Category: pharmacological
Aliases: EVG, GS-9137
HIV integrase strand transfer inhibitor (INSTI) — earlier-generation INSTI requiring CYP3A4 boost (cobicistat) for adequate exposure. Stribild (EVG/COBI/FTC/TDF) and Genvoya (EVG/COBI/FTC/TAF) were once-daily fixed-dose regimens. Largely displaced by bictegravir (no boost needed) and dolutegravir (low boost requirement, higher barrier to resistance). Substrate of CYP3A4 + UGT1A1/3. PK (Vitekta label, 150 mg PO qd boosted with cobicistat 150 mg or ritonavir 100 mg): Tmax ~4 h, t½ 13 h boosted (vs. ~3 h unboosted — the booster eliminates CYP3A4 first-pass). Protein binding 98–99%. CYP3A substrate (primary) + UGT1A1/3 glucuronidation. F nominally low without booster but clinical-use F is "effective ~0.5" with COBI (the Stribild / Genvoya regimen). Always given with food (increases AUC substantially). Apparent Vd ~120 L (textbook for the boosted state).
PO: 13h