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Curr Opin Pharmacol. 2016 Oct;30:84-92. doi: 10.1016/j.coph.2016.07.015. Epub 2016 Aug 23.

Hepatitis C virus NS3/4a protease inhibitors.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, WP14-2, West Point, PA 19486, USA. Electronic address: john_mccauley@merck.com.
2
Department of Medicinal Chemistry, Merck Research Laboratories, WP14-2, West Point, PA 19486, USA.

Abstract

Hepatitis C virus (HCV) infection is a major health issue around the world and HCV NS3/4a protease inhibitors have been the focus of intensive research for the past 20 years. From the first identification of substrate-derived peptide inhibitors to the complex, macrocyclic compounds, including paritaprevir and grazoprevir, that are currently available, the field has used structure-based design to confront the issues of potency, resistance and pharmacokinetics. Numerous breakthrough structures from a multitude of companies have led to compounds that are now key components of combination therapies with cure rates of >90%. Herein, we detail the compounds that have advanced to clinical trials including their design and their impact on the NS3/4a protease field.

PMID:
27544488
DOI:
10.1016/j.coph.2016.07.015
[Indexed for MEDLINE]

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