Kinase Inhibitors

Table of Contents

• INTRODUCTION
  • STUDY GOALS AND OBJECTIVES
  • REASONS FOR DOING THIS STUDY
  • CONTRIBUTIONS TO THE STUDY AND FOR WHOM
  • SCOPE AND FORMAT
  • METHODOLOGY
  • INFORMATION SOURCES
  • AUTHORS 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
    • INHIBITORS OF PROTEIN KINASES (CONTINUED)
  • 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 3 (CONTINUED)
  • 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
    • Parker Hughes Institute Patent...(Continued)
• 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)
          • Erbitux (Cetuximab) (Continued)
        • Tarceva (Erlotinib)
          • Tarceva (Erlotinib) (Continud)
        • 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)
    • Post-Market Studies...(continued)
    • 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)
          • GW-572016...(Continued)
      • GLOBAL MARKET FOR HER2 INHIBITORS
  • Table 15 GLOBAL MARKET FOR HER2 INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
    • Global Market for Her2 Inhibitors (Continued)
    • 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
          • VX-322 (Continued)
• 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
          • Ruboxistaurin (Continued)
        • 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
      • MAPK Inhibitors for... (Continued)
    • 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 %)
    • MARKET SHARES (CONTINUED)
• 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
    • VERTEX (CONTINUED)
  • 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
        • Venture Capital (Continued)
• FUTURE DIRECTIONS
  • SPECIFICITY AND COMPLEXITY
  • RESISTANCE
  • KINASE ACTIVATORS
  • DEVELOPMENTS IN ENABLING TECHNOLOGIES
    • PHOSPHORYLATION-STATE ANTIBODIES
      • Phosphorylation-State Antibodies (Continued)
    • HIGH THROUGHPUT KINASE ASSAYS
      • High Throughput Kinase Assays (Continued)
• LIST OF TABLES
• Summary Table:
• Table 1 ATTRACTIVE FEATURES OF PROTEIN KINASES
• 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
• Table 6 KINASE DATABASES
• Table 7 COMPARISON OF TYPES OF INHIBITORS
• Table 8 COMPARISON OF ATP COMPETITIVE AND NONCOMPETITIVE INHIBITORS
• 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
• Table 11 KINASE INHIBITOR PATENTS BY ASSIGNEE
• Table 12 KINASE INHIBITOR PATENTS BY REGION, 2004
• Table 13 GLOBAL FORECAST FOR RECEPTOR TYROSINE KINASE INHIBITORS MARKET BY PRODUCT, THROUGH 2010 ($ MILLIONS)
• Table 14 GLOBAL MARKET FOR EGFR INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
• Table 15 GLOBAL MARKET FOR HER2 INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
• Table 16 GLOBAL FORECAST FOR NONRECEPTOR TYROSINE KINASE INHIBITORS MARKET BY PRODUCT, THROUGH 2010 ($ MILLIONS)
• Table 17 GLOBAL FORECAST FOR ABL INHIBITORS MARKET BY REGION, THROUGH 2010 ($ MILLIONS)
• Table 18 GLOBAL FORECAST FOR SERINE-THREONINE KINASE INHIBITORS MARKET BY PRODUCT, THROUGH 2010 ($ MILLIONS)
• Table 19 GLOBAL MARKET FOR MTOR INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
• Table 20 GLOBAL MARKET FOR RHO KINASE INHIBITORS BY REGION, THROUGH 2010 ($ MILLIONS)
• Table 21 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET BY CURRENT APPLICATIONS, THROUGH 2010 (UNIT?)
• Table 22 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET IN CANCER TREATMENT BY PRODUCT, THROUGH 2010 ($ MILLIONS)
• Table 23 WORLDWIDE MARKET FOR KINASE INHIBITORS IN IMMUNE AND INFLAMMATORY DISEASE BY PRODUCT, THROUGH 2010 (UNITS MILLIONS)
• Table 24 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET IN CARDIOVASCULAR DISEASE TREATMENT BY PRODUCT, THROUGH 2010 ($ MILLION)
• 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 %)
• Table 28 GLOBAL FORECAST FOR KINASE INHIBITORS MARKET BY REGION, THROUGH 2010 ($ MILLIONS)
• LIST OF FIGURES
• Summary Figure:
• Figure 1 GLOBAL FORECAST FOR RECEPTOR TYROSINE KINASE INHIBITORS MARKET BY PRODUCT, 2002-2010 ($ MILLIONS)
• Figure 2 GLOBAL FORECAST FOR NONRECEPTOR TYROSINE KINASE INHIBITORS MARKET, 2002-2010 ($ MILLIONS)
• Figure 3 GLOBAL FORECAST FOR SERINE-THREONINE KINASE INHIBITORS MARKET BY PRODUCT, 2002-2010 ($ MILLIONS)
• Figure 4 REGIONAL SHARE OF GLOBAL MARKET FOR KINASE INHIBITORS, 2005 AND 2010 (%)