Кобицистат

Описание

Cobicistat, a selective, mechanism-based CYP3A inhibitor, was discovered and developed by Gilead Sciences, Inc. In 2013, European Medicines Agency (EMA) approved cobicistat (Tybost) for the treatment of HIV-1 infection in combination with protease inhibitors (PIs) atazanavir or darunavir. Interestingly, cobicistat does not interact with HIV directly, but instead serves as a pharmacokinetic enhancer to boost the anti-HIV effect of atazanavir or darunavir through blockade of CYP3A. Cobicistat slows CYP-mediated metabolism of atazanavir and darunavir, resulting in prolonged systemic exposure of the drug(s). Cobicistat is also available as part of a fixed-dose combination tablet (Stribild) of four additional drugs with CYP3A liabilities (elvitegravir, cobicistat, emtricitabine and tenofovir disoproxil fumarate), which was approved in U.S. in 2012, and subsequently approved in Europe and Japan in 2013.

Использование

Cobicistat is a HIV protease inhibitor and have been coadministered with low-dose ritonavir (R535000) as a pharmacoenhancer, significantly increasing their plasma concentrations.