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GS-9256 is a small molecule inhibitor of the hepatitis C virus (HCV) NS3/4A serine protease, developed for the treatment of chronic HCV infection. It features a macrocyclic structure with a novel phosphinic acid pharmacophore and demonstrates potent antiviral activity, particularly against HCV genotype 1. In preclinical studies, GS-9256 showed strong inhibition of viral replication with low cytotoxicity and favorable pharmacokinetic properties. Clinical trials have evaluated its efficacy both as monotherapy and in combination with other direct acting antivirals (DAAs), such as ribavirin, tegobuvir (GS‑9190), interferon-alpha, and ledipasvir. The drug was generally well tolerated in clinical studies but development did not progress beyond Phase 2[1][2][5][7].
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