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Discovery of ITX 4520: a highly potent orally bioavailable hepatitis C virus entry inhibitor.

Abstract：

:The manuscript reports an identification of a highly potent, orally bioavailable hepatitis C virus entry inhibitor through optimization of a previously reported class of molecules (1) that were not stable in the rat plasma. Compound 39 (ITX 4520) exhibited an excellent PK profile in both rats and dogs with good oral exposure, half-life and oral bioavailability. The compound is also well-tolerated in the preliminary in vivo toxicity studies and has been selected as a pre-clinical candidate for our HCV clinical pipeline.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Mittapalli GK,Zhao F,Jackson A,Gao H,Lee H,Chow S,Kaur MP,Nguyen N,Zamboni R,McKelvy J,Wong-Staal F,Macdonald JE

doi

10.1016/j.bmcl.2012.06.038

subject

Has Abstract

pub_date

2012-08-01 00:00:00

pages

4955-61

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00789-5

journal_volume

22

pub_type

杂志文章

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