Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance

Author:

Rand Arthur C.123,Leung Siegfried S. F.4563,Eng Heather7893,Rotter Charles J.7893,Sharma Raman7893,Kalgutkar Amit S.7893,Zhang Yizhong7893,Varma Manthena V.7893,Farley Kathleen A.10893,Khunte Bhagyashree10893,Limberakis Chris10893,Price David A.108113,Liras Spiros108113,Mathiowetz Alan M.108113,Jacobson Matthew P.4563,Lokey R. Scott123

Affiliation:

1. Department of Chemistry

2. University of California Santa Cruz

3. USA

4. Department of Pharmaceutical Chemistry

5. University of California San Francisco

6. San Francisco

7. Pharmacokinetics and Drug Metabolism

8. Pfizer Inc

9. Groton

10. Worldwide Medicinal Chemistry

11. Cambridge

Abstract

The impact of side chain functionality on the pharmacokinetics of an orally bioavailable cyclic peptide scaffold is investigated.

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

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