Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS.
Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS.
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DOI：
10.2147/hiv.s39178
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发表时间：
2014
期刊：
影响因子：
--
通讯作者：
Pandey KK
中科院分区：
文献类型：
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作者：
Pandey KK
人类免疫缺陷病毒1型（HIV-1）整合酶抑制剂属于一类新型抗逆转录病毒药物，具有高效和更好的耐受性。埃替拉韦（EVG）是美国食品和药物管理局批准的第二种整合酶抑制剂，与新型药物增强剂cobicistat（COBI）和两种核苷/核苷酸逆转录酶抑制剂恩曲他滨（FTC）和富马酸替诺福韦二吡呋酯（TDF）联合使用。这种药物组合（EVG/COBI/FTC/TDF）由吉利德科学公司开发和销售。（Foster City，CA，USA）作为ESPBILD ®，是第一种基于整合酶受体的单片剂方案，每天给药一次。在美国，它已被批准用于抗逆转录病毒治疗初治的HIV-1患者，估计肌酐清除率>70 mL/min。卫生与公众服务部已批准EVG/COBI/FTC/TDF作为HIV-1治疗的首选一线方案之一。在欧洲，欧洲药品管理局已批准在未经治疗的患者以及对瑞替卡韦中所含的任何抗病毒药物均无耐药突变的患者中使用瑞替卡韦。其作为固定剂量组合和每日一次剂量的可用性使得坚持的可能性很高。然而，如果需要，它也会降低剂量调整的可能性。
Human immunodeficiency virus type 1 (HIV-1) integrase inhibitors belong to a novel class of antiretroviral drugs with high potency and better tolerability. Elvitegravir (EVG) is the second integrase inhibitor approved by the US Food and Drug Administration when administered in combination with a novel pharmacoenhancer, cobicistat (COBI), and two nucleoside/nucleotide reverse transcriptase inhibitors, emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF). This combination of drugs (EVG/COBI/FTC/TDF) developed and marketed by Gilead Sciences Inc. (Foster City, CA, USA) as STRIBILD®, is the first integrase inhibitor-based single-tablet regimen administered once-daily. In the USA, it has been approved for use in antiretroviral treatment-naïve HIV-1 patients with estimated creatinine clearance of >70 mL/min. The Department of Health and Human Services has approved EVG/COBI/FTC/TDF as one of preferred first-line regimens for HIV-1 treatment. In Europe, the European Medicines Agency has approved STRIBILD in treatment-naïve patients as well as in patients having no resistant mutation to any of the antiviral agents contained in STRIBILD. Its availability as a fixed-dose combination and once-daily dosage makes the adherence highly likely. However, it also discounts the possibility of dosage adjustment if needed.