PI3k/Akt/mTOR途徑:開發平台分析

PI3k/Akt/mTOR途徑:開發平台分析 是由出版商Insight Pharma Reports在2011年11月所出版的。 這份英文市場調查報告書價格從美金2495起跳。

簡介

PI3k/Akt/mTOR訊號傳遞對大多的生理學，病理生理學發揮作用，成為在各種各樣的癌症治療中重要的因素。

本報告提供PI3k，Akt，mTOR抑制劑及多蛋白激酶抑制劑的開發情形調查分析，各種的治療性介入和治療策略，PI3k，Akt，mTOR的各抑制劑，雙重抑制劑的開發情形，再加上主要企業的配合措施，專家的採訪等彙整資料，為您概述為以下內容。

第1章 簡介

• PI3k/mTOR/Akt訊號傳遞
• 活性化和主要蛋白激酶
• 內容組織

第2章 治療性介入

• PI3K
  • 複數的異構體
  • 已知的基因突變
• Akt
  • 蛋白激酶
  • 已知的基因突變
• mTOR
  • mTORC1·mTORC2
  • 已知的基因突變
• PDK1·p70S6k
• 治療策略
  • 單一的蛋白激酶的阻礙
  • 複數的蛋白激酶的阻礙
  • 替代調製

第3章 PI3k/AKT連鎖和疾病

• 癌症
• 發炎
• 其他的適應症
• 目前治療可供選擇

第4章 PI3k抑制劑

• 開發發展階段的PI3k抑制劑
  • PX-866
  • BKM-120
  • XL-147 (SAR-245408)
  • GS-1101
  • Pan-active PI3k抑制劑
• 異構體選擇性抑制劑
  • PI3Kd
  • PI3Ka
• 摘要

第5章 AKT抑制劑

• Akt結構
• 臨床開發階段的Akt·S6k抑制劑
  • GSK-2110183·GSK-2141795
  • RX-0201
  • MK-2206
  • Perifosine
• 摘要

第6章 mTOR抑制劑

• mTOR·TORC1·TORC2
• Rapalogs
  • 認證化合物
  • 正在開發的化合物
• 蛋白激酶抑制劑
• Ridaforolimus
• OSI-027
• AZD-8055
• 摘要

第7章 雙重抑制劑

• 開發階段的雙重抑制劑
  • 前臨床階段的化合物
• 階段I的化合物
  • GDC-0980
  • GSK-2126458
  • SF-1126
• 階段II的化合物
  • BEZ-235
  • XL-765 (SAR-245409)
• 摘要

第8章 主要企業

第9章 目前預測

第10章 PI3k/AKT/mTOR連鎖:專家的採訪

詢問調查的內容

企業目錄

圖表

目錄

This report includes:

• Pipeline reviews of PI3K, Akt, mTOR, and dual kinase inhibitors in development and an assessment of the current prospects for each approach
• Role of the PI3K/Akt/mTOR cascade in various diseases and potential intervention strategies
• Survey results offering unique insights into industry sentiment concerning development of inhibitors of this pathway
• Profiles of selected companies that are targeting components of the PI3K signaling cascade, highlighting their distinct strategies
• Significant licensing deals and acquisitions related to targeting the PI3K cascade
• An overall assessment of progress in developing agents to modulate the PI3K/Akt/mTOR cascade and commercial prospects
• Selected expert interviews on modulating the PI3K/Akt/mTOR cascade

In recent years it has become apparent that the activation of phosphatidylinositol 3-kinases (PI3Ks) initiates a complex sequence of intracellular events that include the activation of a number of other kinases, with Akt and mammalian target of rapamycin kinase (mTOR) both playing pivotal roles. The evidence for this PI3K cascade being heavily implicated in many types of cancer is very strong, with significant evidence for it also being important in other conditions, notably inflammatory diseases. This has led to extensive interest in the development of novel modulators of the activity of this cascade, primarily for the treatment of cancer.

The complexity of this cascade and the multiplicity of potential intervention points have prompted the structuring of The PI3K/Akt/mTOR Pathway: A Pipeline Analysis report to focus upon each of the main targets of this cascade in turn. The major components of the cascade are described in more detail before outlining potential intervention strategies. The evidence for the role of this cascade in various diseases is then considered, highlighting the limited scope for modulating it with currently approved therapies. The report considers inhibition of PI3K, Akt, mTOR, and dual kinases, highlighting the inhibitors that are in development and assessing the current prospects for each approach.

The interest in therapeutically exploiting the PI3K cascade has seen a number of companies emerge that focus either exclusively or significantly on targeting one or more of the components in this cascade. Their successes in identifying promising inhibitors have also seen a number of high-value deals, both co-development agreements and acquisitions, demonstrating the perceived value of the targets that such companies are pursuing. Specialist key players are profiled, highlighting their distinct strategies, and also the considerable interest seen in deal-making in this area.

Finally, we consider the prospects of commercial success for agents that modulate the PI3K/Akt/mTOR cascade. As more detailed clinical data become available, it can be expected that the level of interest in this cascade, and expectations of what can be achieved by its modulation, will be increased.

Peter Norman, MBA, PhD, is a pharmaceutical consultant and analyst based in Burnham Beeches, near Windsor, England, with specialist knowledge of the respiratory disease and inflammation markets.

Insight Pharma Reports are written by experts in consulting and industry who collaborate with us to provide a series of reports that evaluate the salient issues in pharmaceutical technology, business, and therapy markets. Insight Pharma Reports are used by leading pharmaceutical, biotech, diagnostic, consulting, and financial companies to keep abreast of the latest advances in pharmaceutical R&D, their potential applications and business impacts, and their current and future position in the marketplace.

Table of Contents

INTRODUCTION

• 1.1. The PI3K/mTOR/Akt Signaling Cascade
• 1.2. Activation and Key Kinases
• 1.3. Report Structure

THERAPEUTIC INTERVENTION

• 2.1. PI3K
  • Multiple Isoforms
  • Known Mutations
• 2.2. Akt
  • The Kinase
  • Known Mutations
• 2.3. mTOR
  • mTORC1 and mTORC2
  • Known Mutations
• 2.4. PDK1 and p70S6k
• 2.5. Therapeutic Strategies
  • Monokinase Inhibition
  • Dual Kinase Inhibition
  • Alternative Modulation

THE PI3K/AKT CASCADE AND DISEASE

• 3.1. Cancer
• 3.2. Inflammation
• 3.3. Other Indications
• 3.4. Current Treatment Options

PI3K INHIBITORS

• 4.1. PI3K Inhibitors in Advanced Development
  • PX-866
  • BKM-120
  • XL-147 (SAR-245408)
  • GS-1101
  • Pan-active PI3K Inhibitors
• 4.2. Isoform-Selective Inhibitors
  • PI3Kd
  • PI3Ka
  • Other Specificities
• 4.3. Summary

AKT INHIBITORS

• 5.1. Akt Structure
• 5.2. Akt and S6k Inhibitors in Clinical Development
  • GSK-2110183 and GSK-2141795
  • RX-0201
  • MK-2206
  • Perifosine
• 5.3. Summary

mTOR INHIBITORS

• 6.1. mTOR, TORC1, and TORC2
• 6.2. Rapalogs
  • Approved Compounds
  • Development Compounds
• 6.3. Kinase Inhibitors
• 6.4. Ridaforolimus
• 6.5. OSI-027
• 6.6. AZD-8055
• 6.7. Summary

DUAL INHIBITORS

• 7.1. Dual Inhibitors in Development
  • Preclinical Compounds
• 7.2. Phase I Compounds
  • GDC-0980
  • GSK-2126458
  • SF-1126
• 7.3. Phase II Compounds
  • BEZ-235
  • XL-765 (SAR-245409)
• 7.4. Summary

KEY PLAYERS

• Aquinox Pharmaceuticals
• Arno Therapeutics
• Cellzome
• Emiliem
• Exelixis
• Intellikine
• Karus Therapeutics
• Oncothyreon
• Paloma Pharmaceuticals
• Pathway Therapeutics
• S*Bio
• Semafore Pharmaceuticals
• Xcovery
• Significant Acquisitions and Deals
• Astellas (OSI)
• Roche (Piramed)
• Gilead (Calistoga Pharmaceuticals)
• ARIAD and Merck

CURRENT OUTLOOK

• Development Status of Inhibitors Targeting the PI3K Cascade Commercial Prospects

PI3K/AKT/mTOR CASCADE: EXPERT INTERVIEWS

• Joseph R. Garlich, PhD, Co-Founder, Chief Scientific Officer, and Director, Semafore Pharmaceuticals, Westfield, IN
• Christian Rommel, PhD, Chief Scientific Officer, Intellikine, La Jolla, CA
• David Sherris, PhD, President and CEO, Paloma Pharmaceuticals, Jamaica Plain, MA
• Prof. Steve Ward, Head of Pharmacology, Department of Pharmacy and Pharmacology, University of Bath, United Kingdom

References

Appendix A

• RESULTS FROM INSIGHT PHARMA REPORTS' “PI3K CASCADE” SURVEY

SURVEY QUESTIONS

• A1. How attractive a target would you rate this cascade compared to a) other exploited options, and b) other options under investigation?
• A2. Compared to other protein kinase targets, how tractable do you rate each of these three kinases?
• A3. The PI3K cascade offers multiple target options. For the treatment of cancer, which of these options do you feel offers greater promise?
• A4. Isoform-selective PI3K inhibitors are an option for certain indications. On a scale of 0 (low) to 4 (high), please indicate how you perceive the attractiveness of each of the following options.
• A5. With respect to clinical utility, do you see inhibitors of the PI3K cascade being positioned as monotherapy (for treating cancer) or in combination with other agents?
• A6. Do you view the use of inhibitors of the PI3K cascade in combination with MEK inhibitors as the best option for combination therapy?
• A7. On a scale of 0 (low) to 4 (high), please rate how you see the (potential) clinical usefulness of modulators of the PI3K cascade in targeting each of the following indications.

Appendix B

• ACRONYMS

Company Index

• Table 4.1. Pan-active PI3K Inhibitors in Development
• Table 4.2. Isoform-Selective PI3K Inhibitors in Development
• Table 5.1. Akt Inhibitors in Development
• Table 5.2. Phase II Study Program for MK-2206
• Table 6.1. Rapalogs Approved for Clinical Use
• Table 6.2. Rapalogs in Development
• Table 6.3. mTOR Kinase Inhibitors in Development
• Table 7.1. Dual Kinase Inhibitors in Development
• Table 8.1. Exelixis' PI3K Cascade Inhibitor Pipeline
• Table 8.2. Intellikine's PI3K Cascade Inhibitor Pipeline
• Table 8.3. Pathway Therapeutics' PI3K Cascade Inhibitor Pipeline
• Table 8.4. Xcovery's PI3K Cascade Inhibitor Pipeline

• Figure 1.1. Outline of PI3K Cascade
• Figure 2.1. Components of the mTORC1 and mTORC2 Complexes
• Figure 2.2. Potential Intervention Points in the PI3K Cascade
• Figure 5.1. Schematic Representation of Akt Kinases
• Figure 7.1. The Impact of Dual PI3K/mTOR Inhibitors
• Figure 7.2. Selectivity Profiles of Dual PI3K/mTOR Inhibitors
• Figure 8.1. Target Strategies of Profiled Companies
• Figure 9.1. Development Status of Different Classes of Kinase Inhibitors Targeting the PI3K Cascade

相關商品

藥物開發相關市場調查報告書

分析工具：癌症治療的蛋白激脢抗化劑
Analytical Tool - Protein Kinase Inhibitors in Oncology
價格 : US $ 6674
出版日期 : 2012年05月

乳癌，肺癌，Protein Kinase抗化劑:藥物開發策略分析
Triple Analysis: Breast Cancer, Lung Cancer and Protein Kinase Inhibitors
價格 : US $ 5175
出版日期 : 2012年05月

白血病，肺癌，Protein Kinase抗化劑:藥物開發策略分析
Triple Analysis: Leukemia, Lung Cancer and Protein Kinase Inhibitors
價格 : US $ 5175
出版日期 : 2012年05月

Insight Pharma Reports發行的製藥相關市場調查報告書

後備化合物策略:商業的·策略的考察

Backup Compound Strategies: Commercial and Tactical Considerations

價格 : US $ 2495

出版日期 : 2012年04月

基於片段的藥物研發(FBDD):技術·用途·開發平台

Fragment-Based Drug Discovery: Technologies, Applications, and Pipelines

價格 : US $ 795

出版日期 : 2012年04月

血癌治療藥:開發平台·市場·商務相關考察

Hematological Cancer Therapies: Pipelines, Markets, and Business Considerations - Overview

價格 : US $ 2495

出版日期 : 2012年02月

Email Alert(Email 通知) - 最新市場調查報告書

GII 將每天定期更新最新市場調查報書資訊，選擇您有興趣的市場分類，我們將用Email的方式讓您收到最新訊息!