Raltegravir does not revert efflux activity of MDR1-P-glycoprotein in human MDR cells.

ABSTRACT:

Background

Raltegravir (Isentress®)(RALT) has demonstrated excellent efficacy in both treatment-experienced and naïve patients with HIV-1 infection, and is the first strand transfer integrase inhibitor to be approved for use in HIV infected adults worldwide. Since the in vivo efficacy of this class of antiviral drugs depends on their access to intracellular sites where HIV-1 replicates, we analyzed the biological effects induced by RALT on human MDR cell systems expressing multidrug transporter MDR1-P-glycoprotein (MDR1-Pgp).

Methods

Our study about RALT was performed by using a set of consolidated methodologies suitable for evaluating the MDR1-Pgp substrate nature of chemical and biological agents, namely: i) assay of drug efflux function; ii) analysis of MDR reversing capa

SUBMITTER: Dupuis ML 

PROVIDER: S-EPMC3852167 | biostudies-literature | 2013 Sep

REPOSITORIES: biostudies-literature