Transforming Drug Discovery Innovative Platforms Transforming Drug Discovery Transforming Drug Discovery Innovative Innovative Platforms Platforms Martin Mackay, Ph.D. Martin Mackay, Ph.D. Senior Vice President Senior Vice President Worldwide Research and Technology Worldwide Research and Technology Valid as of November 30, 2006
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Transforming Drug Discovery Innovative ...€¦ · Drug Discovery at Scale PDE-1b – ADHD PDE-2 – Bone Healing, Cognition, Inflammatory Pain PDE-4 – COPD, Asthma PDE-4B – Cognition
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Transforming Drug DiscoveryInnovative Platforms
Transforming Drug DiscoveryTransforming Drug DiscoveryInnovativeInnovative PlatformsPlatforms
Martin Mackay, Ph.D.Martin Mackay, Ph.D.Senior Vice PresidentSenior Vice President
Worldwide Research and TechnologyWorldwide Research and Technology
A New Era of Kinase InhibitorsA New Era of Kinase Inhibitors
Janus Kinase 3 (JAK 3)Janus Kinase 3 (JAK 3)
cc--MetMet
Valid as of November 30, 2006
CPCP--690,550 690,550 Shows Potential Across Many DiseasesShows Potential Across Many Diseases
Human Genetics Human Genetics Implicated JAK 3 as Implicated JAK 3 as Target for ImmuneTarget for Immune--System DisordersSystem Disorders
CPCP--690,550 Shown to be 690,550 Shown to be Effective in Organ Effective in Organ TransplantTransplant
Rheumatoid Arthritis is Rheumatoid Arthritis is an Autoimmune Disorder an Autoimmune Disorder Hence our Desire to Test Hence our Desire to Test in this Indicationin this Indication
Valid as of November 30, 2006
CPCP--690,550 690,550 Promising Results in RAPromising Results in RA
Patients With ACR20 Response (%)Patients With ACR20 Response (%)Patients With ACR20 Response (%)
0
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80
100
0 2 4 6
Weeks
5 mg 15 mg 30 mg Placebo
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80
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0 2 4 6
Weeks
5 mg 15 mg 30 mg Placebo
CP-690,550CPCP--690,550690,550
0
20
40
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80
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0 2 4 6 8 10 12
Weeks
20 mg 40 mg 80 mg Placebo
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0 2 4 6 8 10 12
Weeks
20 mg 40 mg 80 mg Placebo
Humira®HumiraHumira®®
Valid as of November 30, 2006
cc--Met Inhibitors Met Inhibitors Offer a New Treatment for CancerOffer a New Treatment for Cancer
Tumor Invasion and MetastasisTumor Invasion and Metastasis
Tumor AngiogenesisTumor Angiogenesis
Valid as of November 30, 2006
PFPF--2,341,066 2,341,066 Significantly Reduces Tumor Burden in MiceSignificantly Reduces Tumor Burden in Mice
PFPF--23410662341066
Tum
or V
olum
e (m
m3)
Tum
or V
olum
e (m
m3)
ControlControl
Time (days)Time (days)
16001600
12001200
800800
400400
001010 2020 3030 4040 60605050
Valid as of November 30, 2006
A Winning StrategyA Winning Strategy
Leading Kinase CollaborationsLeading Kinase CollaborationsLeading Kinase CollaborationsAcademic Institutions - e.g. Lauffenberger and Sorger, MIT, Kinase Pathway Analysis; I. Hunter, MIT, Novel Technology for Kinase-cmpd Analysis
Biotech Companies - e.g. Caliper, Biosource, Novel Kinase Screening Technologies
Kinase Drug Pfinder program e.g. J. Blenis-Harvard, S6K; J. Liao-B&W Hospital, Rho Kinase; Dr. Tsichlis-Tufts, Cot; L. Rameh-BBRI, PI5P4K
Academic Institutions - e.g. Lauffenberger and Sorger, MIT, Kinase Pathway Analysis; I. Hunter, MIT, Novel Technology for Kinase-cmpd Analysis
Biotech Companies - e.g. Caliper, Biosource, Novel Kinase Screening Technologies
Kinase Drug Pfinder program e.g. J. Blenis-Harvard, S6K; J. Liao-B&W Hospital, Rho Kinase; Dr. Tsichlis-Tufts, Cot; L. Rameh-BBRI, PI5P4K