Drug intelligence / Profile preview

Truvada + estradiol

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

Overview

This drug combination refers to the co-administration of Truvada (a fixed-dose combination of tenofovir disoproxil fumarate and emtricitabine) and estradiol, often accompanied by leuprolide acetate (Lupron) for testosterone suppression, as part of a gender-affirming hormone therapy (GAHT) regimen. It is primarily studied by Johns Hopkins University in Phase I clinical trials to evaluate the two-way pharmacokinetic and pharmacodynamic interactions in transgender women using Truvada for HIV pre-exposure prophylaxis (PrEP). Truvada acts by inhibiting HIV reverse transcriptase through its components tenofovir disoproxil fumarate (a nucleotide reverse transcriptase inhibitor) and emtricitabine (a nucleoside reverse transcriptase inhibitor), while estradiol serves as exogenous estrogen for feminization. Research in this area aims to determine if estrogen-based hormone therapy reduces the protective concentrations of PrEP medications, as some studies have suggested a potential decrease in tenofovir levels in the presence of exogenous estrogens.

Brand names
Lupron
Other names
tenofovir disoproxil fumarate + emtricitabine + estradiolTDF/FTC + estradiolPrEP-GAHT Interactions in TGW
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseESR2 (ERβ)ESR1 (ERα)

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