与唑抗真菌药物动力学和耐受性Letermovir Coadministered(泊沙康唑和伏立康唑)在健康受试者。

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马歇尔王,麦克雷博士JB,玛莎,门泽尔K,刘F, van Schanke,德哈喝酒,Hussaini,乔丹人力资源,德雷克塞尔M, Kantesaria BS,蔡C,曹CR、Hulskotte EGJ, Butterton JR Iwamoto M

与唑抗真菌药物动力学和耐受性Letermovir Coadministered(泊沙康唑和伏立康唑)在健康受试者。

中国新药杂志。2018年7月,58 (7):897 - 904。doi: 10.1002 / jcph.1094。Epub 2018年3月26日。

PubMed ID

29578577 (在PubMed

]

文摘

Letermovir是人类巨细胞病毒terminase抑制剂预防巨细胞病毒感染的造血干细胞移植受者。泊沙康唑(POS)的基质glucuronosyltransferase 22,和伏立康唑(VRC) CYP2C9/19衬底,通常管理移植受者。因为共同的唑类letermovir预计,letermovir接触这些抗真菌的影响进行了研究。进行了两个试验在健康女性受试者18 - 55岁。在实验1中,单剂POS 300毫克独自管理,紧随其后的是一个7天冲刷;然后letermovir 480毫克每日一次给14天的POS 300毫克coadministered 14天。在实验2中,第一天VRC 400毫克每12小时;天2和3,VRC 200毫克每12个小时,第四天VRC 200毫克。天5到8,letermovir 480毫克每天一次。天重复9至12天1到4 coadministered letermovir 480毫克每日一次。 In both trials, blood samples were collected for the assessment of the pharmacokinetic profiles of the antifungals, and safety was assessed. The geometric mean ratios (90%CIs) for POS+letermovir/POS area under the curve and peak concentration were 0.98 (0.83, 1.17) and 1.11 (0.95, 1.29), respectively. Voriconazole+letermovir/VRC area under the curve and peak concentration geometric mean ratios were 0.56 (0.51, 0.62) and 0.61 (0.53, 0.71), respectively. All treatments were generally well tolerated. Letermovir did not affect POS pharmacokinetics to a clinically meaningful extent but decreased VRC exposure. These results suggest that letermovir may be a perpetrator of CYP2C9/19-mediated drug-drug interactions.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
Letermovir	细胞色素P450 2 c9	蛋白质	人类	没有	诱导物	细节