Drug intelligence / Profile preview

lopinavir + ritonavir + tenofovir + nucleoside

Development stage
Unknown
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

This combination antiretroviral therapy (ART) regimen consists of the protease inhibitors lopinavir and ritonavir, the nucleotide reverse transcriptase inhibitor tenofovir, and an additional nucleoside reverse transcriptase inhibitor (NRTI). This specific regimen was utilized as an active comparator in Phase III clinical trials sponsored by Bristol Myers Squibb, such as the AI424-045 study, which evaluated the efficacy and safety of atazanavir-based regimens in treatment-experienced HIV-1 infected patients. Lopinavir and ritonavir (often co-formulated as Kaletra) work by inhibiting the HIV protease enzyme, with ritonavir serving as a pharmacokinetic enhancer by inhibiting CYP3A4 metabolism to increase lopinavir exposure. Tenofovir and the NRTI component inhibit the HIV reverse transcriptase enzyme, acting as chain terminators to prevent the synthesis of viral DNA.

Other names
Lopinavir/ritonavir + tenofovir + nucleoside reverse transcriptase inhibitor
02

Targets

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

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