Literature DB >> 26467681

Rolapitant: first global approval.

Yahiya Y Syed1.   

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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Year:  2015        PMID： 26467681     DOI： 10.1007/s40265-015-0485-8

Source DB:  PubMed          Journal:  Drugs        ISSN： 0012-6667            Impact factor:   9.546


  5 in total

1.  Safety and efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting after administration of moderately emetogenic chemotherapy or anthracycline and cyclophosphamide regimens in patients with cancer: a randomised, active-controlled, double-blind, phase 3 trial.

Authors:  Lee S Schwartzberg; Manuel R Modiano; Bernardo L Rapoport; Martin R Chasen; Cesare Gridelli; Laszlo Urban; Allen Poma; Sujata Arora; Rudolph M Navari; Ian D Schnadig
Journal:  Lancet Oncol       Date:  2015-08-10       Impact factor: 41.316

2.  Safety and efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting after administration of cisplatin-based highly emetogenic chemotherapy in patients with cancer: two randomised, active-controlled, double-blind, phase 3 trials.

Authors:  Bernardo L Rapoport; Martin R Chasen; Cesare Gridelli; Laszlo Urban; Manuel R Modiano; Ian D Schnadig; Allen Poma; Sujata Arora; Vikram Kansra; Lee S Schwartzberg; Rudolph M Navari
Journal:  Lancet Oncol       Date:  2015-08-10       Impact factor: 41.316

3.  Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC).

Authors:  Bernardo Rapoport; Daniel Chua; Allen Poma; Sujata Arora; Yan Wang; Luis Enrique Fein
Journal:  Support Care Cancer       Date:  2015-05-05       Impact factor: 3.603

4.  Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets.

Authors:  Ruth A Duffy; Cynthia Morgan; Robert Naylor; Guy A Higgins; Geoffrey B Varty; Jean E Lachowicz; Eric M Parker
Journal:  Pharmacol Biochem Behav       Date:  2012-03-31       Impact factor: 3.533

Review 5.  Current pharmacotherapy for chemotherapy-induced nausea and vomiting in cancer patients.

Authors:  Michelle C Janelsins; Mohamedtaki A Tejani; Charles Kamen; Anita R Peoples; Karen M Mustian; Gary R Morrow
Journal:  Expert Opin Pharmacother       Date:  2013-04       Impact factor: 3.889
  5 in total
  3 in total

Review 1.  Rolapitant: A Review in Chemotherapy-Induced Nausea and Vomiting.

Authors:  Young-A Heo; Emma D Deeks
Journal:  Drugs       Date:  2017-10       Impact factor: 9.546

Review 2.  Management of Chemotherapy-Induced Nausea and Vomiting (CINV): A Short Review on the Role of Netupitant-Palonosetron (NEPA).

Authors:  Vito Lorusso; Anna Russo; Francesco Giotta; Paolo Codega
Journal:  Core Evid       Date:  2020-07-27

Review 3.  Management of chemotherapy-induced nausea and vomiting by risk profile: role of netupitant/palonosetron.

Authors:  Vito Lorusso
Journal:  Ther Clin Risk Manag       Date:  2016-06-07       Impact factor: 2.423
  3 in total

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