Drug intelligence / Profile preview

elvucitabine + efavirenz + tenofovir

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

A combination of three antiretroviral drugs—**elvucitabine**, **efavirenz**, and **tenofovir**—investigated for use in the treatment of **HIV-1 infection**. - **Elvucitabine** is a nucleoside reverse transcriptase inhibitor (NRTI), structurally related to lamivudine and emtricitabine, and works by inhibiting HIV reverse transcriptase, causing DNA chain termination. - **Efavirenz** is a non-nucleoside reverse transcriptase inhibitor (NNRTI), which binds directly to HIV reverse transcriptase, causing a conformational change and inhibiting its activity. - **Tenofovir** (used clinically as tenofovir disoproxil fumarate or tenofovir alafenamide) is a nucleotide reverse transcriptase inhibitor (NtRTI), inhibiting HIV-1 reverse transcriptase by competing with natural substrates and causing DNA chain termination. The use of this triple combination leverages the complementary mechanisms of action of NRTIs, NNRTIs, and NtRTIs for optimal suppression of HIV-1 replication and reduction of resistance development. The combination is not marketed under a known brand name and differs from the widely used combination of efavirenz, emtricitabine, and tenofovir (Atripla), as elvucitabine is used here instead of emtricitabine.

02

Targets

Human immunodeficiency virus type 1 reverse transcriptase

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