Cobicistat Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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.
Verwenden
Cobicistat is a HIV protease inhibitor and have been coadministered with low-dose ritonavir (R535000) as a pharmacoenhancer, significantly increasing their plasma concentrations.
Cobicistat Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
