Drug interaction profile for GSK2248761, a next generation non-nucleoside reverse transcriptase inhibitor.

ABSTRACT:

Aim

To evaluate potential drug interactions with antiretroviral therapies or supportive therapies for use in conjunction with the once daily, next generation non-nucleoside reverse transcriptase inhibitor GSK2248761 in patients with HIV-1 infection.

Methods

A series of phase I drug interaction studies was conducted.

Results

GSK2248761 was shown to be a weak CYP3A4 and CYP2D6 inhibitor in a clinical study with a probe cocktail. Mean plasma concentration-time profiles for atazanavir, tenofovir disoproxil fumarate/emtricitabine (TDF/FTC), darunavir (DRV, administered with ritonavir [RTV]), and drospirenone/ethinylestradiol were similar following co-administration of GSK2248761. Plasma raltegravir AUC(0,τ) and C(max) increased by 18% with no change in Cτ when raltegravir

SUBMITTER: Piscitelli S 

PROVIDER: S-EPMC3630753 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature