Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue

David A. Price; Heather Eng; Kathleen A. Farley; Gilles H. Goetz; Yong Huang; Zhaodong Jiao; Amit S. Kalgutkar; Natasha M. Kablaoui; Bhagyashree Khunte; Spiros Liras; Chris Limberakis; Alan M. Mathiowetz; Roger B. Ruggeri; Jun-Min Quan; Zhen Yang

doi:10.1039/C7OB00096K

Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue†

David A. Price,

*^a Heather Eng,^b Kathleen A. Farley,

^b Gilles H. Goetz,^b Yong Huang,^c Zhaodong Jiao,^c Amit S. Kalgutkar,^a Natasha M. Kablaoui,^a Bhagyashree Khunte,^b Spiros Liras,^a Chris Limberakis,^b Alan M. Mathiowetz,^a Roger B. Ruggeri,^b Jun-Min Quan^c and Zhen Yang^c

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* Corresponding authors

^a Pfizer Inc. Medicine Design, 610 Main Street, Cambridge, Massachusetts, 02155 USA
E-mail: david.a.price@pfizer.com

^b Pfizer Inc. Medicine Design, 224 Eastern Point Road, Groton, Connecticut, 06340 USA

^c Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen, China

Abstract

The synthesis and in vivo pharmacokinetic profile of an analogue of cyclosporine is disclosed. An acyclic congener was also profiled in in vitro assays to compare cell permeability. The compounds possess similar calculated and measured molecular descriptors however have different behaviors in an RRCK assay to assess cell permeability.

This article is part of the themed collection: Macrocycles with bio-related applications

Organic & Biomolecular Chemistry

Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue†

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Comparative pharmacokinetic profile of cyclosporine (CsA) with a decapeptide and a linear analogue

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