Darunavir Stands Up as Preferred HIV Protease Inhibitor.

杜鲁特格拉维尔 达芦那韦 利比韦林 雷特格韦 阿巴卡韦 医学 苄腈 耐受性 马拉维洛克 整合酶抑制剂 病毒载量 病毒学 养生 药理学 钴试剂 奈韦拉平 固定剂量组合 蛋白酶抑制剂(药理学) 内科学 人类免疫缺陷病毒(HIV) 抗逆转录病毒疗法 不利影响
作者
Josep Mallolas
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期刊:PubMed 卷期号:19 (2): 105-112 被引量:19
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Current antiretroviral therapy reaches and maintains viral suppression over the years in more than 90% of treated HIV-infected individuals. Although integrase inhibitors are the preferred third agent in antiretroviral therapy in the current guidelines, rilpivirine, a non-nucleoside reverse transcrip- tase inhibitor, and darunavir (DRV), a second-generation protease inhibitor, are the preferred third companion to be used along with a backbone of two nucleos(t)ide reverse transcriptase inhibitors as first-line triple HIV combination treatment. However, rilpivirine is not recommended in patients with plasma HIV-RNA above 100,000 copies/mL. Raltegravir requires uncomfortably twice daily dosing, whereas dolutegravir is often given as coformulation with abacavir, a drug that requires prior HLA-B5701 testing. Antiretroviral combinations based on DRV provide a unique robustness in terms of antiviral potency and resistance barrier, rendering this drug pivotal as part of rescue regimens for the treatment failures. Furthermore, dual antiretroviral therapy with DRV plus lami- vudine has been tested with success as maintenance therapy. Finally, DRV has demonstrated its safety and efficacy in special patient populations, including pregnant women, pediatrics, HIV-2 infection, and individuals coinfected with viral hepatitis. Single-tablet regimens containing DRV coformulated with cobicistat alone or with other antiretrovirals should improve drug adherence. These fixed-dose combinations represent a step forward universal antiretroviral regimen, ensuring maximal efficacy, tolerability, and convenience.

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