非核苷类反转录酶抑制剂及其第二代制剂的耐药与疗效

Resistance and efficacy of nonnucleoside reverse transcriptase inhibitor and its second-generation agents

非核苷类反转录酶抑制剂(nonnucleoside reverse transcriptase inhibitors,NNRTIs)是目前首选的抗HIV-1感染的药物,临床应用人数已经超过蛋白酶抑制剂。然而,NNRTIs具有低耐药基因屏障和高交叉耐药的特性,很多HIV感染者有过NNRTIs治疗失败的经历。因此,交叉耐药使第一代NNRTIs失去疗效。依曲韦林和利匹韦林是第二代NNRTIs,交叉耐药性小,对现有的NNRTIs耐药毒株具有极强的抗病毒活性,是HIV感染者重要的治疗药物。

Nonnucleoside reverse transcriptase inhibitors（NNRTIs） are preferably recommended as the first line therapeutic agents for treatment-naive patients with HIV-1 infection,and its popularity overweighs protease inhibitor-based antiretroviral therapy.However,NNRTIs available now possess inherent characteristics,such as low genetic barrier to resistance and high degree of cross-resistance,which limit their use in HIV therapy.Many HIV-infected patients have experienced treatment failure with a certain NNRTIs.Cross-resistance makes other first-generation NNRTIs ineffective.Etravirine and rilpivirine are second-generation NNRTIs which are not significantly hampered by cross-resistance and possess potent antiretroviral activity against current NNRTIs-resistant viral strains.These agents provide new and important therapy options for many HIV-infected patients.