Resistance to non-nucleoside inhibitors of HIV-I reverse transcriptase

Non-nucleoside reverse transcriptase inhibitors (NNRTls) are a structurally diverse group of compounds which function as inhibitors of HIV-I replication in vitro and in vivo. Viral resistance is mediated through alterations in the amino acids which form the allosteric site on the HIV-I reverse transcriptase 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 HIV replication when used in combination therapy. An understanding of the development of resistance to NNRTIs is critical to the effective use of this class of antiretroviral agents.