Division of Infectious Disease, Emory University School of Medicine, Atlanta, Georgia 30303, USA.
Curr Opin HIV AIDS. 2012 Sep;7(5):409-14. doi: 10.1097/COH.0b013e3283562a27.
In this review we will discuss recent findings on the use of inhibitors of the HIV-1 integrase enzyme for the treatment of antiretroviral naive patients. We will also discuss differences between integrase inhibitors, and comment on the use of this class of drugs in the future.
Raltegravir when taken twice daily is as effective and well tolerated as efavirenz. Once daily dosing of raltegravir is virologically inferior to raltegravir taken twice daily. A novel nucleoside-free regimen of raltegravir in combination with a once daily ritonavir-boosted protease inhibitor did not produce adequate viral suppression, although raltegravir with a twice daily protease inhibitor yielded better results. Subset analyses have demonstrated a favorable impact of raltegravir on lipid levels and body fat composition. Two once daily integrase inhibitors not yet Food and Drug Administration-approved, elvitegravir and dolutegravir, have completed phase-2 testing and are also virologically noninferior to efavirenz.
Integrase inhibitors provide potent antiretroviral activity, little short-term toxicity and excellent tolerability. For patients with preexisting atherosclerosis or cardiac risk factors this class of therapy is a logical preferred treatment choice. Raltegravir is a preferred option for those in whom therapy for hepatitis C virus infection is anticipated.
在这篇综述中，我们将讨论最近关于 HIV-1 整合酶抑制剂用于治疗抗逆转录病毒初治患者的发现。我们还将讨论整合酶抑制剂之间的差异，并对该类药物的未来应用进行评论。
每日两次服用拉替拉韦的疗效与依非韦伦相当，且耐受性良好。每日一次服用拉替拉韦的病毒学疗效不如每日两次服用拉替拉韦。虽然每日两次服用蛋白酶抑制剂联合拉替拉韦的新型无核苷方案未能产生足够的病毒抑制，但每日一次服用利托那韦增强的蛋白酶抑制剂的拉替拉韦并未产生足够的病毒抑制作用。亚组分析表明，拉替拉韦对血脂水平和体脂组成有有利影响。两种尚未获得美国食品和药物管理局批准的每日一次整合酶抑制剂，艾维雷格和多替拉韦，已完成 2 期临床试验，与依非韦伦相比也具有非劣效性。
整合酶抑制剂具有强大的抗逆转录病毒活性、较少的短期毒性和极好的耐受性。对于存在动脉粥样硬化或心脏危险因素的患者，此类治疗方法是合理的首选治疗方案。对于那些预期需要治疗丙型肝炎病毒感染的患者，拉替拉韦是首选。
