Pandey Krishan K
Institute for Molecular Virology, Saint Louis University Health Sciences Center, St Louis, MO, USA.
HIV AIDS (Auckl). 2014 May 16;6:81-90. doi: 10.2147/HIV.S39178. eCollection 2014.
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.
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，具有高效能和更好的耐受性。埃替格韦（EVG）是美国食品药品监督管理局批准的第二种整合酶抑制剂，它与新型增效剂考比司他（COBI）以及两种核苷/核苷酸逆转录酶抑制剂恩曲他滨（FTC）和替诺福韦酯富马酸盐（TDF）联合使用。由吉利德科学公司（美国加利福尼亚州福斯特城）研发并上市的这种药物组合（EVG/COBI/FTC/TDF）商品名为“绥美凯（STRIBILD）”，是首个基于整合酶抑制剂的每日一次单一片剂方案。在美国，它已被批准用于估算肌酐清除率>70 mL/min的初治HIV-1患者。美国卫生与公众服务部已批准将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绥美凯用于初治患者以及对绥美凯中所含任何抗病毒药物均无耐药突变的患者。其固定剂量组合和每日一次给药的特性使患者很可能坚持用药。然而，如果需要，这也排除了剂量调整的可能性。
