Drug intelligence / Profile preview

emtricitabine + tenofovir disoproxil fumarate + lopinavir + ritonavir

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

Overview

This combination antiretroviral therapy (ART) regimen consists of two nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs), emtricitabine and tenofovir disoproxil fumarate, and two protease inhibitors (PIs), lopinavir and ritonavir. The regimen was specifically evaluated in the Phase 3 2LADY trial (ANRS 12169) conducted by the French National Agency for Research on AIDS and Viral Hepatitis (ANRS, now part of Emerging Infectious Diseases) in Sub-Saharan Africa. Emtricitabine and tenofovir work by inhibiting the HIV-1 reverse transcriptase enzyme, thereby preventing viral DNA synthesis and replication. Lopinavir inhibits the HIV-1 protease enzyme, which is essential for the cleavage of viral polyproteins into functional units. Ritonavir is included at a low dose primarily as a pharmacokinetic enhancer (booster) that inhibits the Cytochrome P450 3A4 (CYP3A4) enzyme, thereby increasing and sustaining therapeutic concentrations of lopinavir. This combination was a World Health Organization (WHO) recommended second-line treatment strategy for HIV-1 infected patients who had failed initial non-nucleoside reverse transcriptase inhibitor (NNRTI)-based therapy.

Brand names
TruvadaKaletraAluvia
Other names
TDF/FTC + LPV/rTDF + FTC + LPV + RTVemtricitabine/tenofovir + lopinavir/ritonavir
02

Targets

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

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