Mercadel Candice J, Skelley Jessica W, Kyle Jeffrey A, Elmore Lindsey K
Samford University, Birmingham, AL, USA.
St. Vincent's Health System, Birmingham, AL, USA.
J Pharm Technol. 2014 Dec;30(6):216-226. doi: 10.1177/8755122514544126. Epub 2014 Jul 22.
To review the efficacy, safety, pharmacokinetics, pharmacodynamics, administration, drug interactions, and cost of dolutegravir (Tivicay), a third in class integrase strand transfer inhibitor (INSTI), for the treatment of human immunodeficiency virus (HIV-1) in adults. : MEDLINE, , ClinicalTrials.gov, and Google Scholar searches (January 2000 to May 2014) were conducted for articles published in English and limited to human subjects, using the key words antiretroviral drugs, HIV integrase strand transfer inhibitors, dolutegravir, DTG, and S/GSK1349572. : Following MEDLINE, , ClinicalTrials.gov, and Google Scholar searches, 6 clinical trials were identified and included in this review. Phase III/IV studies evaluating the safety and efficacy of dolutegravir in humans were selected and evaluated. : In treatment naïve and experienced patients dolutegravir was noninferior to raltegravir at suppressing viral load when added to background therapy. Abacavir/lamivudine/dolutegravir was noninferior to efavirenz/emtricitabine/tenofovir disoproxil fumarate and darunavir/ritonavir plus background therapy at suppressing viral load. In patients with multiple-class antiretroviral resistance at baseline, dolutegravir decreased HIV RNA by 1.4 log copies/mL at day 8, 63% of patients had achieved virologic suppression at week 8, and retained potency in treatment-experienced INSTI-resistant patients up to week 48 or 96 of follow-up. : Dolutegravir is a safe, effective, and well-tolerated treatment option for adults with HIV-1, even in the setting of resistance to other antiretrovirals.
为了评估多替拉韦(特威凯)的疗效、安全性、药代动力学、药效学、给药方式、药物相互作用及成本,多替拉韦是整合酶链转移抑制剂(INSTI)类中的第三种药物,用于治疗成人人类免疫缺陷病毒(HIV-1)感染。对MEDLINE、ClinicalTrials.gov和谷歌学术进行检索(2000年1月至2014年5月),查找以英文发表且限于人类受试者的文章,使用关键词抗逆转录病毒药物、HIV整合酶链转移抑制剂、多替拉韦、DTG和S/GSK1349572。在MEDLINE、ClinicalTrials.gov和谷歌学术检索之后,确定了6项临床试验并纳入本综述。选择并评估了评估多替拉韦在人类中的安全性和疗效的III/IV期研究。在初治和经治患者中,多替拉韦添加至背景治疗时在抑制病毒载量方面不劣于拉替拉韦。阿巴卡韦/拉米夫定/多替拉韦在抑制病毒载量方面不劣于依非韦伦/恩曲他滨/替诺福韦酯富马酸盐以及达芦那韦/利托那韦加背景治疗。在基线时具有多类抗逆转录病毒耐药性的患者中,多替拉韦在第8天使HIV RNA下降1.4 log拷贝/mL,63%的患者在第8周实现了病毒学抑制,并且在接受过治疗的对INSTI耐药的患者中,直至随访第48周或96周仍保持效力。多替拉韦是成人HIV-1感染的一种安全、有效且耐受性良好的治疗选择,即使在对其他抗逆转录病毒药物耐药的情况下也是如此。