Ugandan CFAR Laboratories, Division of Infectious Diseases, Department of Medicine, Case Western Reserve University, Cleveland, Ohio 44106, USA.
Cold Spring Harb Perspect Med. 2012 Apr;2(4):a007161. doi: 10.1101/cshperspect.a007161.
The most significant advance in the medical management of HIV-1 infection has been the treatment of patients with antiviral drugs, which can suppress HIV-1 replication to undetectable levels. The discovery of HIV-1 as the causative agent of AIDS together with an ever-increasing understanding of the virus replication cycle have been instrumental in this effort by providing researchers with the knowledge and tools required to prosecute drug discovery efforts focused on targeted inhibition with specific pharmacological agents. To date, an arsenal of 24 Food and Drug Administration (FDA)-approved drugs are available for treatment of HIV-1 infections. These drugs are distributed into six distinct classes based on their molecular mechanism and resistance profiles: (1) nucleoside-analog reverse transcriptase inhibitors (NNRTIs), (2) non-nucleoside reverse transcriptase inhibitors (NNRTIs), (3) integrase inhibitors, (4) protease inhibitors (PIs), (5) fusion inhibitors, and (6) coreceptor antagonists. In this article, we will review the basic principles of antiretroviral drug therapy, the mode of drug action, and the factors leading to treatment failure (i.e., drug resistance).
HIV-1 感染医学管理方面的最大进展是采用抗病毒药物治疗患者，这种方法可以将 HIV-1 复制抑制到检测不到的水平。HIV-1 被发现是艾滋病的致病因子，对病毒复制周期的认识不断提高，这为研究人员提供了知识和工具，有助于开展以特定药理药物靶向抑制为目标的药物发现工作。迄今为止，已有 24 种获得美国食品和药物管理局 (FDA) 批准的药物可用于治疗 HIV-1 感染。这些药物根据其分子机制和耐药谱分为六类：(1) 核苷类似物逆转录酶抑制剂 (NNRTIs)，(2) 非核苷逆转录酶抑制剂 (NNRTIs)，(3) 整合酶抑制剂，(4) 蛋白酶抑制剂 (PIs)，(5) 融合抑制剂，和 (6) 辅助受体拮抗剂。本文将综述抗逆转录病毒药物治疗的基本原则、药物作用模式以及导致治疗失败的因素（即耐药性）。
