Drug intelligence / Profile preview

lopinavir + ritonavir + abacavir + lamivudine

Development stage
Unknown
Lead developer
Drugs for Neglected Diseases initiative
Modality
Small Molecules
Administration
Oral
01

Overview

This combination antiretroviral therapy consists of lopinavir, ritonavir, abacavir, and lamivudine. It was specifically evaluated in the Phase 4 KRETA clinical trial (GESIDA-6008-KRETA) sponsored by the Fundacion SEIMC-GESIDA to assess its efficacy in peripheral fat recovery (lipoatrophy) in HIV-infected patients. The regimen combines a boosted protease inhibitor (lopinavir/ritonavir) with two nucleoside reverse transcriptase inhibitors (abacavir/lamivudine). Lopinavir acts as the primary protease inhibitor, while ritonavir serves as a pharmacokinetic enhancer by inhibiting the Cytochrome P450 3A4 (CYP3A4) enzyme, thereby increasing lopinavir plasma concentrations. Abacavir and lamivudine function as chain terminators that inhibit the HIV reverse transcriptase enzyme, preventing viral DNA synthesis. The KRETA study compared this four-drug regimen against lopinavir/ritonavir monotherapy in patients who had developed lipoatrophy while on zidovudine-containing regimens.

Brand names
KaletraKivexaEpzicom
Other names
LPV/r + ABC/3TClopinavir/ritonavir + abacavir/lamivudine
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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