Date Published 
September 2013

Page Count
97

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Macrocycles: Discovery, Development & Technologies - 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