Maturation inhibitor

A maturation inhibitor is a type of antiretroviral drug used in treating HIV infected patients that inhibits the last protease cleavage event between capsid protein p24 and spacer peptide SP1 in Gag, resulting in the release of immature, noninfectious particles. Maturation inhibitors have a mechanism of action that is different from any other antiretroviral drug used in treating HIV infected patients.From: Advances in Chromatographic Techniques for Therapeutic Drug Monitoring [2019], Kucers’ The Use of Antibiotics [2017]

Investigational Antiviral Drugs

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Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017

John Mills, Suzanne M. Crowe, Marianne Martinello

GSK 2838232 is a maturation inhibitor with an EC50 of 0.8–4.3nM against a broad spectrum of HIV strains with a range of genotypes. It is not affected by previous protease inhibitor experience. Three phase Ia studies in healthy subjects have been completed to study pharmacokinetics and safety. A dose escalation study of GSK2838232 with ritonavir boosting in HIV-infected subjects is active as of July 2016 (NCT02795754) (Wang et al., 2015a).

Current insights into anti-HIV drug discovery and development: a review of recent patent literature (2014–2017)

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Published in Expert Opinion on Therapeutic Patents, 2018

Xiaofang Zuo, Zhipeng Huo, Dongwei Kang, Gaochan Wu, Zhongxia Zhou, Xinyong Liu, Peng Zhan

Triterpene derivative bevirimat (49) was an HIV-1 maturation inhibitor that reached phase II clinical trials before being discontinued [103]. BMS-955176 (50) is a potent, orally active, new generation HIV-1 maturation inhibitor, which is currently in phase IIb clinical trials as part of a combination antiretroviral regimen [104,105].

Maturation inhibitor

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Investigational Antiviral Drugs

Current insights into anti-HIV drug discovery and development: a review of recent patent literature (2014–2017)