An HIV maturation inhibitor
GSK2838232 is an HIV-1 maturation inhibitor [1] [2].
HIV-1 maturation inhibitors disrupt the cleavage of the HIV-1 gag protein immediate precursor by the enzyme HIV-1 protease. Maturation inhibitors bind the gag protein, which leads to the formation of immature, noninfectious virus particles incapable of infecting other cells. Also, maturation inhibitors inhibit HIV infections with resistance.
GSK2838232 is a HIV-1 maturation inhibitor and is active against a broad range of isolates, including those resistant to bevirimat [1]. GSK2838232 was developed for the treatment of chronic HIV infection. A phase I study in HIV-negative individuals had been completed. Single doses of 5, 10 or 20 mg GSK2838232 were used to evaluate the initial safety, tolerability, pharmacokinetics profile, and the effects of food and ritonavir on GSK2838232’s bioavailability and pharmacokinetics [2].
参考文献:
[1].? Olender SA, Taylor BS, Wong M, et al. CROI 2015: Advances in Antiretroviral Therapy. CROI 2015 Highlights: Antiretroviral Therapy Volume 23 Issue 1 March/April 2015.
[2].? Horn T, Collins S. The Antiretroviral Pipeline. Antiretrovirals, 2014 PIPELINE REPORT.
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