDKEN, Principal Scientist, Discovery Dermatology & Fibrosis, AbbVie

Table 1: Broadening The Chemical Space Of DNA Encoded LibrariesModerator: JOHANNES OTTL, Director, Novartis Institutes for BioMedical Research, Chemical Biology & Therapeutics, Chemical Genetics

Table 2: New Approaches To Therapeutic Discovery In Oncology

Moderator: JAMES PRUDENT, President & Chief Executive Offi cer, Centrose

Delegates are welcome to attend the co-located presentations

R&D Series EU 2019 - Neuroscience in Discovery & Development DAY TWO: 12 JUNE

R&D Series EU 2019 - Neuroscience in Discovery & Development DAY TWO: 12 JUNE

13:50-

14:20

Panel Discussion: Overcoming Biomarker Challenges In Neuroscience

Panel Moderator: THOMAS MISKO, Lead Scientist & Senior Scientifi c Director, Translational Neuroscience, AbbVie Neuroscience DevelopmentPanellists Include:ROLAND HEYM, Team Leader, Molecular and Imaging Biomarker, Neuroscience DiscoveryAbbVie Deutschland GmbH & Co. KGMORITZ VON HEIMENDAHL, Principle Scientist,Boehringer Ingelheim Pharma GmbH & Co. KG

14:20-

14:50

Fluid Biomarkers For Parkinson’s Disease

• Aggregated alpha-synuclein in the brain is the hallmark of Parkinson’s disease (PD)• Total and phosphorylated alpha-synuclein in the CSF have limited value as PD biomarkers• Monitoring the seeding activity of aggregated alpha-synuclein in the CSF is a promising approach for PD diagnosis• Multicandidate approaches identify new biomarker candidates in the CSF and plasma of PD patients

ROLAND HEYM, Team Leader, Molecular and Imaging Biomarker, Neuroscience DiscoveryAbbVie Deutschland GmbH & Co. KG

14:50-

15:20

Exhibition AreaAfternoon Coff ee & Refreshments, Poster Presentation Sessions

15:20-

15:50

Translational Approaches To Drug Discovery In Neuropsychiatry

• Identifi cation of a uniform circuit pathology of psychiatric syndromes has proven diffi cult• Linking psychiatric symptoms, rather than syndromes, to specifi c circuit dysfunction appears more promising• Circuit-Symptom understanding can be back-translated into experimental circuit lesions in rodents, yielding an animal model of a symptom• Characterization of models on multiple levels (physiology and behavior) increases translational confi dence• Models may be used for both target identifi cation and validation

MORITZ VON HEIMENDAHL, Principle Scientist,Boehringer Ingelheim Pharma GmbH & Co. KG

15:50-

16:20

KCC2 Gain Of Function For Spasticity Treatment And Other Neurological Disorders

• The potassium-chloride cotransporter KCC2 maintain low intracellular chloride concentration required for inhibition in mature neurons• KCC2 dysfunction and impairment of chloride extrusion is associated with many central nervous system disorders like epilepsy, neuropathic pain and spasticity of spinal cord injury origin• We will review the literature data and present our internal small molecule program targeting KCC2 gain of function and supporting KCC2 as a promising target in neurosciences

CEDRIC POINSARD, Chief Executive Offi cer, Genochem

16:20 End of Congress

TRANSLATION, STRATIFICATION AND PRECISION MEDICINE

Conference Room: Salon 6

PART 2: PARTNERING STRATEGIES

Conference Room 5

VENUE INFORMATION

Maritim ProArte Hotel BerlinFriedrichstraße 151,

10117 Berlin, Germany

maritim-proarte-hotel-berlin.hotel-in-berlin.org/en

Maritim ProArte Hotel Berlin Friedrichstraße 151, 10117 Berlin, Germany Tel: +49 30 2502-0 | Fax: +49 30 2502-1119 Email: [email protected]

The Maritim proArte Hotel is centrally situated between the Brandenburg Gate and the Gendarmenmarkt directly on the Friedrichstrasse. From here, you can reach many of the city’s attractions by foot: the Friedrichstadt-Palast Theatre, Museum Island, the Reichstag building, the “Unter den Linden” shopping street, various theatres and lots more.

The hotel is easily accessable by rail, car, and air. Detailed travel directions can be found at: www.oxfordglobal.co.uk/rd-series-eu/venue/

Berlin is a major center of politics, culture, media, and science. Noted for its cultural flair, its diverse art scene encompasses hundreds of galleries, events, and museums, including those centered around Museum Island, a UNESCO World Heritage Site.

Oxford Global has secured a limited number of discounted rooms at the Maritim proArte Hotel with breakfast included. If you would like to take advantage of this deal, please book directly through the Maritim proArte Hotel website by clicking here. Please note that the cut-off date for the discounted rooms is 10th May 2019.

Number of delegates:

Industry del(s) Academic dels(s) Vendor dels(s) Special Offer: 3 for 2 Offer is only valid on the series and for those registering at Industry or Academic rates Please choose one of the following payment options:

CREDIT CARD:

An Oxford Global representative will contact you directly following return of contract / booking form to process card payment. If payment will be made by a colleague within your company, please complete the following; Card Payment Contact Name: ___________________________________ Phone Number: _________________________________________________ INVOICE:

Invoice Address (if different from above) ________________________

__________________________________________________________________

__________________________________________________________________ *Please note there is a €65 handling charge for payment via invoice

Agreed Terms between the Organiser (Oxford Global Marketing Ltd) and the Delegate: Delegate Booking Fee The Delegate Booking Fee includes: lunches and refreshments throughout the series, presentations and panel sessions, scheduled one-to-one meetings and networking/social events, series and speaker notes. Delegates may attend, free of charge, all sessions arranged by the Organiser.

An admin surcharge of €65 will be applied to payments settled following the receipt of an invoice. This charge will not be applied to payments settled online.

Vendor Delegates will not be eligible for one to one meetings unless they purchase a sponsorship meetings package. These can only be purchased directly from Oxford Global Marketing Ltd and not via the online booking facility.

Acceptance of a Complimentary Pass If you are offered a free delegate pass and you are unable to attend the series, you may nominate a substitute of equal standing (in terms of business and financial responsibility). A substitute delegate must be nominated within a week of cancellation and must be approved by the Organiser in advance in order to avoid a non-attendance charge of €245 being applied. Your complimentary delegate place is not officially confirmed until we have had chance to check that you qualify for the complimentary pass. Please do not make any travel arrangements before we have confirmed acceptance of your application. We will not be liable for any expenses incurred.

Delegate Registration Form Each Delegate must complete the online delegate registration form issued by the Organiser on receipt of the Delegate Booking Form. This information will only be used for the organisation of the series, for material produced for Delegates and Sponsors and to facilitate the networking sessions.

Cancellation and Curtailment If a Registered Delegate is unable to attend the series, he/she may nominate a substitute of equal standing within their Company. A substitute delegate must be nominated within a week of cancellation and must be approved by the Organiser in advance in order to avoid cancellation charges being applied. Delegates and vendor delegates are subject to the following charges and refunds upon withdrawal or cancellation.

More than 6 months prior 35% cancellation fee / 65% refund Between 6 and 3 months prior 75% cancellation fee / 25% refund Less than 3 months prior to the event Full cancellation fee / No refund

Data Protection The data controller is the organiser (Oxford Global Marketing Ltd). The Organiser may disclose such personal information as name, company, job title, telephone and email address to Registered Event Sellers (Solution Providers) and other Delegates but solely for the purposes of the Series. Registration details will be retained and used in accordance with our privacy policy. If you wish to opt out please email [email protected]

Miscellaneous The Organiser will determine the scope and content of series events, seminars, workshops and activities throughout the series. The Organiser reserves the right to cancel the series without liability to Delegate’s Company or individual Delegate. If for any reason the Organiser has to cancel or postpone this series, the Organiser reserves the right to transfer this Booking to another Congress within the same sector to be held within twelve months. Should another Congress in the same sector not be available within this period, the Booking Fee will be refunded. For promotional purposes, there may be professional photography and video production taking place during the series. Delegates who do not wish to be filmed or recorded should advise the organisers by email to [email protected] prior to the event. These terms and conditions are binding upon the delegate submitting a registration form.

I cannot attend but would like to purchase access to the following: Access to the online conference presentations €605

Please complete fully and clearly. Please photocopy for additional delegates. Please tick which event(s) in the series you are interested in: Drug Discovery Discovery Chemistry Bispecific Neuroscience Title:_____ Forename:__________________ Surname:__________________ Job Title:___________________________________________________________ Company/Organisation:___________________________________________ Email:_____________________________________________________________ Address:___________________________________________________________ Postcode: ________________________ Country: _________________________ Direct Telephone _______________ Direct Fax: ________________ Mobile: ________________________ Switchboard: _____________

I would like to attend: (Please tick as appropriate) Industry Delegates (Biopharma, Pharma or Biotech Companies)

2-day pass €1,085 1-day pass €725

Day 1 Day 2 Academic Delegates 2-day pass €630 1-day pass €390 Day 1 Day 2 Vendor Delegates (CROs, Consultants, Technology and Service Providers)

Series Only €2,110 Poster Presentation €305 PROMOTIONAL LITERATURE DISTRIBUTION

Distribution of your company’s promotional literature to all series attendees €1205

R&D Series EU 20th Annual Drug Discovery Summit | 7th Annual Discovery Chemistry & Drug Design Congress | Bispecifics In

Discovery & Development Congress | Neuroscience In Discovery & Development Congress

11—12 June 2019 | Maritim proArte Hotel, Berlin, Germany www.oxfordglobal.co.uk/rd-series-eu

HOW TO REGISTER: FAX your booking form to +44(0)1865 689120 | PHONE on +44(0)1865 248455 | EMAIL: [email protected]

If you have any further queries please call the marketing team on +44(0)1865 248455 or email [email protected]

Delegate Details

Terms & Conditions of Booking

I agree to the above Terms and Conditions

Registration Fees: 4 events in 1

Documentation

How to Pay

Oxford Global Marketing Ltd.

Part 1st Floor, Godstow Court Minns Business Park Botley, Oxford, OX2 0JB

Tel: +44 (0)1865 248455 Fax: +44 (0)1865 250985 www.oxfordglobal.co.uk

Join the Conversation

@drugdiscovery1 #RNDSeries19 #DDSEU19

COMPLIMENTARY RESOURCES

Visit www.oxfordglobal.co.uk/rd-series-eu/resources to gain access to our complimentary resources, including Live and Recorded Webinars, Speaker Publications, Sponsor White Papers, and more!

FORTHCOMING EVENTS

FOR MORE DETAILS, PLEASE VISIT WWW.OXFORDGLOBAL.CO.UK

Immuno-Oncology Series

UK

5th Annual Advances in Immuno-Oncology CongressMay 2020 | London, UK Autoimmunity & Immunology Congress CongressMay 2020 | London, UK

US 2nd Annual Advances in Immuno-Oncology USA Congress08 - 09 October 2019 | San Diego, USA

Co-lo

cate

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ents

Formulation & Delivery Series

UK

6th Annual Formulation & Drug Delivery CongressApril 2020 | London, UK5th Annual Inhalation & Respiratory Drug Delivery CongressApril 2020 | London, UKBiomanufacturing CongressApril 2020 | London, UK

US

3rd Annual Formulation & Drug Delivery USA CongressMarch 2020 | San Diego, USA3rd Annual Inhalation & Respiratory Drug Delivery USA CongressMarch 2020 | San Diego, USA

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R&D Series

EU

21st Annual Drug Discovery SummitJune 2020 | Berlin, Germany

8th Annual Discovery Chemistry & Drug Design CongressJune 2020 | Berlin, Germany

2nd Annual Neuroscience in Discovery & Development CongressJune 2020 | Berlin, Germany

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Biologics Series

UK

13th Annual Proteins & Antibodies CongressApril 2020 | London, UK7th Annual Peptides CongressApril 2020 | London, UK

2nd Annual Bispecifi cs in Discovery & Development CongressApril 2020 | London, UK

US Proteins & Antibodies USA Congress18 - 19 November 2019 | Boston, USA

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Cell Series

UK

8th Annual Cell Culture & Bioprocessing Congress24 - 25 October 2019 | London, UK6th Annual Stem Cell & Regenerative Medicine Congress24 - 25 October 2019 | London, UK5th Annual Cell & Gene Therapy Congress24 - 25 October 2019 | London, UK

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PharmaTec Series

UK

17th Annual Pharmaceutical IT & Data Congress25 - 26 September 2019 | London, UK

3rd Annual Artifi cial Intelligence in Drug Development Congress25 - 26 September 2019 | London, UK

Cyber Security & Data Protection in Pharma & Healthcare Congress25 - 26 September 2019 | London, UK

SmartLabs & Laboratory Informatics Congress25 - 26 September 2019 | London, UK

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SynGen Series

UK

11th Annual Next Generation Sequencing & Clinical Diagnostics Congress07 - 08 November 2019 | London, UK

7th Annual Single Cell Analysis Congress07 - 08 November 2019 | London, UK

5th Annual Genome Editing Congress07 - 08 November 2019 | London, UK

2nd Annual Synthetic Biology Congress07 - 08 November 2019 | London, UK

Digital PCR Congress07 - 08 November 2019 | London, UK

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US

6th Annual Next Generation Sequencing & Clinical Diagnostics USA CongressMay 2020 | Boston, USA

6th Annual Single Cell Analysis USA CongressMay 2020 | Boston, USA

4th Annual Genome Editing USA CongressMay 2020 | Boston, USA

3rd Annual Synthetic Biology USA CongressMay 2020 | Boston, USA

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Biomarkers Series

UK

15th Annual Biomarkers Congress18 - 20 February 2020 | Manchester, UKGenomics Markers Congress18 - 20 February 2020 | Manchester, UK

US 4th Annual Biomarkers & Precision Medicine USA Congress08 - 09 October 2019 | San Diego, USA

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