Bevirimat

Bevirimat (research code MPC-4326) is an anti-HIV drug derived from a betulinic acid-like compound, first isolated from Syzygium claviflorum, a Chinese herb.

[3] On June 8, 2010 Myriad Genetics announced that it was abandoning their HIV portfolio to focus more on cancer drug development.

Gag undergoes a chain of interactions both with itself and with other cellular and viral factors to accomplish the assembly of infectious virus particles.

HIV assembly is a two-stage process involving an intermediate immature capsid that undergoes a structurally dramatic maturation to yield the infectious particle.

This alteration is mediated by the viral protease, which cleaves the Gag polyprotein precursor, allowing the freed parts to reassemble to form the core of the mature virus particle.

First, bevirimat enters a growing virus particle as it buds from an infected cell and binds to the Gag polypeptide at the CA/SP1 cleavage site.

[7] Bevirimat was initially evaluated for safety and pharmacokinetics in a single-dose, randomized, double-blind, placebo-controlled phase clinical study in healthy volunteers.

[9] In vitro studies have shown that presence of a number of single nucleotide polymorphisms in the CA/SP1 cleavage site have resulted in resistance to bevirimat.

It has been shown that protease inhibitor resistance can result in an increase in the occurrence of mutations within the downstream QVT motif.