Kilby J M, Saag M S
University of Alabama at Birmingham 35294-2050.
Infect Agents Dis. 1994 Dec;3(6):313-23.
Because the efficacy of currently approved antiretroviral agents used as prolonged monotherapy is limited, there is an urgent need for alternative agents for the treatment of HIV infection. We review the development of a diverse group of new compounds, the non-nucleoside reverse transcriptase inhibitors (NNRTIs), which are potent and specific inhibitors of HIV replication. Early clinical experience with the NNRTIs has demonstrated antiviral activity and a high therapeutic index, but some patients rapidly develop viral strains resistant to these drugs. The contributions of NNRTI studies to the basic science of HIV pathogenesis and the potential clinical role of these compounds, particularly in combination antiretroviral regimens, are discussed.
由于目前批准的用于长期单一疗法的抗逆转录病毒药物疗效有限,因此迫切需要用于治疗HIV感染的替代药物。我们综述了一组不同的新化合物——非核苷类逆转录酶抑制剂(NNRTIs)的研发情况,它们是HIV复制的强效特异性抑制剂。NNRTIs的早期临床经验已证明其具有抗病毒活性和高治疗指数,但一些患者会迅速产生对这些药物耐药的病毒株。本文讨论了NNRTIs研究对HIV发病机制基础科学的贡献以及这些化合物的潜在临床作用,特别是在联合抗逆转录病毒治疗方案中的作用。