Rolapitant: First Global Approval

被引：13
作者：
Syed, Yahiya Y. [1 ]
机构：
[1] Springer, Auckland 0754, New Zealand
来源：
DRUGS | 2015年 / 75卷 / 16期
关键词：
CHEMOTHERAPY-INDUCED NAUSEA; EMETOGENIC CHEMOTHERAPY; DOUBLE-BLIND; CANCER; PREVENTION; EFFICACY; SAFETY;
D O I：
10.1007/s40265-015-0485-8
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Rolapitant (Varubi (TM)) is an orally active neurokinin-1 receptor antagonist developed by TESARO and approved in the USA for use in combination with other antiemetic agents for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Unlike other approved agents in this class, rolapitant does not interact with cytochrome P450 (CYP) enzyme CYP3A4. It also has a long elimination half-life which means that a single dose could prevent CINV during the entire at-risk period (0-120 h). An intravenous formulation of rolapitant is under clinical development in the USA. Phase II development of rolapitant in postoperative nausea and vomiting, and cough appears to have been discontinued. This article summarizes the milestones in the development of rolapitant leading to the first approval for the prevention of CINV.
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页码：1941 / 1945
页数：5
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