tegobuvir

Tegobuvir is a small molecule, investigational antiviral drug developed for the treatment of chronic hepatitis C virus (HCV) infection, specifically targeting genotype 1. It belongs to a novel class of non-nucleoside inhibitors (NNIs) that selectively inhibit HCV RNA replication by targeting the viral NS5B RNA-dependent RNA polymerase. Tegobuvir acts through a unique mechanism involving metabolic activation within hepatocytes; after CYP-mediated metabolism and glutathione conjugation, it covalently binds to the NS5B polymerase at specific sites in the thumb subdomain, thereby inhibiting viral replication. Resistance mutations have been mapped to positions 316, 445, 448, and 452 of NS5B. Despite potent activity in vitro and in clinical studies against HCV genotype 1a/1b, development was discontinued after Phase 2 trials due to limited efficacy compared with other emerging therapies[1][2][3][4][5][6][7][8].

Other names

tegobuvir