2. Academic Validation
  3. Discovery of ravidasvir (PPI-668) as a potent pan-genotypic HCV NS5A inhibitor

Discovery of ravidasvir (PPI-668) as a potent pan-genotypic HCV NS5A inhibitor

  • Bioorg Med Chem Lett. 2016 Sep 15;26(18):4508-4512. doi: 10.1016/j.bmcl.2016.07.066.
Min Zhong 1,  Eric Peng 2,  Ningwu Huang 2,  Qi Huang 2,  Anja Huq 2,  Meiyen Lau 2,  Richard Colonno 2,  Leping Li 3
Affiliations

Affiliations

  • 1 Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA. Electronic address: mzhong@myokardia.com.
  • 2 Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA.
  • 3 Presidio Pharmaceuticals, Inc., 1700 Owens Street, Suite 585, San Francisco, CA 94158, USA. Electronic address: leping@assemblybio.com.
PMID: 27506559 DOI: 10.1016/j.bmcl.2016.07.066
Abstract

This Letter describes the synthesis, representative structure activity relationship (SAR), activity and PK profiles of a series of functionalized benzimidazole-naphthylene-imidazole derivatives as HCV NS5A inhibitors. This effort successfully led to the discovery of ravidasvir (PPI-668), which has been well tolerated and shown high sustained viral response rates as a key component in all-oral combination regimens in multiple human clinical trials.

Keywords

Benzimidazole–naphthylene–imidazole derivatives; Hepatitis C virus; NS5A inhibitor; PPI-668; Ravidasvir.

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