dasabuvir + ketoconazole

Dasabuvir (formerly ABT-333) + ketoconazole refers to the co-administration of dasabuvir, a non-nucleoside inhibitor of hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and ketoconazole, a potent inhibitor of the cytochrome P450 3A enzyme (CYP3A). Dasabuvir is developed primarily for the treatment of chronic HCV genotype 1 infection. It works selectively by binding to an allosteric site on NS5B polymerase, inhibiting viral replication. Ketoconazole is co-administered in some pharmacokinetic studies to assess interactions, as it is used as a prototypical strong CYP3A inhibitor. In healthy subjects, ketoconazole increases dasabuvir (ABT-333) exposure (Cmax by ~50%, AUC by ~64%), but FDA guidance does not classify dasabuvir as a sensitive substrate of CYP3A since the increase is less than twofold. This drug combination is primarily referenced in clinical pharmacokinetic and drug interaction studies, not as a clinical therapy itself[1].

Other names

dasabuvir + ketoconazole