Category: pharmacological
Aliases: Prezista, DRV, TMC114
HIV protease inhibitor with the highest genetic barrier to resistance among current-era PIs — designed to retain potency against viruses with multiple PI-resistance mutations. Mechanism: competitive HIV-1 aspartyl protease inhibition. Always coadministered with a CYP3A4 booster (cobicistat as DRV/c in Prezcobix/Symtuza; ritonavir as DRV/r). Substrate of CYP3A4 — own clearance is dominated by oxidative metabolism. The DRV component of the Symtuza single-tablet regimen (DRV 800 / cobi 150 / FTC 200 / TAF 10 mg). Common AE: rash (sulfa moiety; rare SJS), GI intolerance. PK (Prezista label, boosted 800/100 mg PO qd with RTV at SS): Cmax ~6973 ng/mL, AUC(0-24) ~78,410 ng·h/mL, t½ 15 h supporting once-daily dosing. CL/F ≈ 10.2 L/h, V/F ≈ 221 L. Must be taken with food (F drops ~30% fasted).
PO: 15h