Non-nucleoside reverse transcriptase inhibitors (NNRTls) are a structurally
diverse group of compounds which function as inhibitors of HIV-I replicati
on in vitro and in vivo. Viral resistance is mediated through alterations i
n the amino acids which form the allosteric site on the HIV-I reverse trans
criptase to which NNRTIs bind. The rapid emergence of resistant viruses has
limited the utility of NNRTI monotherapy; however, recent clinical studies
have shown that potent NNRTIs can contribute to profound suppression of HI
V replication when used in combination therapy. An understanding of the dev
elopment of resistance to NNRTIs is critical to the effective use of this c
lass of antiretroviral agents.