Drug intelligence / Profile preview

GSK2838232 + cobicistat

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK2838232 + cobicistat is an oral combination therapy consisting of **GSK2838232**, a second-generation, potent, small-molecule HIV-1 maturation inhibitor, and **cobicistat**, a cytochrome P450 3A (CYP3A) inhibitor used as a pharmacokinetic booster. GSK2838232 prevents the maturation of HIV-1 by blocking the final step in the processing of the Gag protein, resulting in the production of non-infectious viral particles. Cobicistat, with no intrinsic anti-HIV activity, inhibits CYP3A-mediated metabolism, significantly increasing the systemic exposure of GSK2838232 and permitting effective once-daily dosing. This combination has shown efficacy in reducing HIV-1 RNA levels and increasing CD4+ cell counts in short-term monotherapy studies. GSK2838232 is developed primarily for use in combination antiretroviral therapy for adults with HIV-1 infection[1][2][6].

02

Targets

CYP3A4 (Cytochrome P450 3A4)HIV-1 CA/SP1 junction (HIV-1 Gag capsid/spacer peptide 1 junction)

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