Skip to main content
SpringerLink
Log in

Rolapitant: First Global Approval

  • AdisInsight Report
  • Published:
Drugs Aims and scope Submit manuscript

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. Janelsins MC, Tejani MA, Kamen C, et al. Current pharmacotherapy for chemotherapy-induced nausea and vomiting in cancer patients. Expert Opin Pharmacother. 2013;14(6):757–66.

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  2. National Comprehensive Cancer Network. NCCN clinical practice guidelines in oncology (NCCN Guidelines®): antiemesis, version I.2015. 2015. http://www.nccn.org. Accessed 22 Sep 2015.

  3. Duffy R, Morgan C, Naylor R, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012;102(1):95–100.

    Article  CAS  PubMed  Google Scholar 

  4. TESARO. Varubi™ (rolapitant) tablets, for oral use: US prescribing information. 2015. http://varubirx.com. Accessed 4 Sep 2015.

  5. US FDA. FDA approves new drug treatment for nausea and vomiting from chemotherapy [media release]. 2 Sep 2015. http://www.fda.gov.

  6. Rapoport BL, Chasen MR, Gridelli C, et al. 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. Lancet Oncol. 2015;16(9):1079–89.

    Article  CAS  PubMed  Google Scholar 

  7. Schwartzberg LS, Modiano MR, Rapoport BL, et al. 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. Lancet Oncol. 2015;16(9):1071–8.

    Article  CAS  PubMed  Google Scholar 

  8. OPKO Health. OPKO Health completes acquisition of NK-1 compounds from Schering Corporation [media release]. 11 Nov 2009. http://www.opko.com.

  9. TESARO. TESARO and OPKO Health sign exclusive license agreement for rolapitant [media release]. 14 Dec 2010. http://www.tesarobio.com.

  10. TESARO. Tesaro and Jiangsu Hengrui Medicine announce rolapitant license agreement for China [media release]. 30 Jul 2015. http://www.tesarobio.com.

  11. Poma A, Christensen J, Davis J, et al. Phase 1 positron emission tomography (PET) study of the receptor occupancy of rolapitant, a novel NK-1 receptor antagonist [abstract no. e20690]. J Clin Oncol. 2014;32(15 Suppl 1).

  12. Poma A, Christensen JC, Pentikis HP, et al. Rolapitant and its major metabolite do not affect the pharmacokinetics of midazolam, a sensitive cytochrome P450 3A4 substrate [abstract no. MASCC-0441]. Support Care Cancer. 2013;21(Suppl 1):S154.

    Google Scholar 

  13. Rapoport B, Chua D, Poma A, et al. 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). Support Care Cancer. 2015. doi:10.1007/s00520-015-2738-1.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand

    Yahiya Y. Syed

Authors
  1. Yahiya Y. Syed
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Yahiya Y. Syed.

Ethics declarations

Disclosure

The preparation of this review was not supported by any external funding. During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. Y. Y. Syed is a salaried employee of Adis, Springer SBM.

Additional information

This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Syed, Y.Y. Rolapitant: First Global Approval. Drugs 75, 1941–1945 (2015). https://doi.org/10.1007/s40265-015-0485-8

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-015-0485-8

Keywords

Search

Navigation