NationalNationalInstitute InstituteooffScience Science...
Transcript of NationalNationalInstitute InstituteooffScience Science...
EliezerEliezer J. BarreiroJ. BarreiroProfessor Professor
INCTINCT--INOFAR, a Brazilian network forINOFAR, a Brazilian network for
drug design, discovery and developmentdrug design, discovery and developmentNationalNational InstituteInstitute ofof Science Science andand Technology in Technology in DrugsDrugs andand MedicinesMedicines
www.inctwww.inctwww.inctwww.inctwww.inctwww.inctwww.inctwww.inct--------inofar.ccs.ufrj.brinofar.ccs.ufrj.brinofar.ccs.ufrj.brinofar.ccs.ufrj.brinofar.ccs.ufrj.brinofar.ccs.ufrj.brinofar.ccs.ufrj.brinofar.ccs.ufrj.brINCT-INOFAR - Av. Carlos Chagas Filho 373, Centro de Ciências da Saúde (CCS), UFRJ, Bloco K, 2º andar, Sala 23,
Cidade Universitária; PO Box: 68043, ZIP: 21944-971, Rio de Janeiro, R.J., Brazil
INCT-INOFAR - Av. Carlos Chagas Filho 373, Centro de Ciências da Saúde (CCS), UFRJ, Bloco K, 2º andar, Sala 23,
Cidade Universitária; PO Box: 68043, ZIP: 21944-971, Rio de Janeiro, R.J., Brazil eliezer 2013
SummarySummary
��Prologue: a brief view of scientific research Prologue: a brief view of scientific research nowadays & nowadays & the the
interdisciplinarityinterdisciplinarity of complex of complex ddrug rug ddiscovery iscovery (DD) (DD) process;process;
��The pharmaceutical innovation and the role of the universityThe pharmaceutical innovation and the role of the university��The pharmaceutical innovation and the role of the universityThe pharmaceutical innovation and the role of the university
��The INCTThe INCT--INOFAR: INOFAR: our missionour mission
�� The INCTThe INCT--INOFAR: Who INOFAR: Who we are & what we are & what we dowe do
�� The INCTThe INCT--INOFAR: INOFAR: Final Final remarks remarks
�� AcknowledgmentsAcknowledgments
Galileo, Newton, Darwin, & Einstein
The scientific
research
through the
ages...
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Marshall Peterson, William Rowe, Robert Sanders, John Scott, Michael Simpson, Thomas Smith, Arlan Sprague, Timothy Stockwell, Russell Turner,
Eli Venter, Mei Wang, Meiyuan Wen, David Wu, Mitchell Wu, Ashley Xia, Ali Zandieh, and Xiaohong Zhu
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Technological innovation is a
process mostly dynamic in
industrial activity.
This dynamism is
accentuated in
pharmaceuticalpharmaceutical innovation pharmaceuticalpharmaceutical innovation
which, more than any other,
depend on the effective and
productive interaction
between
Science & Technology.
20112011
Why companies involved in DD fail than succeed at releasing the creative energy Why companies involved in DD fail than succeed at releasing the creative energy of its of its scientists? scientists?
MM AbouAbou--GharbiaGharbia,, WEWE Childers,Childers, DiscoveryDiscovery ofof InnovativeInnovative TherapeuticsTherapeutics:: Today’sToday’s RealitiesRealities andand Tomorrow’sTomorrow’s
VisionVision.. 11.. CriticismsCriticisms FacedFaced byby thethe PharmaceuticalPharmaceutical IndustryIndustry ,, JJ.. MedMed.. ChemChem.. 20132013,, 5656,, 56595659;; LJSLJS KnutsenKnutsen,,
DrugDrug discoverydiscovery management,management, smallsmall isis stillstill beautifulbeautiful:: WhyWhy aa numbernumber ofof companiescompanies getget itit wrongwrong,, DrugDrug
DiscovDiscov.. TodayToday 20112011,, 1616,, 476476..
New chemical entities 1993-2012
The The The The The The The The drugdrugdrugdrugdrugdrugdrugdrug world world world world world world world world marketmarketmarketmarketmarketmarketmarketmarket, in , in , in , in , in , in , in , in 2012 2012 2012 2012 2012 2012 2012 2012 = = = = = = = = cacacacacacacaca. . . . . . . . US$ US$ US$ US$ US$ US$ US$ US$ 895 895 895 895 895 895 895 895 bibibibibibibibi
“The productivity gap”“The productivity gap”
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= = ffully ully iintegrated ntegrated ppharmaceutical harmaceutical ccompanyompany
To To ffully ully iintegrated ntegrated ppharmaceutical harmaceutical nnetworketwork
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The scientific manpowerThe scientific manpower
SourceSource: C. H. Brito Cruz & C. A. Pacheco, “Conhecimento & Inovação: Desafios do Brasil : C. H. Brito Cruz & C. A. Pacheco, “Conhecimento & Inovação: Desafios do Brasil no Século no Século XXI”, XXI”, atat
www.inovacao.unicamp.br/report/intcwww.inovacao.unicamp.br/report/intc--pachecopacheco--brito.pdfbrito.pdf (2009/01)(2009/01)
TheThe NationalNational InstitutesInstitutes ofof ScienceScience andand TechnologyTechnology (INCT’s)(INCT’s) programprogram
hashas ambitiousambitious andand largelarge goalsgoals inin termsterms ofof mobilizingmobilizing nationalnational efforteffort ofof
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ofof science,science, toto contributecontribute forfor sustainablesustainable developmentdevelopment ofof thethe countrycountry..
INCT-INOFAR
www.inctwww.inct--inofar.ccs.ufrj.brinofar.ccs.ufrj.br
GovernanceGovernance
committeecommittee
INCT-INOFAR
The TeamThe Team
INCT-INOFAR
Radical Radical InInovationovationRadical Radical InInovationovation
Discovery of novel Discovery of novel
anticancer drug anticancer drug anticancer drug anticancer drug
candidates designed as candidates designed as
novel novel combretastatincombretastatin
A4 analogues A4 analogues
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PCT BR 2013 000095PCT BR 2013 000095
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lung diseases in mice lung diseases in mice
Laboratory of Laboratory of
Inflammation Inflammation
FIOCRUZ, RJFIOCRUZ, RJ
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new new NN--acylhydrazone acylhydrazone
derivatives and analogues derivatives and analogues
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In Brazil the market ofIn Brazil the market of
ActActive pharmaceutical ingredients ive pharmaceutical ingredients
(API’s)
Generic drugsGeneric drugs*
"The art is to select [generics] that will be winners versus ones where there will be enormous competition.“
M McCoy, Generic Drugs, M McCoy, Generic Drugs, C&ENC&EN 20022002 (#13) (#13) 8080, 23, 23
In Brazil the market ofIn Brazil the market of
generic drugs isgeneric drugs is
caca. . 23,5% (2012)23,5% (2012)((BR BR LowLow # 9787, 02/10/1999) # 9787, 02/10/1999) > 92%
•• AtorvastatinAtorvastatin19911991
•• NewNew stereoselectivestereoselective synthesissynthesis byby
Professor Professor Luiz Carlos DiasLuiz Carlos Dias & &
DrDr Adriano S. VieiraAdriano S. Vieira, UNICAMP, SP , UNICAMP, SP
(2010) (2010) –– INPI INPI PatentPatent, 2011 (BR), 2011 (BR)
super blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbuster––––––––drugdrugdrugdrugdrugdrugdrugdrug
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functionalized functionalized
pyrrolheptenoicpyrrolheptenoic acidacid
•• PatentPatent US 5273995 Pfizer (1991)US 5273995 Pfizer (1991)
LipitorLipitorTMTM
•• SunitinibSunitinib
World total sales: World total sales:
US$ > 120 bi US$ > 120 bi (1991(1991--2011)2011)
super blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbustersuper blockbuster––––––––drugdrugdrugdrugdrugdrugdrugdrug
**PatentPatent US 7211600 (2001) US 7211600 (2001)
•• SunitinibSunitinib20062006
SutentSutentTMTM••Multi TK Multi TK inhibitorinhibitor indicatedindicated to renal carcinoma to renal carcinoma
functionalizedfunctionalized
22--oxooxo--11HH--indol indol --11HH--pyrrolepyrrole--33--carboxamidecarboxamide
•• Total Total synthesissynthesis Professor Professor AngeloAngelo da Cunha da Cunha Pinto Pinto & Dra & Dra Bárbara Vasconcellos da SilvaBárbara Vasconcellos da SilvaUFRJ, RJ (UFRJ, RJ (20112011) (BR)) (BR)
Total sales of Total sales of tinibstinibs inin
US market: US$ 18,5 biUS market: US$ 18,5 bi
(2009)(2009)
AnnualAnnual ActivitiesActivities ReportReport
www.inctwww.inct--inofar.ccs.ufrj.br/download/aar/2012.pdfinofar.ccs.ufrj.br/download/aar/2012.pdf
Coordinator:Coordinator:
EliezerEliezer J. BarreiroJ. Barreiro
““For For allall thethe effortsefforts toto industrializeindustrialize andand
automateautomate discoverydiscovery,, historyhistory suggestssuggests
drugdrug discoverydiscovery is is artart
as as wellwell as as sciencescience andand reliesrelies heavilyheavily onon
FinalFinal remarksremarks
as as wellwell as as sciencescience andand reliesrelies heavilyheavily onon
thethe skillskill ofof experiencedexperienced drugdrug
huntershunters...“...“
Charles H. ReynoldsCharles H. Reynolds
Johnson & Johnson Pharmaceutical Research and Development, Spring House, PaJohnson & Johnson Pharmaceutical Research and Development, Spring House, Pa
em em Pharma'sPharma's Road AheadRoad Ahead ,, C&ENC&EN SpecialSpecial IssueIssue, , Volume 84, number 25, Volume 84, number 25, JuneJune 19, 200619, 2006
www.inct-inofar.ccs.ufrj.br
ThankThank youyou for for youryour attentionattention
AcknowledgmentsAcknowledgments
eliezer 2013