Drug intelligence / Profile preview

INI-based regimen + tenofovir alafenamide + emtricitabine

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

Overview

This regimen is an **antiretroviral therapy (ART) combination** used for the treatment of HIV-1 infection. It consists of an **integrase strand transfer inhibitor (INSTI or "INI")** as the anchor drug (such as bictegravir or dolutegravir) combined with **tenofovir alafenamide** and **emtricitabine**, both of which are **nucleoside reverse transcriptase inhibitors (NRTIs)**. The **INSTI** component blocks the integration of HIV-1 DNA into the host genome, while **tenofovir alafenamide (a prodrug of tenofovir)** and **emtricitabine** inhibit reverse transcriptase, causing chain termination of viral DNA synthesis. This three-drug regimen is recommended as a first-line, once-daily therapy due to its high efficacy, high genetic barrier to resistance (especially with bictegravir or dolutegravir), and favorable safety and tolerability profile. Fixed-dose combinations with these agents are approved for HIV-1 treatment in adults and pediatric patients above certain weight thresholds[2][3][4].

Brand names
Biktarvy
Other names
integrase inhibitor-based regimen + tenofovir alafenamide + emtricitabine
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseIntegrase allosteric pocket (HIV)

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