Drug intelligence / Profile preview

lersivirine + tenofovir disoproxil fumarate + emtricitabine

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **triple fixed-dose combination** of antiretroviral agents designed to treat HIV-1 infection. It consists of: - **Lersivirine**, a next-generation **nonnucleoside reverse transcriptase inhibitor (NNRTI)** that binds allosterically to HIV-1 reverse transcriptase and inhibits the enzyme through a mixed noncompetitive mechanism, maintaining activity against multiple resistance-associated mutations[2]. - **Tenofovir disoproxil fumarate**, a prodrug of tenofovir, a **nucleotide reverse transcriptase inhibitor (NtRTI)**, inhibits HIV-1 reverse transcriptase by competing with deoxyadenosine 5'-triphosphate, leading to DNA chain termination[4][5]. - **Emtricitabine**, a **nucleoside reverse transcriptase inhibitor (NRTI)**, inhibits HIV-1 reverse transcriptase by competing with deoxycytidine 5'-triphosphate and terminating DNA chain elongation[4][5][6]. This combination is intended for use as **antiretroviral therapy** for HIV-1 infection, taking advantage of different inhibitory mechanisms and resistance profiles across the three classes. Lersivirine shows broad activity against mutant virus strains and may offer advantages where NNRTI resistance is present. The combination can potentially be administered orally as a single daily dose (based on similar NNRTI/NRTI/NtRTI triple combinations)[1][2][3]. As of now, lersivirine has not reached commercial approval, and this exact triple-drug combination is considered investigational.

Brand names
none known for this specific combination
Other names
none known for this specific combination
02

Targets

Human immunodeficiency virus type 1 reverse transcriptase

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