Raltegravir: The First HIV Type 1 Integrase Inhibitor
Raltegravir: The First HIV Type 1 Integrase Inhibitor
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DOI：
10.1086/597290
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发表时间：
2009-04-01
影响因子：
11.8
通讯作者：
Gulick, Roy M.
中科院分区：
文献类型：
--
作者：
Hicks, Charles;Gulick, Roy M.
雷特格韦是第一个批准的人类免疫缺陷病毒1型（HIV-1）整合酶抑制剂;它的目标是HIV-1整合的链转移步骤。临床试验表明，含雷特格韦的方案具有强效抗逆转录病毒活性，并且在HIV-1感染者中耐受性良好。在经历过抗逆转录病毒治疗的耐药HIV感染者中，含雷特格韦的治疗与优化的背景方案上级单独使用优化的背景方案。在初治患者中，当与替诺福韦和拉米夫定或恩曲他滨联合用药时，雷特格韦并不劣于依法韦仑。雷特格韦通过葡萄糖醛酸化代谢，而不是通过肝脏代谢;因此，药物相互作用的可能性降低。由编码HIV-1整合酶的基因中的取代所赋予的耐药性在病毒学失败后相对频繁地发展。作为一种具有新作用机制的抗逆转录病毒药物，雷特格韦是HIV-1治疗方案的重要进展。
Raltegravir is the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor; it targets the strand transfer step of HIV-1 integration. Clinical trials have demonstrated that raltegravir-containing regimens have potent anti-retroviral activity and are well tolerated in HIV-1-infected individuals. In antiretroviral treatment-experienced persons with drug-resistant HIV infection, raltegravir-containing treatment with an optimized background regimen was superior to an optimized background regimen alone. In treatment-naive persons, raltegravir was not inferior to efavirenz when the drugs were administered with tenofovir and lamivudine or emtricitabine. Raltegravir is metabolized by glucuronidation, not hepatically; thus, the potential for drug-drug interactions is decreased. Drug resistance, conferred by substitutions in the gene coding for the HIV-1 integrase enzyme, develops relatively frequently after virologic failure. As an antiretroviral drug with a novel mechanism of action, raltegravir is an important advancement in HIV-1 treatment options.