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硫酸阿扎那韦+考比司他治疗人类免疫缺陷病毒(HIV)感染。

Atazanavir sulfate + cobicistat for the treatment of HIV infection.

机构信息

a Instituto de Saúde Ambiental, Faculdade de Medicina da Universidade de Lisboa , Lisboa , Portugal.

出版信息

Expert Rev Anti Infect Ther. 2017 Jun;15(6):569-576. doi: 10.1080/14787210.2017.1323634. Epub 2017 May 9.

Abstract

During last two decades several drugs were developed to offer long-term benefits in terms of virologic efficacy, favourable tolerability and toxicity profiles in treatment of HIV infection. Pharmacokinetics boosting of protease inhibitor allows a higher genetic barrier, as few or no drug-resistant mutations are detected in patients with virologic failure. Areas covered: Atazanavir sulfate + cobicistat (ATV/c) was recently approved for the treatment of HIV-1 infection. Bioequivalence between cobicistat (COBI) and ritonavir (RTV) as a pharmacoenhancer of ATV was established. Additionally, randomized clinical trials demonstrated that ATV/c and ATV/ritonavir had comparable efficacy and safety profiles. Low rates of virologic failure and no ATV resistance mutations were observed in these clinical trials. Therefore, COBI shows increased advantages over RTV, such as no activity against HIV, fewer drug-drug interactions and better solubility, which promotes coformulation strategies with less pill burden, better tolerability, and, potentially, higher life-long treatment adherence. Expert commentary: ATV/c regimen supports its useas an effective treatment option for HIV-1 infected patients with increased cardiovascular disease and chronic kidney disease risk associated with aging. In addition, ATV/c is a new opportunity to expand the strategy of switch to a dual therapy to lower the risk of long-term toxicities as well as the advantage of its cost-benefit.

摘要

在过去的二十年中,已经开发出了几种药物,这些药物在治疗 HIV 感染方面具有长期的病毒学疗效、良好的耐受性和毒性特征。蛋白酶抑制剂的药代动力学增强作用可提供更高的遗传屏障,因为在病毒学失败的患者中很少或没有检测到耐药性突变。

涵盖领域

硫酸阿扎那韦+考比司他(ATV/c)最近被批准用于治疗 HIV-1 感染。考比司他(COBI)和利托那韦(RTV)作为 ATV 的药物增强剂具有生物等效性。此外,随机临床试验表明,ATV/c 和 ATV/利托那韦在疗效和安全性方面具有相似的特征。这些临床试验中观察到病毒学失败率低,且未发现 ATV 耐药突变。因此,COBI 相对于 RTV 具有更多优势,如对 HIV 无活性、药物相互作用较少、溶解度更高,这促进了与较少药丸负担、更好耐受性和潜在更高终身治疗依从性的联合配方策略。

专家评论

ATV/c 方案支持将其用作与老龄化相关的心血管疾病和慢性肾脏病风险增加的 HIV-1 感染患者的有效治疗选择。此外,ATV/c 是一种新的机会,可以扩大双重治疗策略,以降低长期毒性的风险,以及其成本效益的优势。

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