HIV-1 maturation inhibitors: An update

Journal Article (Review;Journal)

HIV-1 maturation inhibitors are compounds other than HIV-1 protease inhibitors that inhibit HIV-1 maturation. This review focuses on triterpene derivatives, as their preclinical and clinical pharmacological profiles have been relatively well studied. Among the triterpene anti-HIV-1 maturation inhibitors, the betulinic acid derivative bevirimat dimeglumine (MPC-4326, formerly PA-457) is at the most advanced stage of drug development. Myriad Pharmaceuticals acquired all rights to bevirimat from Panacos Pharmaceuticals and continues to develop it under the new name MPC-4326. Although bevirimat is a potent HIV-1 maturation inhibitor, the results from phase II clinical trials indicate that it is less effective in a subset (30-40%) of HIV-1-positive individuals due to Gag polymorphisms in the glutamine-valine-threonine (QVT) motif of spacer peptide SP1. In addition to clinical development, recent medicinal chemistry approaches to obtain HIV-1 maturation inhibitors that are more potent than bevirimat are summarized. Copyright © 2009 Prous Science, S.A.U. or its licensors. All rights reserved.

Full Text

Duke Authors

Cited Authors

  • Dang, Z; Huang, L; Chen, C

Published Date

  • October 1, 2009

Published In

Volume / Issue

  • 34 / 10

Start / End Page

  • 797 - 802

International Standard Serial Number (ISSN)

  • 0377-8282

Digital Object Identifier (DOI)

  • 10.1358/dof.2009.34.10.1428207

Citation Source

  • Scopus