Open Innovation in Small Molecule Lead Discovery
“Center for Open Innovation in Drug Discovery”
From Molecules to Business – 25 September 2014
Jac Wijkmans
Take Home Messages
Great need to organize pharma R&D in a different way
Academia hold the key to bridge the innovation gap between
exploratory research & early clinical development
Merge the strengths of academic & industrial drug research
Initiated a feasibility study to create “Center of Open
Innovation in Drug Discovery” to place RU/Radboudumc at
forefront of translational medicine
Similar successful initiatives exist abroad that have proven
to provide a sustainable academic drug discovery enterprise
The Pharma Landscape
Society
‒ Increasing incidence of chronic diseases.
‒ Escalating health care costs
‒ Increased patient awareness
‒ Personalized health care
Industry
‒ Declining productivity
‒ Risk aversion
‒ R&D externalization
‒ Late stage focus
‒ Innovation pull
‒ Driver: Shareholder value
Academia
‒ Austerity measures
‒ Clinical trial experts
‒ Increasingly entrepreneurial
‒ Early stage focus
‒ Valorization push
‒ Driver: Publications & health
Evolving R&D Process
<2005: The ‘good old days’
2005 - present: Shift from R&D to S&D (Search & Development)
IndustryAcademia Pre-clinical candidate
Need to Organize Early R&D Differently
Spin-offCRO #1 CRO #2
CRO #3
?
A:
B:
‒ Too early to out-license
‒ Shortage in funds
‒ Missing skills
‒ No open innovation (recycling of knowledge, molecules, IP)
Issues
Academia Hold the Key, however, …
… while targets, assays, compound synthesis & patients are present, medicinal chemistry capabilities are
critically missing
Frye et al. Nature Rev. Drug Discov. 10, 2011, 409
Medicinal Chemistry
Optimizing Molecular properties to get into Business
IdealNot acceptable
1. Affinity
2. Selectivity
3. Efficacy
4. Solubility
5. Metabolic Stability
6. Protein binding
7. Toxicity
Medicinal Chemistry
Optimizing Molecular properties to get into Business
IdealNot acceptable
1. Affinity
2. Selectivity
3. Efficacy
4. Solubility
5. Metabolic Stability
6. Protein binding
7. Toxicity
Multidimensionaloptimization
paradigm
Empower Academic Drug Research
Academic
biomedical
research
Medicinal
chemistry
capabilities
“Blend academic biomedical research with industry-
standard drug discovery capabilities to valorize innovation”
“Establish a leading force in academic drug discovery”
Center for Open Innovation in Drug
Discovery
COIDD
Creating Value Chains
A Sustainable Pharma R&D Ecosystem
IP
(pre-)clinical candidates
Platform technologies
Spin-offs
Publications
Synergies/cross-overs
Education & training
$$$$$$
Potential projects identified
European Lead FactoryHTS
Center for Open Innovation in Drug Discovery (COIDD)
Incorporate the highest level of drug discovery into
academic research and advance the most exciting scientific
breakthroughs towards the development of drug candidates
suited for clinical studies
Vision
Establish an unique & sustainable pharmaceutical R&D
ecosystem to create new small molecule therapeutics to
improve public health and place RU/Radboudumc at
forefront of translational medicine
Mission
COIDD Core Expertise
MedicinalChemistry
Chemical Biology
Drug discovery
Tool compounds
Project Management & Development
Leads & (pre)clinicalcandidates
New projects
industry-trained professionals
Dedicated facilities
Open Innovation in Practice
New molecular target or
differentiating assay
ClinicalNeed?
amenablefor HTS?
HTS & compound
optimization
Pre-clinical candidate
out-licensing/
partnership
For example:
Revolving funds
A Validated & Sustainable Model!“De-risking investments in new treatments for brain
disorders by blending academic based research with state-of-
the-art drug discovery resources”
“Bringing dedicated medicinal chemistry expertise to bear on
biological targets being investigated by UNC faculty”
A Validated & Sustainable Model!
Vanderbilt Center for Neuroscience Drug Discovery
Founded in 2003, Track Record:
2009: Drug discovery pact with J&J
2010: Research collaboration with Seaside Therapeutics
2011: Partnership Michael J. Fox Foundation
2011: License deal Karuna Pharma
2012: BMS Parkinson R&D collaboration
2013: Licensing & research deal with AstraZeneca
“De-risking investments in new treatments for brain
disorders by blending academic based research with state-of-
the-art drug discovery resources”
A Validated & Sustainable Model!
“Exploiting and transforming innovative
research into pharmaceutical applications in
close cooperation with academic partners”
Lead Discovery Centre Dortmund
Founded in 2007, Track Record:
2011: First LDC lead licensed to Bayer
2013: 2nd LDC lead licensed to Qurient
Drug discovery alliance AstraZeneca
Strategic partnership Merck Serono
2014: Drug discovery alliance Daiichi Sankyo
Embedding in Health Valley Region
Radboud Nanomedicine
Alliance
“HealthyBrain”
Technology centers
Feasibility Study – Next Steps
1. Get buy in and commitment from major stakeholders
2. Determine focus, identify key partners, select projects
3. Learn from “best practices”
4. Further develop business plan (revenue model, financial
requirements, organization, team)
5. Apply for grants, raise capital investments
6. Build team
3Q 4Q 1Q 2Q 3Q
20152014
preparation phase financing phase
Go/NoGo
AccelerateProject
XProject
Y
Start
Conclusions
Great need to organize pharma R&D in a different way
Academia hold the key to bridge the innovation gap
between exploratory research & early clinical development
Merge the strengths of academic & industrial drug research
The COIDD will place RU/Radboudumc at forefront of
translational medicine
Successful & sustainable precedents of COIDD exist but
The Netherlands are falling behind … and we are
determined to change this!
Initiators
Prof. Floris Rutjes
Dr. Thea van Kemenade
Prof. Alain van Gool
Dr. Pedro Hermkens
Dr. Jac Wijkmans
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