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bevirimat

Development stage
Phase 2
Lead developer
Myriad Genetics
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Bevirimat is a first-in-class HIV-1 maturation inhibitor derived from a betulinic acid-like compound originally isolated from the Chinese herb Syzygium claviflorum. It acts by binding to the Gag polyprotein at the CA/SP1 cleavage site and specifically inhibits protease-mediated cleavage of the capsid protein (CA) from its precursor (CA-SP1). This disruption prevents proper core condensation and results in the release of immature, non-infectious virus particles. Bevirimat has demonstrated potent activity against both wild-type and drug-resistant HIV-1 isolates in vitro and in vivo. The drug was developed as an oral small molecule for HIV infection but encountered resistance issues related to mutations near its target site. Clinical trials reached phase 2; however, further development was hampered by these resistance concerns[1][4][5][6].

Other names
bevirimatum3-O-(3',3'-dimethylsuccinyl) betulinic acid
02

Targets

HIV-1 CA/SP1 junction (HIV-1 Gag capsid/spacer peptide 1 junction)MHR (HIV-1 Gag major homology region)

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