Drug intelligence / Profile preview

GSK2838232 + ritonavir

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK2838232 + ritonavir is a combination of a novel HIV-1 maturation inhibitor (GSK2838232) and ritonavir, a pharmacokinetic enhancer. GSK2838232 acts by binding to the HIV Gag protein, thereby inhibiting viral maturation and forming immature, non-infectious viral particles. When administered with ritonavir, which inhibits CYP3A-mediated metabolism, the plasma exposure of GSK2838232 is significantly increased, optimizing its therapeutic effect. GSK2838232 was developed by GSK for use in combination antiretroviral therapy, particularly as an oral, once-daily regimen. Clinical studies have shown this combination is generally well tolerated and achieves plasma concentrations above target thresholds in healthy subjects and HIV-1-infected individuals[1][2][3][4].

02

Targets

CYP3A (CYP3A family)Gag (HIV-1 Gag polyprotein)PR (Progesterone receptor)

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