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

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

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

Affiliation

Price DA; Pfizer Inc. Medicine Design, 610 Main Street, Cambridge, Massachusetts, 02155 USA. david.a.price@pfizer.com.

Org Biomol Chem ; 15(12): 2501-2506, 2017 Mar 28.

Article in En | MEDLINE | ID: mdl-28266673

ABSTRACT

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.

Subject(s)

Cyclosporine/pharmacokinetics; Oligopeptides/pharmacokinetics; Animals; Cyclosporine/administration & dosage; Cyclosporine/chemistry; Male; Molecular Conformation; Oligopeptides/administration & dosage; Oligopeptides/chemistry; Rats; Rats, Wistar; Stereoisomerism

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Oligopeptides / Cyclosporine Limits: Animals Language: En Journal: Org Biomol Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2017 Document type: Article

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