Drug intelligence / Profile preview

elsulfavirine + rifampin

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

Overview

**Elsulfavirine + rifampin** is a combination therapy considered for patients with **HIV infection and concomitant tuberculosis (TB)**. Elsulfavirine is a pro-drug that is rapidly converted to deselsulfavirine (VM-1500A), a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with long-acting pharmacology, superior safety/tolerability, and low risk of resistance to existing NNRTI mutations. Rifampin is a broad-spectrum antibiotic and first-line agent for TB that acts as a potent inducer of various cytochrome P450 enzymes. Elsulfavirine has been specifically studied in ART regimens for patients who require rifampin (such as those with HIV/TB co-infection), where it shows efficacy and tolerability without significant new safety concerns. The mechanism of action for elsulfavirine is NNRTI inhibition of HIV-1 reverse transcriptase; for rifampin, inhibition of bacterial DNA-dependent RNA polymerase. This combination is of particular importance for treating HIV patients with co-existing TB, as rifampin is essential for TB therapy and can interact with antiretrovirals, necessitating careful selection and monitoring of ART components[1].

Brand names
Elpida
Other names
deselsulfavirinerifampicin
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCA7 (Carbonic anhydrase VII)CA1 (Carbonic anhydrase 1)CA2 (Carbonic Anhydrase 2)

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