Drug intelligence / Profile preview

GSK2838232

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK2838232 is a second-generation, potent, small-molecule HIV-1 maturation inhibitor developed for oral administration. It acts by binding to the HIV-1 gag protein and disrupting its cleavage by the viral protease, a process essential for forming mature and infectious virus particles. This mechanism maintains antiviral efficacy even against drug-resistant strains of HIV-1, including those with polymorphic gag sequences that were problematic for earlier drugs in this class. The compound is intended for use as part of combination antiretroviral therapy (ART) and has demonstrated safety and antiviral activity in phase 1 and phase 2a clinical studies when boosted with pharmacoenhancers such as cobicistat or ritonavir[1][4][6].

Other names
(2S)-1-[(2S,4R)-4-Benzyl-2-hydroxy-5-{[(1S,2R,5S)-2-hydroxy-5-methylcyclopentyl]amino}-5-oxopentyl]-4-{[6-chloro-5-(4-methyl-1-piperazinyl)-2-pyrazinyl]carbonyl}-N-(2-methyl-2-propanyl)-2-piperazinecarboxamide(2S)-1-((2S,4R)-4-benzyl-2-hydroxy-4-(((1S,2R,5S)-2-hydroxy-5-methylcyclopentyl)carbamoyl)butyl)-N-tert-butyl-4-(6-chloro-5-(4-methylpiperazin-1-yl)pyrazine–carbonyl)piperazine–carboxamiden-[2(s)-cyclopentyl–hydroxy–methyl]-[(tert-butylaminocarbonyl)-(n-methylpiperazinylchlo ro-pyrazin-carbon yl)piperazino]-hydroxy–phen ylmeth yl-pentanamide
02

Targets

Gag (HIV-1 Gag polyprotein)

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