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市場調查報告書
R&D最新情報：既有的血管生成抑制劑改良
R&D Update: How Can Companies Improve on Existing Antiangiogenesis Agents?
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本報告已在2011年12月21日停止出版。
抗血管生成藥在抗腫瘤療法的新藥物類群中與細胞毒性藥、標的治療藥、免疫調整劑併用於癌症治療上，由Genentech公司研發出的首度抗血管生成藥Avastin是創造全球性頂尖銷售成績的抗癌藥劑之一。
本報告書內容包括：腫瘤的血管生成、市售的血管生成抑制劑、新的血管生成抑制劑、血管生成抑制劑改良策略等分析。內容綱要摘記如下：
第1章 實施概要
第2章 介紹
第3章 腫瘤的血管生成生態學
- VEGF路徑
- Integrin訊息傳導
- PDGFR
- 細胞缺氧症
第4章 針對癌症治療的經認可的血管生成抑制劑
- Genentech的Avastin
- Bayer的Nexavar
- Pfizer的Sutent
第5章 針對癌症治療的新的血管生成抑制劑
- 新的小分子抗血管生成薬
- Celgene的沙利竇邁(Thalidomide)衍生物
- Merck的Cilengitide
- GlaxoSmithKline的Pazopanib
- AstraZeneca的Zactima
- AstraZeneca的Cediranib
- 新的巨大分子抗血管生成藥
- Regeneron/Sanofi-Aventis的Aflibercept
- PLD BioPharma/Biogen Idec的Volociximab
- UCB/IｍClone的CDP-791
- Amgen的AMG-386
- 血管生成抑制劑的改良
第6章 展望
Abstract
Introduction
Antiangiogenic drugs represent a new class of antitumor therapeutics that will
be used along with cytotoxic agents, targeted agents, and immunomodulatory
agents to fi ght cancer. The fi rst antiangiogenic compound on the market,
Genentech' s Avastin (bevacizumab), has become one of the top-selling
anticancer drugs worldwide. In November 2007, another antiangiogenic agent,
Onyx/Bayer' s Nexavar, became the fi rst agent approved to treat hepatocellular
carcinoma. Based on Avastin' s success, pharmaceutical and biotechnology
companies are developing a rich pipeline of antiangiogenic agents, including
multitargeted kinase inhibitors, other smallmolecule compounds, and
large-molecule biological agents.
Get the Answers You Need to Shape Your Strategy
- The vascular endothelial growth factor (VEGF) pathway is the most well
understood of the angiogenic pathways and all approved antiangiogenic
drugs--Avastin, Onyx/Bayer' s Nexavar (sorafenib), and Pfi zer' s Sutent
(sunitinib)- primarily target this pathway and its receptors. What other
pathways are associated with angiogenesis? What are the disadvantages of
targeting the VEGF pathway? What pathways do emerging antiangiogenic drugs
target?
- Current antiangiogenic agents offer only limited benefi t to patients in
terms of improved survival and quality of life. How have emerging
antiangiogenic compounds fared in clinical trials? What strategies are drug
developers exploring to improve the effi cacy of antiangiogenic drugs?
- Resistance to anti-VEGF agents remains a challenge to the long-term effi
cacy of existing anti-angiogenic agents. What approaches are pharmaceutical
companies taking to address VEGF resistance? Does the targeting of HIF
(hypoxia-inducible factor) or mTOR (mammalian target of rapamycin) represent a
viable strategy to overcoming VEGF resistance?
Scope
- Tumor angiogenesis: the systems that contribute to its growth and
those that inhibit its growth.
- Marketed antiangiogenic agents: Genentech' s Avastin (bevacizumab),
Onyx/Bayer' s Nexavar (sorafenib), and Pfi zer' s Sutent (sunitinib).
- Emerging antiangiogenic agents: Adnexus' s Angiocept, Amgen' s
AMG-386, AstraZeneca' s cediranib, AstraZeneca' s Zactima, Celgene' s thalidomide
derivatives, GlaxoSmithKline' s pazopanib, MedImmune' s abegrin, Merck KGaA' s
cilengitide, Novartis' s vatalanib, PDL BioPharma/Biogen Idec' s volociximab,
Pfi zer' s axitinib, Regeneron/Sanofi -Aventis' s afl ibercept, UCB/ImClone' s
CDP-791.
- Strategies to improve antiangiogenic agents: maximizing the effi
cacy of antiangiogenic compounds and preventing development of resistance to
the compounds.
Table of Contents
- Executive Summary
- Strategic Implications
- Stakeholder Implications
- Introduction
- Biology of Tumor Angiogenesis
- VEGF Pathway
- Integrin Signaling
- PDGFR
- Cell Hypoxia
- Antiangiogenic Agents Approved to Treat Cancer
- Genentech' s Avastin
- Bayer' s Nexavar
- Pfizer' s Sutent
- Emerging Antiangiogenesis Agents to Treat Cancer
- Emerging Small-Molecule Antiangiogenic Drugs
- Celgene' s Thalidomide Derivatives
- Merck' s Cilengitide
- GlaxoSmithKline' s Pazopanib
- AstraZeneca' s Zactima
- AstraZeneca' s Cediranib
- Emerging Large-Molecule Antiangiogenic Drugs
- Regeneron/Sanofi -Aventis' s Afl ibercept
- PDL BioPharma/Biogen Idec' s Volociximab
- UCB/ImClone' s CDP-791
- Amgen' s AMG-386
- Improving on Antiangiogenesis Agents
- Improving the Effi cacy of Antitumor Agents
- Preventing Resistance to Antiangiogenic Drugs
- Outlook
Tables:
- 1. Major Angiogenic Growth Factors
- 2. Key Angiogenesis Inhibitors
- 3. Antiangiogenic Agents Approved for the Treatment of Cancer
- 4. Emerging Small-Molecule Antiangiogenic Agents
- 5. Emerging Large-Molecule Antiangiogenic Agents
Figures:
- 1. The Angiogenic Process
- 2. The Role of mTor in the Regulation of HIF-1�� and Angiogenesis
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