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      Rolapitant: first global approval.

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      Drugs

      Springer Nature

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          Abstract

          Rolapitant (Varubi™) 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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          Author and article information

          Journal
          Drugs
          Drugs
          Springer Nature
          1179-1950
          0012-6667
          Nov 2015
          : 75
          : 16
          Affiliations
          [1 ] Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. dru@adis.com.
          Article
          10.1007/s40265-015-0485-8
          10.1007/s40265-015-0485-8
          26467681

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