The current standard of care for HIV/AIDS in the developed world is HAART therapy, usually a combination
of two reverse transcriptase inhibitors and a protease inhibitor. Despite the success of this regimen,
there is a continuing need for new drug options to overcome problems with tolerability and the emergence
of viral resistance. In this review we discuss the discovery of a potential new class of antiretroviral
therapeutics, known as maturation inhibitors, and the development of the first-in-class compound, bevirimat.
Bevirimat is distinguished from the currently available antiretrovirals by its unique target and
mode of action. While the specific interactions responsible for activity have yet to be fully characterized,
it is clear that the target for bevirimat is the Gag polyprotein precursor, the main structural protein responsible
for assembly and budding of virion particles. As basic research continues on the precise
mechanism of action of bevirimat, clinical development is progressing, with demonstration of both
safety and efficacy in early-stage trials. These encouraging results, coupled with the discovery and development
of future generations of maturation inhibitors, suggest that maturation inhibitors may be
added to the growing set of tools available to control HIV/AIDS.