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市場調査レポート
腫瘍学におけるプロテインキナーゼ阻害薬の戦略的見解
Strategic Outlook on Protein Kinase Inhibitors in Oncology
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Abstract
Since the discovery that the v-Src oncogene encoded a protein kinase in 1978,
kinases have become a targeted therapy strategy in oncology for the
pharmaceutical industry. The perfect date between Gleevec and Chronic Myeloid
Leukemia (CML) will be hard to achieve by other inhibitors currently in
development, because of CML・ strong link to a sole pathogenic event - the
Philadelphia chromosome. Thus, it is expected that multiple inhibitors may
have to be used together to effect higher cure rates in cancers with multiple
genetic abnormalities.
Scope of this report
Drugs according to protein kinase target; Dual or multiple kinase inhibitor
analysis Targets according to indication Competitive landscape assessment
Protein kinase inhibitors on market Thorough review of the seven largest
cancer indications in the field of protein kinase inhibitors
Research and analysis highlights
The number of protein kinase inhibitor (PKI) drugs has risen sharply, as the
number of targets. The fiercest competition in PKI drug development is found
in breast, lung, leukemia, prostate, and colorectal cancer. Several big pharma
companies are out hunting for promising technology and drugs to complement
their internal pipeline.
Key reasons to read this report
- Understand the clinical and strategic challenges to the commercialization
of protein kinase inhibitor treatments
- Assess opportunities and risks for the continued development of innovative
developmental treatments
- Adopt knowledge from this analysis to drive strategic planning decisions
in oncology drug developmentTable of Contents
Table of Contents
- 1 Executive Summary _______________________________________________2
- 2 Cancer Highlights ________________________________________________3
- 3 Methodology_____________________________________________________4
- 4 Table of Contents _________________________________________________6
- 4.1 List of Boxes______________________________________________________ 7
- 4.2 List of Figures ____________________________________________________
7
- 4.3 List of Tables _____________________________________________________
7
- 5 Rationale for Development of Kinase Inhibitors in Oncology______________9
- 6 Protein Kinase Targets -- A Growing Family __________________________11
- 6.1 Challenges in Protein Kinase Drug Discovery
_________________________ 15
- 6.1.1 Enabling Structure-Based Drug Design is the Key
____________________________15
- 6.1.2 Specific Kinase Inhibitors without Kinase Profiling?
__________________________16
- 6.2 Drugs according to Target _________________________________________
19
- 6.2.1 Cyclin-dependent Kinase Target Inhibitors
__________________________________19
- 6.2.2 Aurora Kinase Target Inhibitors
__________________________________________21
- 6.2.3 Cell Cycle Checkpoint Target Controls Inhibitors
____________________________22
- 6.2.4 Tyrosine Kinase Receptor Inhibitors
_______________________________________23
- 6.2.5 Other Serine/Threonine Kinase Target Inhibitors
_____________________________32
- 6.3 Dual or Multiple Kinase Inhibitor Analysis
___________________________ 35
- 6.3.1 Presentation of Drugs Targeting A to F Kinases
______________________________35
- 6.3.2 Presentation of Drugs Targeting G to T Kinases
______________________________38
- 6.4 Targets According to Indication ____________________________________
41
- 6.4.1 Breast
Cancer_________________________________________________________41
- 6.4.2 Prostate Cancer: What Cannot be Found in the
'Groins'?_______________________42
- 6.4.3 Lung Cancer: A Need for Improved Survival Rates
___________________________43
- 6.4.4 Colorectal Cancer: EGFR & VEGFR are Strong Targets but there are
Others _______45
- 6.4.5 Leukemia: Show Me the Power of PKI
_____________________________________47
- 6.4.6 Melanoma
___________________________________________________________48
- 6.4.7 Lymphoma: We Are In
_________________________________________________50
- 7 Growing Competition in the Field___________________________________51
- 7.1 Big Pharma Outlook: The Race is On________________________________ 52
- 7.1.1 Novartis Deals - Digs Deeper into Cell Cycle
Inhibitors________________________52
- 7.1.2 AstraZeneca -- Wheeling and Dealing
______________________________________55
- 7.1.3 Pfizer's Long Look at OSI Pharmaceuticals
_________________________________57
- 7.1.4 GlaxoSmithKline Gains Momentum
_______________________________________59
- 7.2 Strategic Deals Creating Competitive Edge
___________________________ 61
- 7.2.1 Mergers
_____________________________________________________________61
- 7.2.2 Astex -- the PKI
Switchboard_____________________________________________62
- 7.2.3 Big Pharma's Darling
__________________________________________________63
- 8 Current Protein Kinase Inhibitors in Therapy _________________________65
- 8.1 Mechanism, Target and Developmental History _______________________
65
- 8.2 Approvals: Indications & Markets __________________________________
69
- 9 Protein Kinase Inhibitors in Drug Development -- A Progress
Analysis_____72
- 9.1 Progress Analysis - Breast Cancer___________________________________
74
- 9.2 Progress Analysis - Prostate Cancer
_________________________________ 76
- 9.3 Progress Analysis - Lung Cancer____________________________________
78
- 9.4 Progress Analysis - Colorectal Cancer
_______________________________ 81
- 9.5 Progress Analysis - Leukemia ______________________________________
84
- 9.6 Progress Analysis -- Melanoma _____________________________________
87
- 9.7 Progress Analysis - Lymphoma _____________________________________ 88
- 10 Selected Company profiles_______________________________________91
- 11 Disclaimer____________________________________________________98
- 12 Drug Index ___________________________________________________99
- 13 Company Index ______________________________________________105
4.1 List of Boxes
- Box 1: The Power of Ambit's Kinase Profiling
......................................................................................17
- Box 2: Summary Terms of the Exelixis
Transaction...............................................................................60
4.2 List of Figures
- Figure 1: Top 10 PKI Drug Developing
Companies_______________________________________51
- Figure 2: Clinical Trial Distribution in Breast Cancer for PKI
Drugs_________________________74
- Figure 3: Clinical Trial Distribution in Prostate Cancer for PKI Drugs
_______________________77
- Figure 4: Clinical Trial Distribution in Lung Cancer for PKI
Drugs__________________________79
- Figure 5: Clinical Trial Distribution in Colorectal Cancer for PKI Drugs
_____________________82
- Figure 6: Clinical Trial Distribution in Leukemia for PKI Drugs
____________________________85
- Figure 7: Clinical Trial Distribution in Melanoma for PKI
Drugs____________________________87
- Figure 8: Clinical Trial Distribution in Lymphoma for PKI Drugs
___________________________89
4.3 List of Tables
- Table 1: Overview of Targets in Commercial Development
_________________________________14
- Table 2: Cyclin-dependent Kinase Targets in Development
_________________________________20
- Table 3: Aurora Kinase Targets in Development
_________________________________________22
- Table 4: Cell Cycle Checkpoint Targets in Development
___________________________________23
- Table 5: Epidermal Growth Factor Receptor Targets in Development
________________________25
- Table 6: FMS-like tyrosine kinases and their
Synonyms____________________________________26
- Table 7: Fms-related Tyrosine Kinase Targets in Development
______________________________28
- Table 8: Platelet-derived Growth Factor Receptor Targets in Development
____________________29
- Table 9: Kinase Insert Domain Targets in Development
___________________________________30
- Table 10: Drugs in Development Targeting the PI3K/Akt/mTOR pathway
_____________________31
- Table 11: Drugs in Development Targeting the Ras-Raf-MEK-ERK (ERK) pathway
_____________32
- Table 12: Serine/Threonine Kinase Inhibitors in Development
______________________________33
- Table 13: Protein Kinase Targets in Clinical Trials for Breast Cancer
________________________41
- Table 14: Protein Kinase Targets in Clinical Trials for Prostate Cancer
______________________42
- Table 15: Protein Kinase Targets in Clinical Trials for Lung Cancer
_________________________44
- Table 16: Protein Kinase Targets in Clinical Trials for Colorectal
Cancer_____________________46
- Table 17: Protein Kinase Targets in Clinical Trials for Leukemia
____________________________48
- Table 18: Protein Kinase Targets in Clinical Trials for Melanoma
___________________________49
- Table 19: Protein Kinase Targets in Clinical Trials for
Lymphoma___________________________50
- Table 20: Drugs in Therapy -- Mechanism &
Targets______________________________________65
- Table 21: Current and Developmental History of PKI Drugs in Therapy
______________________68
- Table 22: Approvals: Indications & Markets
____________________________________________71
- Table 23: Top 10 Drugs in Terms of Number of Clinical Trials
______________________________72
- Table 24: List of Cancer Indications Targeted by Protein Kinase Inhibitors
____________________73
- Table 25: PKI Drugs in Development for Breast Cancer
___________________________________76
- Table 26: PKI Drugs in Development for Prostate
Cancer__________________________________78
- Table 27: PKI Drugs in Development for Lung Cancer
____________________________________80
- Table 28: PKI Drugs in Development for Colorectal
Cancer________________________________83
- Table 29: PKI Drugs in Development for Leukemia
_______________________________________86
- Table 30: PKI Drugs in Development for Melanoma
______________________________________88
- Table 31: PKI Drugs in Development for
Lymphoma______________________________________89
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