Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA, 94404, USA.
Clin Pharmacokinet. 2018 Nov;57(11):1369-1383. doi: 10.1007/s40262-018-0654-5.
Ledipasvir/sofosbuvir (Harvoni), a fixed-dose combination tablet of an NS5A inhibitor ledipasvir and an NS5B polymerase inhibitor sofosbuvir, is approved for the treatment of chronic hepatitis C virus infection. Ledipasvir/sofosbuvir exhibits a favorable drug-drug interaction profile and can be administered with various medications that may be used by hepatitis C virus-infected patients, including patients with comorbidities, such as co-infection with human immunodeficiency virus or immunosuppression following liver transplantation. Ledipasvir/sofosbuvir is not expected to act as a victim or perpetrator of cytochrome P450- or UDP-glucuronosyltransferase 1A1-mediated drug-drug interactions. With the exception of strong inducers of P-glycoprotein, such as rifampin, ledipasvir/sofosbuvir is not expected to act as a victim of clinically relevant drug-drug interactions. As a perpetrator of pharmacokinetic drug-drug interactions via P-glycoprotein/BCRP, ledipasvir/sofosbuvir should not be used with rosuvastatin and elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate, whereas its co-administration with amiodarone is not recommended because of a pharmacodynamic interaction. This review summarizes a number of drug interaction studies conducted in support of the clinical development of ledipasvir/sofosbuvir.
雷迪帕韦/索非布韦（Harvoni），一种 NS5A 抑制剂雷迪帕韦和 NS5B 聚合酶抑制剂索非布韦的固定剂量组合片剂，被批准用于治疗慢性丙型肝炎病毒感染。雷迪帕韦/索非布韦具有良好的药物相互作用特征，可以与可能被丙型肝炎病毒感染患者使用的各种药物一起使用，包括合并感染人类免疫缺陷病毒或肝移植后免疫抑制的患者。雷迪帕韦/索非布韦预计不会作为细胞色素 P450 或 UDP-葡萄糖醛酸转移酶 1A1 介导的药物相互作用的受害者或肇事者。除了利福平等强 P-糖蛋白诱导剂外，雷迪帕韦/索非布韦预计不会成为具有临床相关性的药物相互作用的受害者。作为通过 P-糖蛋白/BCRP 发生的药代动力学药物相互作用的肇事者，雷迪帕韦/索非布韦不应与瑞舒伐他汀和艾维雷韦/考比司他/恩曲他滨/替诺福韦二吡呋酯联合使用，而与胺碘酮联合使用不被推荐，因为存在药效学相互作用。这篇综述总结了一些支持雷迪帕韦/索非布韦临床开发的药物相互作用研究。
