lersivirine + rifabutin

Lersivirine + rifabutin is a combination of two small molecule antiretroviral agents. Lersivirine is a nonnucleoside reverse transcriptase inhibitor (NNRTI) with a unique resistance profile and potent activity against both wild-type HIV-1 and NNRTI-resistant strains; it binds HIV-1 reverse transcriptase in a novel binding mode. Lersivirine is metabolized by CYP3A4 and UGT2B7 and is a weak inducer of CYP3A4, as well as a P-glycoprotein inhibitor. Rifabutin is an antibacterial drug used primarily for tuberculosis (TB), and it acts as a potent inducer of drug metabolism enzymes such as CYP3A4, which can decrease plasma concentrations of coadministered drugs. When lersivirine and rifabutin are administered together, rifabutin decreases lersivirine exposure significantly, while lersivirine has a moderate reducing effect on the exposure to the active metabolite of rifabutin (25-O-desacetyl-rifabutin). There is no unique brand for the combination; this regimen is used primarily for HIV-infected individuals with TB or mycobacterial co-infection in research settings. Lersivirine was developed by Pfizer.

Other names

lersivirinerifabutin