Drug intelligence / Profile preview

tenofovir disoproxil fumarate + emtricitabine + dolutegravir

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

Overview

Tenofovir disoproxil fumarate + emtricitabine + dolutegravir is a triple-drug antiretroviral therapy (ART) regimen used for the treatment of HIV-1 infection. It combines two nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs)—tenofovir disoproxil fumarate (TDF, 300 mg) and emtricitabine (FTC, 200 mg)—with the integrase strand transfer inhibitor (INSTI) dolutegravir (DTG, 50 mg). TDF and FTC act as chain terminators that inhibit the HIV-1 reverse transcriptase enzyme, while dolutegravir blocks the HIV-1 integrase enzyme, preventing the viral DNA from integrating into the host cell genome. This combination is considered a standard-of-care first-line treatment for HIV-1 and is often used as a reference arm in clinical trials evaluating newer regimens, such as the Phase 4 study by Fundación Huésped comparing it to the two-drug regimen dolutegravir/lamivudine in pregnant women.

Other names
tenofovir disoproxil fumarate + emtricitabine + dolutegravirTDF/FTC + DTGTDF/FTC/DTG
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseOCT2 (Organic cation transporter 2)Integrase allosteric pocket (HIV)

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