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マクロサイクル:創薬・開発・技術‐概要

Macrocycles: Discovery, Development & Technologies

発行 Insight Pharma Reports 商品コード 282138
出版日 ページ情報 英文 111 Pages
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マクロサイクル:創薬・開発・技術‐概要 Macrocycles: Discovery, Development & Technologies
出版日: 2013年09月13日 ページ情報: 英文 111 Pages
概要

当レポートでは、創薬におけるマクロサイクルについて調査し、各企業における薬剤候補としてのマクロサイクル研究戦略の分析を提供しており、企業概要、技術プラットフォーム、メリット、課題、競争上の優位性、提携・将来の期待および独占インタビューなどを、概略下記の構成で取り上げております。

エグゼクティブサマリー

第1章 マクロサイクルとは何か?

第2章 薬物速度論的特性はどれほど重要か?

  • 吸収
  • 配分
  • 代謝
  • 排出
  • 薬物速度論的要件への到達における課題

第3章 Bicycle Therapeutics

  • 企業背景
  • 環化化学プラットフォーム
  • 環化化学プラットフォームのメリット
  • 課題・改善領域
  • Rolf Guenther氏、Christophe Bonny氏へのインタビュー

第4章 Encycle Therapeutics

  • 企業背景
  • 化学技術プラットフォーム
  • 提携、競争上の優位性、および将来の展望
  • Jeffery Coull氏へのインタビュー

第5章 Ensemble therapeutics

  • 企業背景
  • DNAプログラム化学プラットフォーム
  • 競争上の優位性
  • 提携および将来の成長
  • Nick Terrett氏へのインタビュー

第6章 Lanthio Pharma

  • 企業背景
  • 乳酸連鎖球菌プラットフォーム
  • 乳酸連鎖球菌プラットフォームのメリット
  • 直面する課題
  • 競争上の優位性
  • 提携および将来の成長
  • Gert Moll 氏へのインタビュー

第7章 Oncodesign Biotechnology

  • 企業背景
  • 開発プラットフォーム
  • ナノサイクル(Nanocyclix)プラットフォーム
  • ナノサイクルプラットフォームのメリット
  • 直面する課題
  • 競争上の優位性
  • 提携および将来の成長
  • Jan Hoflack氏へのインタビュー

第8章 Pepscan Therapeutics

  • 企業背景
  • 化学的に結合したペプチド足場(CLIPS)プラットフォーム
  • CLIPSプラットフォームのメリット
  • CLIPSプラットフォームの課題
  • 競争上の優位性
  • 提携および将来の成長
  • Peter Timmerman氏へのインタビュー

第9章 PeptiDream Incorporation

  • 企業背景
  • ペプチド創薬開発プラットフォームシステム(PDPS)
  • PDPS・マクロサイリック作成の課題
  • 競争上の優位性、提携、および将来の期待
  • Patrick Reid氏へのインタビュー

第10章 Ra Pharmaceuticals

  • 企業背景
  • 翻訳プラットフォームおよびマクロサイクリック作成
  • 直面する課題
  • 競争上の優位性、提携、および将来の期待
  • Doug Treco 氏へのインタビュー

第11章 Tranzyme Pharmaceuticals

  • 企業背景
  • マクロサイクリックテンプレートケミストリー(MATCH)プラットフォーム
  • MATCHプラットフォームのメリット・競争上の優位性
  • 提携および将来の期待
  • Mark L. Peterson 氏へのインタビュー

第12章 Aileron Therapeutics

  • 企業背景
  • ステープルドペプチドプラットフォーム
  • 競争上の優位性
  • 改良分野
  • 提携および将来の期待
  • Vincent Guerlavais 氏へのインタビュー

第13章 何故マクロサイクルか?

  • 従来の小分子に対してマクロサイクルはどのような改善を示すか?
  • 治療アプリケーション
  • 直面する課題
  • マクロサイクル研究者

参考資料

Cambridge Healthtech Institute について

図表

目次

Available September 2013!

New to Insight Pharma Reports is Macrocycles: Discovery, Development & Technologies.

Macrocycles are a drug class consisting of small to medium sized natural, semi-natural, or artificial molecules where atoms are connected in such a way that they form a ring, providing rigidity and stability to the structure. Traditionally, macrocycles are cyclic compounds or peptides that vary in size, and are typically 500-2,000 Da. With such a variety in size, the bigger the molecule the more flexibility in structural combinations, allowing scientists to fine-tune the molecules' function and performance. Macrocycles are unique compounds in that larger molecules still maintain structural organization and stability, whereas linear molecules can usually adopt several different combinations; providing the necessary structural foundation for scientists to work with and apply to various areas of drug development, creating a footprint for a wide line of therapeutics.

This report covers background material including a more in depth analysis of what macrocycles are and the pharmacokinetic properties (absorption, distribution, metabolism, and excretion) they exhibit. Challenges, benefits, and additional properties that are considered with their development as drugs are covered as well. Additionally, this report details specifics in technologies and current research in development. Chapters 3-12 detail various companies and their strategies for studying macrocycles as drug candidates and Insight Pharma Reports has received the participation of:

  • Bicycle Therapeutics
  • Encycle Therapeutics
  • Ensemble Therapeutics
  • Lanthio Pharma
  • Oncodesign
  • Pepscan
  • PeptiDream
  • RA Pharmaceuticals
  • Tranzyme Pharmaceuticals
  • Aileron Therapeutics

Specific highlights covered in each section include detailed descriptions of company overviews, technology platforms, benefits, challenges, competitive advantages, partnerships and future aspirations. Also provided are exclusive interviews at the end of each section.

Also exclusive to this report is a survey conducted by Insight Pharma Reports. This survey includes over 90 participants from the various organizations including academic and government institutions, pharmaceutical companies, and biotechnology companies. These results are mentioned and analyzed at the end of the report.

Table of Contents

Executive Summary

Chapter 1: What are macrocycles?

Chapter 2: How Important are Pharmacokinetic Properties?

  • 2.1 Absorption
  • 2.2 Distribution
  • 2.3 Metabolism
  • 2.4 Excretion
  • 2.5 Challenges in reaching pharmacokinetic requirements
    • 2.5.1 Plasma concentrations
    • 2.5.2 Drug-drug interactions
    • 2.5.3 Drug dose administration
    • 2.5.4 Drug absorption design
      • 2.5.4.1 Cell permeability
      • 2.5.4.2 Oral bioavailability

Chapter 3: Bicycle Therapeutics

  • 3.1 Company Background
  • 3.2 Cyclization chemistry platform
  • 3.3 Benefits to the cyclization chemistry platform
  • 3.4 Challenges and areas of improvement
  • 3.5 Interview with Rolf Guenther and Christophe Bonny
    • 3.6.1 Company background
    • 3.6.2 Cyclization chemistry platform
    • 3.6.3 Macrocyclic properties
    • 3.6.4 Partnerships and future aspirations

Chapter 4: Encycle Therapeutics

  • 4.1 Company background
  • 4.2 Chemical technology platform
  • 4.3 Partnerships, competitive advantage, and future outlook
  • 4.4 Interview with Jeffery Coull
    • 4.4.1 Company background
    • 4.4.2 Chemical technology platform
    • 4.4.3 Tracking and properties of macrocycles
    • 4.4.4 Partnerships and future aspirations

Chapter 5: Ensemble therapeutics

  • 5.1 Company background
  • 5.2 DNA-programmed chemistry platform
    • 5.2.1 Benefits to DNA-programmed chemistry platform
    • 5.2.2 Challenges to DNA-programmed chemistry platform
  • 5.3 Competitive advantage
  • 5.4 Partnerships and future growth
  • 5.5 Interview with Nick Terrett
    • 5.5.1 Company background
    • 5.5.2 Macrocycle background and goals
    • 5.5.3 Macrocyclic creations and properties
    • 5.5.4 DNA-programmed chemistry platform
    • 5.5.5 Macrocyclic structures and expected interactions
    • 5.5.6 Challenges and properties in macrocyclic development
    • 5.5.7 Partnerships and future aspirations

Chapter 6: Lanthio Pharma

  • 6.1 Company background
  • 6.2 Lactococcus lactics platform
  • 6.3 Benefits to Lactococcus lactis platform
  • 6.4 Challenges encountered
  • 6.5 Competitive advantage
  • 6.6 Partnerships and future growth
  • 6.7 Interview with Gert Moll
    • 6.7.1 Company background
    • 6.7.2 Lactococcus lactis platform
    • 6.7.3 Macrocyclic properties
    • 6.7.4 Challenges encountered
    • 6.7.5 Competitive advantage
    • 6.7.6 Partnerships and future aspirations

Chapter 7: Oncodesign Biotechnology

  • 7.1 Company Background
  • 7.2 Platforms developed
  • 7.3 Nanocyclix platform
  • 7.4 Benefits of Nanocyclix platform
  • 7.5 Challenges encountered
  • 7.6 Competitive advantage
  • 7.7 Partnerships and future growth
  • 7.8 Interview with Jan Hoflack
    • 7.7.1 Company background
    • 7.7.2 Nanocyclix platform
    • 7.7.3 Nanocyclix properties
    • 7.7.4 Partnerships and future aspirations

Chapter 8: Pepscan Therapeutics

  • 8.1 Company background
  • 8.2 Chemical linkage of peptides onto scaffolds (CLIPS) platform
  • 8.3 Benefits of the CLIPS platform
  • 8.4 Challenges of the CLIPS platform
  • 8.5 Competitive advantage
  • 8.6 Partnerships and future aspirations
  • 8.7 Interview with Peter Timmerman
    • 8.7.1 Company background
    • 8.7.2 CLIPS platform
    • 8.7.3 Macrocyclic properties
    • 8.7.4 Partnerships and future aspirations

Chapter 9: PeptiDream Incorporation

  • 9.1 Company background
  • 9.2 Peptide discovery platform system (PDPS)
  • 9.3 Challenges to PDPS and macrocyclic creations
  • 9.4 Competitive advantage, partnerships, and future aspirations
  • 9.5 Interview with Patrick Reid
    • 9.5.1 Company background
    • 9.5.2 PDPS platform
    • 9.5.3 Macrocyclic properties
    • 9.5.4 Challenges encountered
    • 9.5.5 Competitive advantage
    • 9.5.6 Partnerships and future aspirations

Chapter 10: Ra Pharmaceuticals

  • 10.1 Company background
  • 10.2 Translation platform and macrocyclic creations
  • 10.3 Challenges encountered
  • 10.4 Competitive advantage, partnerships, and future aspirations
  • 10.5 Interview with Doug Treco
    • 10.5.1 Company background
    • 10.5.2 In vitro translation platform
    • 10.5.3 Macrocycle tracking, creations, and properties
    • 10.5.4 Challenges encountered
    • 10.5.5 Partnerships and future aspirations

Chapter 11: Tranzyme Pharmaceuticals

  • 11.1 Company background
  • 11.2 Macrocyclic template chemistry (MATCH) platform
  • 11.3 Benefits and competitive advantages to MATCH platform
  • 11.4 Areas of improvement to the MATCH platform
  • 11.5 Partnerships and future aspirations
  • 11.6 Interview with Mark L. Peterson
    • 11.6.1 Company background
    • 11.6.2 Macrocyclic properties
    • 11.6.3 MATCH platform
    • 11.6.4 Parthersnips and future aspirations

Chapter 12: Aileron Therapeutics

  • 12.1 Company background
  • 12.2 Stapled Peptide platform
  • 12.3 Competitive advantage
  • 12.4 Areas of improvement
  • 12.5 Partnerships and future aspirations
  • 12.6 Interview with Vincent Guerlavais
    • 12.6.1 Company background
    • 12.6.2 Stapled Peptide platform
    • 12.6.3 Macrocyclic creations and properties
    • 12.6.4 Competitive advantage

Chapter 13: Why Macrocycles?

  • 13.1 What improvements do macrocycles exhibit over conventional small molecules?
    • 13.1.1 Structural modifications
    • 13.1.2 Structural stability
    • 13.1.3 Cell permeability, molecular activity, and half-life
    • 13.1.4 Protein-protein interactions
    • 13.1.5 Higher binding affinity
    • 13.1.6 Improved binding modes
  • 13.2 Therapeutic applications
  • 13.3 Challenges encountered
  • 13.4 Who's working with macrocycles?

References

About Cambridge Healthtech Institute

Figures:

  • Figure 1.1: Example of Macrocycles
  • Figure 3.1: Different Peptide Structures with the same Amino Acid Sequence
  • Figure 4.1: Multicomponent Ugi Reaction Yields a Pentapeptide Constrained in a Macrocycle
  • Figure 5.1: Hybridization of DNA Synthesizes Macrocycle Compounds
  • Figure 6.1: Methyl-Lanthionine-Containing Peptides
  • Figure 6.2: Lanthipeptide Library on Lactococcus lactis Cell Surface
  • Figure 8.1: Linear Peptide vs. CLIPS-Peptide
  • Figure 13.1: Organizations Surveyed
  • Figure 13.2: Time Spent Studying Macrocycles
  • Figure 13.3: Areas of Study
  • Figure 13.4: Problems Encountered
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