Category: pharmacological
Aliases: ABT-378, LPV, Kaletra (with ritonavir)
HIV protease inhibitor — clinically available only as the Kaletra co-formulation with ritonavir (LPV/r 200/50 mg). Ritonavir component is sub-therapeutic for HIV but boosts lopinavir AUC ~80× via CYP3A4 inhibition. Largely displaced by integrase-inhibitor-based first-line regimens (DTG, BIC, RAL); retained for second-line use, pediatric HIV, and post-exposure prophylaxis in some settings. Investigated and rejected for COVID-19 (Recovery trial 2020 — no mortality benefit). Common AE: hyperlipidemia, insulin resistance, GI intolerance (worse than DRV/c). PK (Kaletra label, boosted 400/100 mg PO bid with RTV at SS): Cmax 9.8 ± 3.7 µg/mL, Cmin 5.5 ± 2.7 µg/mL, AUCtau (0-12) 92.6 ± 36.7 µg·h/mL. t½ ~6 h (boost makes effective t½ longer due to CYP3A4 inhibition). CL/F per 12-h interval ≈ 4.3 L/h, V/F ≈ 37 L.
PO: 6h