Temesgen Z, Talwani R, Rizza S A
Division of Infectious Diseases, Mayo Clinic, Rochester, Minnesota, USA.
Division of Infectious Diseases, University of Maryland, Baltimore, Maryland, USA.
Drugs Today (Barc). 2014 Jan;50(1):7-14. doi: 10.1358/dot.2014.50.1.2097790.
Dolutegravir, a next-generation integrase strand transfer inhibitor, was recently approved by the United States Food and Drug Administration to treat antiretroviral therapy-naive as well as treatment-experienced HIV-infected individuals, including those who have been treated with other integrase strand transfer inhibitors. Dolutegravir is the first stand-alone agent in its class, with a pharmacokinetic profile that allows once-daily administration without the requirement for pharmacologic boosting. It is metabolized primarily by UDP-glucuronosyltransferase 1-1 (UGT1A1) and is expected to have a limited propensity for drug-drug interactions. Furthermore, dolutegravir retains significant virologic activity against raltegravir- or elvitegravir-associated HIV-1 resistance mutations.
多替拉韦是一种新一代整合酶链转移抑制剂,最近获得美国食品药品监督管理局批准,用于治疗初治以及经治的HIV感染者,包括那些曾接受过其他整合酶链转移抑制剂治疗的患者。多替拉韦是该类别中的首个单药制剂,其药代动力学特征允许每日一次给药,无需进行药理增强。它主要通过尿苷二磷酸葡萄糖醛酸基转移酶1-1(UGT1A1)代谢,预计药物相互作用的可能性有限。此外,多替拉韦对与拉替拉韦或埃替拉韦相关的HIV-1耐药突变仍具有显著的病毒学活性。