Table of Contents for Kinase Inhibitors
INTRODUCTION
STUDY GOALS AND OBJECTIVES
REASONS FOR DOING THIS STUDY
CONTRIBUTIONS TO THE STUDY AND FOR WHOM
SCOPE AND FORMAT
METHODOLOGY
INFORMATION SOURCES
AUTHOR'S CREDENTIALS
RELATED BCC WORK CREDENTIALS
BCC ONLINE SERVICES
DISCLAIMER
SUMMARY
Summary Table:
GLOBAL FORECAST OF MARKET FOR KINASE INHIBITORS BY TYPE, THROUGH 2010 ($ MILLIONS)
Summary Figure:
GLOBAL FORECAST OF MARKET FOR KINASE INHIBITORS BY TYPE, 2002-2010 ($ MILLION)
OVERVIEW
THE CELLULAR ROLE OF KINASES
INHIBITORS OF PROTEIN KINASES
KINASES AS ATTRACTIVE DRUG TARGETS
Table 1 ATTRACTIVE FEATURES OF PROTEIN KINASES
KINASE INHIBITORS IN CLINICAL USE AND CLINICAL TRIALS
Table 2 FDA-APPROVED* KINASE INHIBITORS
Table 3 KINASE INHIBITORS IN CLINICAL TRIALS
Table 4 NUMBER OF KINASE INHIBITORS IN CLINICAL TRIALS, BY PHASE
Table 5 COMPANIES WITH KINASE INHIBITORS IN CLINICAL TRIALS
DATABASES AND LARGE SCALE INITIATIVES
Table 6 KINASE DATABASES
KINBASE
KINASENET
KINASE SEQUENCE DATABASE (KSD)
KINMUTBASE
SCANSITE
TECHNOLOGY OVERVIEW
DEVELOPMENT PROCESS
TYPES OF KINASE INHIBITORS
Table 7 COMPARISON OF TYPES OF INHIBITORS
SMALL MOLECULE KINASE INHIBITORS
Mechanisms of Small-Molecule Inhibitors
Table 8 COMPARISON OF ATP COMPETITIVE AND NONCOMPETITIVE INHIBITORS
ATP Competitive Inhibitors
Non-ATP Competitive Inhibitors
MONOCLONAL ANTIBODIES
ISSUES OF SPECIFICITY
ISSUES OF SPECIFICITY (CONINUED)
PROTEIN STRUCTURE AND MODELING
RATIONAL DESIGN
PATENT EVALUATION
PATENT SHARE BY KINASE TYPE
Table 9 KINASE INHIBITOR PATENTS BY TARGET MOLECULE, AUGUST 2003 TO AUGUST 2005
Table 10 KINASE INHIBITOR PATENTS BY DISEASE, AUGUST 2003 TO AUGUST 2005
RECENT PATENTS OF SIGNIFICANCE
PHARMACIA CORP. P38 INHIBITOR
CYCLACEL CDK INHIBITORS
PARKER HUGHES INSTITUTE PATENT ON EGFR INHIBITORS AND MODEL
Table 11 KINASE INHIBITOR PATENTS BY ASSIGNEE
Table 12 KINASE INHIBITOR PATENTS BY REGION, 2004
MARKET FOR RECEPTOR TYROSINE KINASE INHIBITORS
TOTAL MARKET SIZE
Table 13 GLOBAL FORECAST FOR RECEPTOR TYROSINE KINASE INHIBITORS MARKET BY PRODUCT, THROUGH 2010 ($ MILLIONS)
Figure 1 GLOBAL FORECAST FOR RECEPTOR TYROSINE KINASE INHIBITORS MARKET BY PRODUCT, 2002-2010 ($ MILLIONS)
RECEPTOR TYROSINE KINASE BIOLOGY
INHIBITORS OF ERBB/HER FAMILY PROTEIN KINASES
EGFR INHIBITORS
IN CLINICAL USE
Erbitux (cetuximab)
Tarceva (Erlotinib)
Iressa (gefitinib)
FDA Approval in the United States
Fast Track Approval in Japan
Post-Market Studies of Iressa
GLOBAL MARKET FOR EGFR INHIBITORS
Table 14 GLOBAL MARKET FOR EGFR INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
IN DEVELOPMENT
PKI-166
Canertinib (CI-1033)
SU-11464
Matuzumab (Emd7200)
EKB-569
Zd6474
HER2 INHIBITORS
IN CLINICAL USE
Herceptin
HER2 INHIBITORS IN CLINICAL DEVELOPMENT
GW-572016 (lapatinib ditosylate)
GLOBAL MARKET FOR HER2 INHIBITORS
Table 15 GLOBAL MARKET FOR HER2 INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
VEGF RECEPTOR TYROSINE KINASES
OVERVIEW
VEGF RECEPTOR KINASE INHIBITORS IN DEVELOPMENT
Zd6474
PKC-412
Sutent (formerly SU-11248)
Vatalanib (Ptk787/ZK222584)
FLT3 KINASE
OVERVIEW
FLT3 INHIBITORS IN CLINICAL DEVELOPMENT
CEP-701
PKC-412
SU5614
Sutent (Formerly SU11248)
MLN518
XL999
VX-322
MARKET FOR NON-RECEPTOR TYROSINE KINASE INHIBITORS
TOTAL MARKET SIZE AND BACKGROUND
Table 16 GLOBAL FORECAST FOR NONRECEPTOR TYROSINE KINASE INHIBITORS MARKET BY PRODUCT, THROUGH 2010 ($ MILLIONS)
Figure 2 GLOBAL FORECAST FOR NONRECEPTOR TYROSINE KINASE INHIBITORS MARKET, 2002-2010 ($ MILLIONS)
ABL KINASES
ABL INHIBITORS IN CLINICAL USE
Gleevec
GLOBAL MARKET FOR ABL INHIBITORS
Table 17 GLOBAL FORECAST FOR ABL INHIBITORS MARKET BY REGION, THROUGH 2010 ($ MILLIONS)
SRC KINASES
OVERVIEW
SRC KINASE INHIBITORS IN DEVELOPMENT
Azd0530
BMS-354825
SKI-606
TARGEGEN INHIBITOR
JANUS (JAK) KINASES
OVERVIEW
JAK INHIBITORS IN DEVELOPMENT
CP-690
AG-490
WHI-P154, WHI-P131
MARKET FOR SERINE-THREONINE KINASE INHIBITORS
TOTAL MARKET SIZE
Table 18 GLOBAL FORECAST FOR SERINE-THREONINE KINASE INHIBITORS MARKET BY PRODUCT, THROUGH 2010 ($ MILLIONS)
Figure 3 GLOBAL FORECAST FOR SERINE-THREONINE KINASE INHIBITORS MARKET BY PRODUCT, 2002-2010 ($ MILLIONS)
MTOR KINASES
OVERVIEW
MTOR INHIBITORS IN CLINICAL USE
Rapamune
Certican (Everolimus)
GLOBAL MARKET FOR MTOR INHIBITORS
Table 19 GLOBAL MARKET FOR MTOR INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
MTOR INHIBITORS IN DEVELOPMENT
AP23573
RHO KINASES
OVERVIEW
RHO KINASE FAMILY INHIBITORS IN CLINICAL USE
Eril (Fasudil hydrochloride)
GLOBAL MARKET FOR RHO KINASE INHIBITORS
Table 20 GLOBAL MARKET FOR RHO KINASE INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
CYCLIN DEPENDENT KINASES
OVERVIEW
CDK INHIBITORS IN CLINICAL DEVELOPMENT
Flavopiridol
Seliciclib (CYC202, roscovitine)
SNS-032 (formerly BMS-387032)
PROTEIN KINASE C (PKC)
OVERVIEW
PKC INHIBITORS IN CLINICAL DEVELOPMENT
Ruboxistaurin
Pkc412
Bryostatin
KAI-9803
PHOSPHATIDYLINOSITOL-3-KINASE (PI3K)
OVERVIEW
PI3 KINASE INHIBITORS IN CLINICAL DEVELOPMENT
SF1126
AURORA KINASES
OVERVIEW
AURORA KINASE INHIBITORS IN CLINICAL DEVELOPMENT
VX-680
Azd1152
MAP/MEK KINASES
OVERVIEW
MAPK/MEK INHIBITORS IN CLINICAL DEVELOPMENT
Arry-142886 (AZD-6244)
SCIO-469
GW681323 (SB-681323)
JUN N-TERMINAL KINASES (JNK)
OVERVIEW
JNK INHIBITORS IN CLINICAL DEVELOPMENT
CC-401
CEP-1347
MARKET FOR KINASE INHIBITORS BY DISEASE APPLICATION
TOTAL MARKET SIZE
Table 21 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET BY CURRENT APPLICATIONS, THROUGH 2010 ($ MILLION)
CURRENT APPLICATIONS
CANCER
Market Size by Kinase Inhibitors
Table 22 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET IN CANCER TREATMENT BY PRODUCT, THROUGH 2010 ($ MILLIONS)
Types of Cancer
Lung Cancer
EGFR Inhibitors for lung cancer treatment
Breast Cancer
ERB/HER2 inhibitors for breast cancer treatment
CDK Inhibitors for Breast Cancer Treatment
Leukemias
Chronic myeloid leukemia (CML)
Acute myeloid leukemia (AML)
BCR-ABL Inhibitors for leukemia treatment
Flt3 Inhibitors for leukemia treatment
Colorectal Cancer
EGFR inhibitors for colorectal cancer
Pancreatic Cancer
EGFR inhibitors for pancreatic cancer treatment
Skin Cancers
Basal cell carcinoma
Squamous Cell Carcinoma
Melanoma
EGFR inhibitors for skin cancer treatment
MAPK/ERK Inhibitors for skin cancer Treatment
PKC Inhibitors for skin cancer Treatment
PI3K Inhibitors for skin cancer Treatment
Ras/Raf Inhibitors in Skin Cancer Treatment
IMMUNE AND INFLAMMATORY DISEASES
Market size by Kinase Inhibitors
Table 23 WORLDWIDE MARKET FOR KINASE INHIBITORS IN IMMUNE AND INFLAMMATORY DISEASE BY PRODUCT, THROUGH 2010 (UNITS MILLIONS)
Immunosuppression for Organ transplantation
mTOR inhibitors for Immunosuppression
Asthma
MAPK Inhibitors in Asthma Treatment
Arthritis
MAPK Inhibitors in Arthritis Treatment
CARDIOVASCULAR DISEASE
Market Size by Kinase Inhibitors
Table 24 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET IN CARDIOVASCULAR DISEASE TREATMENT BY PRODUCT, THROUGH 2010 ($ MILLION)
Rho Kinases for Cardiovascular Disease
MAPK Inhibitors for Cardiovascular Treatment
MEK/MAPK1 Inhibitors for Cardiovascular Disease
JNK inhibitors for Cardiovascular disease
EMERGING APPLICATIONS
DIABETES
VEGF Inhibitors for Treatment of Diabetes
FLT3 Inhibitors for Treatment of Diabetes
PKC Inhibitors in the Treatment of Diabetes
MACULAR DEGENERATION
VEGF Inhibitors for Macular Degeneration
NEUROLOGICAL DISEASE
GSK kinase Inhibitors for Neurological Disease
CDK inhibitors for Neurological Disease
MAJOR COMPANIES AND MARKET SHARE
MARKET SHARES
Table 25 SALES AND MARKET SHARE OF COMPANIES INVOLVED IN KINASE INHIBITORS, 2005 ($ MILLIONS AND %)
Table 26 SALES AND MARKET SHARE OF COMPANIES INVOLVED IN TYROSINE KINASE INHIBITORS, 2005 ($ MILLIONS AND %)
Table 27 SALES AND MARKET SHARE OF COMPANIES INVOLVED IN SERINE THREONINE KINASE INHIBITORS, 2005 ($ MILLIONS AND %)
COMPANY PROFILES
AMBIT BIOSCIENCES
AMGEN
ARIAD PHARMACEUTICALS
ASTRAZENECA
BOEHRINGER INGELHEIM
CEPHALON INC.
CEPTYR, INC.
CGI PHARMACEUTICALS, INC
CHIRON, INC.
CYCLACEL LIMITED
EXELIXIS
GENENTECH INC.
GLAXOSMITHKLINE
GPC BIOTECH AG
IMCLONE SYSTEMS
KAI PHARMACEUTICALS
KÉMIA
KINEXUS BIOINFORMATICS CORP.
MERCK AND CO.
MILLENIUM PHARMACEUTICALS
MYRIAD GENETICS, INC.
NOVARTIS
PFIZER INC.
ROCHE (F. HOFFMANN-LA ROCHE LTD)
SANOFI-AVENTIS
SCIOS
TARGEGEN
VERTEX
WYETH-AYERST
INTERNATIONAL ASPECTS AND REGULATORY ISSUES
MARKET BY REGION
Table 28 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET BY REGION, THROUGH 2010 ($ MILLIONS)
Figure 4 REGIONAL SHARE OF GLOBAL MARKET FOR KINASE INHIBITORS, 2005 AND 2010 (%)
UNITED STATES
DRUG WITHDRAWALS
Vioxx
Iressa
CONSUMER CONFIDENCE
MEDICARE
EUROPEAN UNION
NEW DRUG APPROVALS AND INNOVATION
COSTS OF DRUG DEVELOPMENT
RELOCATION OF R&D
REGULATORY CLIMATE
JAPAN
NEW DRUG APPROVALS
REGULATORY CLIMATE
RELATIONSHIP OF ACADEMIA AND INDUSTRY
VENTURE CAPITAL
FUTURE DIRECTIONS
SPECIFICITY AND COMPLEXITY
RESISTANCE
KINASE ACTIVATORS
DEVELOPMENTS IN ENABLING TECHNOLOGIES
PHOSPHORYLATION-STATE ANTIBODIES
HIGH THROUGHPUT KINASE ASSAYS
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