Department of Medicine I, University of Bonn Bonn, Germany.
Ther Clin Risk Manag. 2007 Aug;3(4):641-51.
Highly active antiretroviral therapy (HAART) has dramatically improved the prognosis of patients with HIV. Low adherence and toxicity among HIV-positive patients starting HAART, however, can lead to discontinuation of therapy and limit long-term treatment success. Moreover, increasing prevalence of primary resistance (>10%) as well as the accumulation of mutations resulting from continued selection pressure exerted by ongoing antiretroviral treatment in patients failing virologically, mean that new compounds are needed that retain antiretroviral activity against resistant strains. Tipranavir (Aptivus((R))) is a novel protease inhibitor (NPPI), which is characterized by a unique genetic resistance profile that allows it to remain active against HIV strains resistant to currently licensed protease inhibitors (PIs). Tipranavir was approved and licensed in the US and Europe in 2005 for treatment-experienced patients. This review summarizes the currently available data and studies on tipranavir and discusses the possible position of tipranavir in the currently available armamentarium of antiretroviral drugs.
高效抗逆转录病毒治疗（HAART）显著改善了 HIV 患者的预后。然而，开始 HAART 的 HIV 阳性患者的低依从性和毒性可能导致治疗中断，并限制长期治疗成功。此外，原发性耐药率的增加（>10%）以及由于继续选择压力导致的突变积累，这些突变是由病毒学失败的患者持续进行的抗逆转录病毒治疗施加的，这意味着需要新的化合物，这些化合物对耐药株仍具有抗逆转录病毒活性。替拉那韦（Aptivus((R)))是一种新型蛋白酶抑制剂（NPPI），其具有独特的遗传耐药谱，使其对目前已批准的蛋白酶抑制剂（PI）耐药的 HIV 株仍具有活性。替拉那韦于 2005 年在美国和欧洲获得批准和许可，用于治疗经验丰富的患者。这篇综述总结了目前关于替拉那韦的可用数据和研究，并讨论了替拉那韦在目前可用的抗逆转录病毒药物武器库中的可能地位。
