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lopinavir + ritonavir + tenofovir disoproxil fumarate + emtricitabine or tenofovir disoproxil fumarate + lamivudine-The HIV Netherlands Australia Thailand Research Collaboration-HIV infection

Development stage
Unknown
Lead developer
HIV-NAT
Modality
Small Molecules
Administration
Oral
01

Overview

This combination regimen is a second-line antiretroviral therapy (ART) used for the treatment of HIV-1 infection, specifically evaluated in patients who have failed first-line non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimens. It consists of a boosted protease inhibitor, lopinavir/ritonavir (marketed as Kaletra), combined with a dual nucleoside/nucleotide reverse transcriptase inhibitor (NRTI) backbone of tenofovir disoproxil fumarate (TDF) plus either emtricitabine (FTC) or lamivudine (3TC). Lopinavir and ritonavir inhibit the HIV-1 protease enzyme, preventing the cleavage of gag-pol polyproteins and resulting in the production of immature, non-infectious viral particles; ritonavir also serves as a pharmacokinetic enhancer by inhibiting CYP3A4. The NRTIs (TDF, FTC, 3TC) act as chain terminators during reverse transcription, blocking the synthesis of viral DNA. This specific regimen was the control arm in the Phase 4 HIV-NAT 079 (HIV STAR) study conducted by the HIV Netherlands Australia Thailand Research Collaboration to assess the non-inferiority of lopinavir/ritonavir monotherapy.

Brand names
KaletraTruvadaEpivir
Other names
TDF/3TC/LPV/rTDF/FTC/LPV/r2 NRTIs + LPV/r
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)OAT1 (Organic anion transporter 1)SLC22A8 (Organic anion transporter 3)PR (Progesterone receptor)

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