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Innovations in Protein Kinase Therapies: Company Pipelines, Therapeutic Applications and Market Forecasts Product Image

Innovations in Protein Kinase Therapies: Company Pipelines, Therapeutic Applications and Market Forecasts

  • ID: 1060392
  • May 2009
  • 335 Pages
  • Scripp Business Insights

FEATURED COMPANIES

  • Abbott Laboratories
  • Array BioPharma Inc
  • Boehringer Ingelheim GmbH
  • Eli Lilly Co
  • Hoffmann-La Roche Ltd
  • Novartis International AG
  • MORE

During the last decade, approvals for several first-in-class kinase inhibitors have resulted in a wider recognition of kinases as an important class of drug targets. In the cancer market, there are now seven launched agents targeting EGFR family kinases, three agents targeting ABL family kinases and two which target VGFR family kinases. Although the kinase market is still relatively young, 173 kinase-related genes are now being targeted in drug developments.

'Innovations in Protein Kinase Therapies’ provides analysis of 608 kinase-targeting drugs in commercial development by 232 originating companies. This report identifies areas of innovation and opportunity for kinase targeting drugs in cancer and examines the non-cancer applications of kinase drugs across inflammatory and autoimmune diseases, restenosis, diabetes and other disorders. Leading kinase drug originating companies are profiled to reveal their drugs in development and co-development strategies. Global sales forecasts to 2013 for kinase-targeted drugs are also provided.

Examine kinase drug targets in cancer and other major indications and review the pipelines of leading kinase drug originating companies...

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FEATURED COMPANIES

  • Abbott Laboratories
  • Array BioPharma Inc
  • Boehringer Ingelheim GmbH
  • Eli Lilly Co
  • Hoffmann-La Roche Ltd
  • Novartis International AG
  • MORE

Executive Summary

Chapter 1 Kinases as drug targets

Summary

Introduction
Overview of human protein kinases
Classification schemes

Kinases in signal transduction pathways
MAPK pathways
MAPK (ERK) pathway
JNK/SAPK pathway
MAPK14 pathway
PI3K/AKT signaling
JAK/STAT signaling
NFKB pathway
Insulin receptor signaling
Immune cell signaling
T cell receptor signaling
B-cell receptor complexes
Signaling in vascular morphogenesis
VEGF receptor signaling
EGF receptor signaling
Cyclic nucleotide metabolism
Cell cycle checkpoint controls

Categories of kinase-targeted drugs
Small molecules
Monoclonal antibodies
Emerging biopharmaceuticals

Kinase drug audit

Chapter 2 Small molecule kinase inhibitor discovery

Summary

Introduction

Mechanisms of kinase inhibition
ATP competitive inhibitors
Irreversible inhibitors
Allosteric inhibitors

Approaches to kinase inhibitor discovery
Traditional kinase inhibitor discovery
High-throughput screening of compound libraries
Lead optimization
Synthesis of inhibitor analogs
Structure-informed drug design
Structure-informed drug re-design
Fragment-based drug discovery

Kinase inhibitor selectivity assays
Protein selectivity assays
Kinase activity assays
Kinase binding assays
Cellular selectivity assays

Identifying substrates of kinases

Chapter 3 Targeting kinases in cancer

Summary

Overview of cancer

Established and emerging therapies

Therapeutic potential of kinase inhibition
Types of kinase targets
Mutationally-activated kinases
Kinases which sustain tumor growth
Kinases with roles in tumorigenesis

Top 20 kinase targets

Group: TK
ABL1 (Abl family)
Target characteristics
Inhibitors on the market
Inhibitors in development
EGFR and ERBB2 (EGFR family)
Target characteristics
Approaches to EGFR inhibition
Inhibitors on the market
Inhibitors in development
FLT3, KIT, PDGFRA, and PDGFRB (PDGFR family)
Target characteristics
Inhibitors on the market
Inhibitors in development
FLT1, FLT4, and KDR (VEGFR family)
Target characteristics
Inhibitors on the market
Inhibitors in development
JAK2 (JakA family)
Target characteristics
Drugs in development
MET (Met family)
Target characteristics
Agents in development

Group: AGC
AKT1 (AKT family)
Target characteristics
Drugs in development

Group: CMGC
CDC2 and CDK2 (CDK family; CDC2 subfamily)
Target characteristics
Drugs in development

Group: Other
AURKA and AURKB (AUR family)
Target characteristics
Drugs in development
PLK1 (PLK family)
Target characteristics
Drugs in development

Group: Atypical
Target characteristics
Inhibitors on the market
Inhibitors in development

Dual specificity lipid/protein kinases
PIK3CA (PI3K)
Target characteristics
Inhibitors in development

Future trends

Chapter 4 Non-cancer applications of kinase drugs

Summary

Introduction

Chronic inflammation and kinases

Leading indications
Arthritis
Diabetes
Inflammation
Immunosuppression
Ophthalmology
Psoriasis
Pulmonary diseases
Cardiovascular
Myelodysplastic disorders
GI disorders
Pain

Leading kinase targets
MAPK14
Target characteristics
Inhibitors in development
FRAP1
Target characteristics
Inhibitors on the market
Inhibitors in development
JAK3
Target characteristics
Inhibitors in development
NTRK1
Target characteristics
Inhibitors in development
ROCK1
Target characteristics
Inhibitors on the market
Inhibitors in development

Chapter 5 Leading kinase drug originating companies

Summary/Introduction

5.1 Abbott Laboratories
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Ambit Biosciences Corp
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Amgen Inc
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Array BioPharma Inc
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

AstraZeneca plc
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Avila Therapeutics Inc
Company overview
Kinase drug pipeline

Boehringer Ingelheim GmbH
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Bristol-Myers Squibb Co
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Cephalon Inc
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Deciphera Pharmaceuticals LLC
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Eli Lilly Co
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Exelixis Inc
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

GlaxoSmithKline plc
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Hoffmann-La Roche Ltd
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Johnson & Johnson
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Kyowa Hakko Kirin Co Ltd
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Novartis International AG
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Pfizer Inc
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Sanofi-Aventis Group
Company overview
Kinase drug pipeline

Wyeth
Company overview
Kinase-related collaborations (2005 onwards)
Kinase drug pipeline

Chapter 6 Market Analysis: Trends and Forecasts

Summary

Prevalence of targeted diseases

Analyses and Forecasts by Type of Agent
Limus agents/mTOR inhibitors
Overview
Standalone mTOR inhibitors
Drug-eluting stents
Drug-eluting stent market
Sirolimus-eluting stents
Everolimus- and zotarolimus-eluting stents
Sales trends in mTOR inhibitors
Forthcoming mTOR inhibitors
EGFR Family inhibitors
Overview
Trastuzumab
Erlotinib
Cetuximab
Gefitinib
Panitumumab
Lapatinib
Nimotuzumab
Sales trends in EGFR Family inhibitors
Forthcoming EGFR Family Inhibitors
ABL/FLT3 Group Inhibitors
Overview
Imatinib
Dasatinib
Nilotinib
Sales trends in ABL1/FLT3 Family Inhibitors
Forthcoming ABL1/FLT3 Family Inhibitors
VEGFR Family
Overview
Sunitinib
Sorafenib
Sales trends in VEGFR Family inhibitors
Forthcoming VEGFR Family Inhibitors
Other launched agents
Overview
Fasudil
Pirfenidone
Sales trends of other agents
Other forthcoming agents

Company sales and trends

Patenting trends

Appendix 1 Kinase-related targets and their abbreviations

Appendix 2 Other abbreviations and acronyms

Appendix 3 Research Methodology

Index

List of Figures
Figure 1.1: Leading kinase-targeted drug applications
Figure 1.2: Kinase target landscape
Figure 6.3: Kinase originator market shares

List of Tables
Table 1.1: Human Kinase Gene Audit
Table 1.2: Hanks Classification of Protein Kinases (1995)
Table 1.3: Hanks Classification of Protein Kinases (1995) (continued)
Table 1.4: Kinase Agents by Development Stage
Table 1.5: Kinase Drugs by Product Type
Table 1.6: Leading developers of therapeutic kinase-targeted drugs
Table 1.7: Kinase Agonists and Stimulants
Table 3.8: Kinases implicated in human cancer
Table 3.9: Kinases implicated in human cancer (continued)
Table 3.10: Top 20 Kinase Targets in Cancer
Table 3.11: Overview of ABL1-targeted agents in cancer
Table 3.12: Overview of ABL1-targeted agents in cancer (continued 1)
Table 3.13: Overview of ABL1-targeted agents in cancer (continued 2)
Table 3.14: Overview of EGFR-targeted agents in cancer
Table 3.15: Overview of EGFR-targeted agents in cancer (Phase III and above)
Table 3.16: Overview of EGFR-targeted agents in cancer (Phase II)
Table 3.17: Overview of EGFR-targeted agents in cancer (Phase I)
Table 3.18: Overview of EGFR-targeted agents in cancer (Preclinical)
Table 3.19: Overview of ERBB2-targeted agents in cancer (Phase III and above)
Table 3.20: Overview of ERBB2-targeted agents in cancer (Phase II)
Table 3.21: Overview of ERBB2-targeted agents in cancer (Phase I and Preclinical)
Table 3.22: Overview of FLT3-targeted agents in cancer (Launched)
Table 3.23: Overview of FLT3-targeted agents in cancer (Phase II and III)
Table 3.24: Overview of FLT3-targeted agents in cancer (Phase I and II)
Table 3.25: Overview of FLT3-targeted agents in cancer (Preclinical and Phase I)
Table 3.26: Overview of KIT-targeted agents in cancer
Table 3.27: Overview of KIT-targeted agents in cancer (Continued 1)
Table 3.28: Overview of KIT-targeted agents in cancer (Continued 2)
Table 3.29: Overview of KIT-targeted agents in cancer (Continued 3)
Table 3.30: Overview of KIT-targeted agents in cancer (Continued 4)
Table 3.31: Overview of KIT-targeted agents in cancer (Continued 4)
Table 3.32: Overview of PDGFRA-targeted agents in cancer
Table 3.33: Overview of PDGFRA-targeted agents in cancer (Continued 1)
Table 3.34: Overview of PDGFRA-targeted agents in cancer (Continued 2)
Table 3.35: Overview of PDGFRA-targeted agents in cancer (Continued 3)
Table 3.36: Overview of PDGFRB-targeted agents in cancer (Phase II and Phase III)
Table 3.37: Overview of PDGFRB-targeted agents in cancer (Preclinical and Phase I)
Table 3.38: Overview of FLT1-targeted agents in cancer
Table 3.39: Overview of FLT1-targeted agents in cancer (Continued 1)
Table 3.40: Overview of FLT1-targeted agents in cancer (Continued 2)
Table 3.41: Overview of FLT1-targeted agents in cancer (Continued 3)
Table 3.42: Overview of FLT4-targeted agents in cancer
Table 3.43: Overview of FLT4-targeted agents in cancer (Continued 1)
Table 3.44: Overview of FLT4-targeted agents in cancer (Continued 2)
Table 3.45: Overview of KDR-targeted agents in cancer
Table 3.46: Overview of KDR-targeted agents in cancer (Continued 1)
Table 3.47: Overview of KDR-targeted agents in cancer (Continued 2)
Table 3.48: Overview of KDR-targeted agents in cancer (Continued 3)
Table 3.49: Overview of KDR-targeted agents in cancer (Continued 4)
Table 3.50: Overview of KDR-targeted agents in cancer (Continued 5)
Table 3.51: Overview of JAK2-Targeted Agents in Cancer
Table 3.52: Overview of JAK2-Targeted Agents in Cancer (continued)
Table 3.53: Overview of MET-Targeted Agents in Cancer (continued)
Table 3.54: Overview of MET-Targeted Agents in Cancer (continued)
Table 3.55: Overview of AKT1-Targeted Agents in Cancer (continued)
Table 3.56: Overview of AKT1-Targeted Agents in Cancer (continued)
Table 3.57: Overview of CDC2-Targeted Agents in Cancer
Table 3.58: Overview of CDK2-Targeted Agents in Cancer
Table 3.59: Overview of CDK2-Targeted Agents in Cancer (continued)
Table 3.60: Overview of AURKA-Targeted Agents in Cancer
Table 3.61: Overview of AURKA -Targeted Agents in Cancer (continued)
Table 3.62: Overview of AURKB -Targeted Agents in Cancer
Table 3.63: Overview of PLK1 -Targeted Agents in Cancer
Table 3.64: Overview of FRAP1 -Targeted Agents in Cancer
Table 3.65: Overview of FRAP1 -Targeted Agents in Cancer (Continued 1)
Table 3.66: Overview of FRAP1 -Targeted Agents in Cancer (Continued 2)
Table 3.67: Overview of PIK3CA -Targeted Agents in Cancer
Table 3.68: Overview of PIK3CA -Targeted Agents in Cancer (Continued)
Table 4.69: Kinase-Targeted Agents With Anti-Arthritic Applications
Table 4.70: Kinase-Targeted Agents With Anti-Arthritic Applications (continued 1)
Table 4.71: Kinase-Targeted Agents With Anti-Arthritic Applications (continued 2)
Table 4.72: Kinase-Targeted Agents With Anti-Arthritic Applications (continued 3)
Table 4.73: Kinase-Targeted Agents With Anti-Arthritic Applications (continued 4)
Table 4.74: Kinase-Targeted Agents With Anti-Arthritic Applications (continued 5)
Table 4.75: Kinase-Targeted Agents With Diabetes Applications
Table 4.76: Kinase-Targeted Agents With Diabetes Applications (continued 1)
Table 4.77: Kinase-Targeted Agents With Diabetes Applications (continued 2)
Table 4.78: Kinase-Targeted Agents With Inflammatory Applications
Table 4.79: Kinase-Targeted Agents With Inflammatory Applications (Continued 1)
Table 4.80: Kinase-Targeted Agents With Inflammatory Applications (Continued 2)
Table 4.81: Kinase-Targeted Agents With Immunosuppresive Applications
Table 4.82: Kinase-Targeted Agents With Immunosuppresive Applications (continued)
Table 4.83: Kinase-Targeted Agents With Ophthalmological Applications
Table 4.84: Kinase-Targeted Agents With Ophthalmological Applications (continued)
Table 4.85: Kinase-Targeted Agents With Psoriasis Applications (continued)
Table 4.86: Kinase-Targeted Agents With Psoriasis Applications (continued)
Table 4.87: Kinase-Targeted Agents With PulmonaryApplications (Launched)
Table 4.88: Kinase-Targeted Agents With PulmonaryApplications (Phase I-III)
Table 4.89: Kinase-Targeted Agents With PulmonaryApplications (Preclinical)
Table 4.90: Kinase-targeted agents with cardiovascular applications
Table 4.91: Kinase-targeted agents with cardiovascular applications (continued)
Table 4.92: Kinase-targeted agents with myelodysplastic disorder applications
Table 4.93: Kinase-targeted agents with myelodysplastic disorder applications (continued)
Table 4.94: Kinase-targeted agents with myelodysplastic disorder applications (continued 2)
Table 4.95: Kinase-targeted agents with myelodysplastic disorder applications (continued 3)
Table 4.96: Kinase-targeted agents with GI disorder applications
Table 4.97: Kinase-targeted agents with GI disorder applications
Table 5.98: Overview of Abbott's kinase pipeline by status
Table 5.99: Overview of Ambit Biosciences' Kinase Pipeline by Status
Table 5.100: Overview of Amgen's kinase pipeline by status
Table 5.101: Overview of Array BioPharma's kinase pipeline by status
Table 5.102: Overview of AstraZeneca’s kinase pipeline by status
Table 5.103: Overview of Avila Therapeutics' kinase pipeline by status
Table 5.104: Overview of Boehringer Ingelheim's kinase pipeline by status
Table 5.105: Overview of Bristol-Myers Squibb's (BMS) kinase pipeline by status
Table 5.106: Overview of Cephalon's kinase pipeline by status
Table 5.107: Overview of Deciphera Pharmaceuticals' kinase pipeline by status
Table 5.108: Overview of Eli Lilly’s kinase pipeline by status
Table 5.109: Overview of Eli Lilly’s kinase pipeline by status (continued)
Table 5.110: Overview of Exelixis’ kinase pipeline by status
Table 5.111: Overview of Exelixis’ kinase pipeline by status
Table 5.112: Overview of Hoffmann-La Roche's kinase pipeline by status
Table 5.113: Overview of Johnson & Johnson's kinase pipeline by status
Table 5.114: Overview of Kyowa Hakko Kirin's kinase pipeline by status
Table 5.115: Overview of Novartis’ kinase pipeline by status
Table 5.116: Overview of Novartis’ kinase pipeline by status (continued)
Table 5.117: Overview of Pfizer’s kinase pipeline by status
Table 5.118: Overview of Sanofi-Aventis' kinase pipeline by status
Table 5.119: Overview of Wyeth’s kinase pipeline by status
Table 6.120: World Prevalence Of Diseases
Table 6.121: World Pharma Market by Indication (US$m), 2008-2013
Table 6.122: World Pharma Market by Region (US$m), 2008-2013
Table 6.123: Kinase Drug Analysis (in 2007-2008) and Forecasts, 2009-2013 ($USm)
Table 6.124: Kinase Inhibitors by Geography ($USm), 2008 and 2013
Table 6.125: Manufacturer Analysis (2008) and Forecasts (US$m), 2009-2013
Table 6.126: Major Kinase Patent Indications
Table 6.127: Leading Kinase Patent Assignees

- Abbott Laboratories
- Ambit Biosciences Corp
- Amgen Inc
- Array BioPharma Inc
- AstraZeneca plc
- Avila Therapeutics Inc
- Boehringer Ingelheim GmbH
- Bristol-Myers Squibb Co
- Cephalon Inc
- Deciphera Pharmaceuticals LLC
- Eli Lilly Co
- Exelixis Inc
- GlaxoSmithKline plc
- Hoffmann-La Roche Ltd
- Johnson & Johnson
- Kyowa Hakko Kirin Co Ltd
- Novartis International AG
- Pfizer Inc
- Sanofi-Aventis Group
- Wyeth

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