整合酶抑制剂:小说类的抗逆转录病毒药物。

文章的细节

引用

复制到剪贴板

谢弗JJ, Squires柯

整合酶抑制剂:小说类的抗逆转录病毒药物。

安Pharmacother。2010年1月,44 (1):145 - 56。doi: 10.1345 / aph.1M309。Epub 2009年12月29日。

PubMed ID

20040702 (在PubMed

]

文摘

目的:复习药理、药效、安全、和电阻配置文件的整合酶抑制剂raltegravir elvitegravir。数据来源:搜索PubMed进行(必威国际app2000 - 2009年8月)使用以下关键词:raltegravir, mk - 0518年elvitegravir, gs - 9137。文章综述了评估内容和参考书目。数据只在摘要主要传染病和艾滋病会议同时进行了对夹杂物。研究选择和数据提取:体外研究包括调查;阶段1、2和3的临床试验;回顾性分析包括案例报告;药代动力学和药效学评价。数据综合:Raltegravir目前美国食品和药物管理局批准在首次治疗或有经验的成年人hiv - 1感染的管理作为一个优化组合方案的一部分。当结合其他活动代理,它展示了类似病毒学疗效96周依法韦伦的组合后,泰诺福韦,emtricitabine首次治疗的病人。 Unlike many antiretrovirals, raltegravir does not enter cytochrome P450 metabolism and instead undergoes glucuronidation. Elvitegravir is in the late stages of clinical development. A Phase 2 study has demonstrated virologic efficacy in treatment-experienced patients comparable to protease inhibitor-based regimens after 24 weeks. Boosting of elvitegravir through inhibition of CYP3A4 metabolism has been investigated and suggests a pharmacokinetic profile conducive to once-daily-dosing. Phase 2 and 3 clinical trials evaluating boosted elvitegravir are in process. The Phase 2 trial combines elvitegravir with a non-ritonavir boosting agent plus tenofovir/emtricitabine given once daily as a "quad-pill" formulation. The Phase 3 trial compares once-daily ritonavir-boosted elvitegravir with twice-daily raltegravir, each given with an optimized background regimen. Both integrase inhibitors are well tolerated and raltegravir has few drug-drug interactions. Resistance mutations have been identified in patients experiencing virologic failure and cross resistance between raltegravir and elvitegravir has been confirmed. CONCLUSIONS: The integrase inhibitors provide a novel target for antiretroviral therapy and provide an option for patients harboring resistance to other antiretrovirals.

DrugBank数据引用了这篇文章

药物

Elvitegravir