Croxtall Jamie D, Keam Susan J
Wolters Kluwer Health/Adis, 41 Centorian Drive, Mairangi Bay, North Shore 0754, Auckland, New Zealand.
Drugs. 2009 May 29;69(8):1059-75. doi: 10.2165/00003495-200969080-00007.
Raltegravir (Isentress), an integrase inhibitor, inhibits the insertion of HIV-1 complementary DNA into the host genome. It is indicated in combination with other antiretroviral therapy (ART) agents for the treatment of HIV-1 infection in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple ART agents. It is the first of a new class of ART agents to be approved that, as a result of a different mechanism of action to other ART agents, has good activity against multidrug-resistant HIV-1 strains. In clinical trials in treatment-experienced patients with HIV-1 infection and evidence of viral replication, the addition of oral raltegravir to an optimized background therapy (OBT) regimen improved virological and immunological responses at 16 and 48 weeks to a greater extent than placebo plus OBT. Raltegravir therapy was generally well tolerated, with a similar incidence of mild to moderate adverse events in the treatment and placebo arms. The introduction of integrase inhibitors extends the options available for managing treatment-experienced patients with multiple-drug-resistant HIV-1 infection. Results to date suggest that the combination of raltegravir and OBT will be a valuable treatment option for this difficult-to-treat patient group.
拉替拉韦(艾生特)是一种整合酶抑制剂,可抑制HIV-1互补DNA插入宿主基因组。它与其他抗逆转录病毒疗法(ART)药物联合使用,用于治疗有病毒复制证据且感染了对多种ART药物耐药的HIV-1毒株的成年经治患者。它是获批的一类新型ART药物中的首个药物,由于其作用机制与其他ART药物不同,因此对多重耐药HIV-1毒株具有良好活性。在有HIV-1感染且有病毒复制证据的成年经治患者的临床试验中,在优化背景疗法(OBT)方案中加用口服拉替拉韦,在16周和48周时的病毒学和免疫学反应改善程度均大于安慰剂加OBT。拉替拉韦治疗一般耐受性良好,治疗组和安慰剂组中轻度至中度不良事件的发生率相似。整合酶抑制剂的引入扩展了治疗多重耐药HIV-1感染的成年经治患者的可用选择。迄今为止的结果表明,拉替拉韦与OBT联合使用将是这类难治患者群体的一种有价值的治疗选择。