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

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

  • Bioorg Med Chem Lett. 2012 Aug 1;22(15):4955-61. doi: 10.1016/j.bmcl.2012.06.038.
Gopi Kumar Mittapalli 1,  Fang Zhao,  Andrew Jackson,  Hongfeng Gao,  Haekyung Lee,  Stephine Chow,  Maninder Pal Kaur,  Natalie Nguyen,  Robert Zamboni,  Jeffrey McKelvy,  Flossie Wong-Staal,  James E Macdonald
Affiliations

Affiliation

  • 1 iTherX Pharmaceuticals, Inc., San Diego, CA 92191-0530, USA.
PMID: 22784640 DOI: 10.1016/j.bmcl.2012.06.038
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-116183
    Hepatitis C Virus Entry Inhibitor
    HCV