Skip to main content
SpringerLink
Log in

Rolapitant: A Review in Chemotherapy-Induced Nausea and Vomiting

  • Adis Drug Evaluation
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

Oral rolapitant (Varubi™; Varuby®), a long-acting neurokinin-1 (NK1) receptor antagonist (RA), is indicated in the USA and EU as part of an antiemetic regimen to prevent delayed chemotherapy-induced nausea and vomiting (CINV) in adults receiving highly or moderately emetogenic chemotherapy (HEC or MEC). In randomized, phase III trials, a single oral dose of rolapitant 180 mg was effective in preventing delayed CINV compared with placebo, when each was used in combination with a 5-HT3 RA plus dexamethasone, in adults receiving their first course of HEC or MEC. The benefits of rolapitant were maintained over multiple cycles of chemotherapy. The tolerability profile of rolapitant is similar to that of placebo and consistent with that of other NK1 RAs. However, rolapitant differs from other existing NK1 RAs in that it does not interact with CYP3A4, thereby negating the need for dexamethasone dose adjustments and potentially making rolapitant a more suitable option for patients receiving CYP3A4 substrates. Thus, oral rolapitant is an effective and well tolerated NK1 RA that expands the treatment options for preventing delayed CINV in adults receiving HEC or MEC.

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. Rapoport BL. Delayed chemotherapy-induced nausea and vomiting: pathogenesis, incidence, and current management. Front Pharmacol. 2017. doi:10.3389/fphar.2017.00019.

  2. Jordan K, Jahn F, Aapro M. Recent developments in the prevention of chemotherapy-induced nausea and vomiting (CINV): a comprehensive review. Ann Oncol. 2015;26(6):1081–90.

    Article  CAS  PubMed  Google Scholar 

  3. Syed YY. Rolapitant: first global approval. Drugs. 2015;75(16):1941–5.

    Article  CAS  PubMed  Google Scholar 

  4. TESARO Inc. VARUBI™ (rolapitant) tablets, for oral use. 2015. http://varubirx.com/. Accessed 5 Jul 2017.

  5. EMA. Varuby: summary of product characteristics. 2017. http://ec.europa.eu/health/. Accessed 5 Jul 2017.

  6. Duffy RA, 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 

  7. Wang X, Zhang ZY, Powers D, et al. Rolapitant absolute bioavailability and PET imaging studies in healthy adult volunteers. Clin Pharmacol Ther. 2017. doi:10.1002/cpt.637.

    Google Scholar 

  8. Wang X, Zhang Z, Powers D, et al. Lack of effect of rolapitant, a cancer supportive care antiemetic, on QTc intervals in healthy subjects [abstract no. E-031]. Clin Pharmacol Ther. 2016;99(Suppl. 1):S28.

    Google Scholar 

  9. 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 

  10. 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 

  11. National Comprehensive Cancer Network. Antiemesis (NCCN Clinical Practice Guidelines in Oncology). 2017. https://www.nccn.org/. Accessed 5 Jul 2017.

  12. Chasen M, Urban L, Schnadig I, et al. Rolapitant improves quality of life of patients receiving highly or moderately emetogenic chemotherapy. Support Care Cancer. 2017;25(1):85–92.

    Article  PubMed  Google Scholar 

  13. EMA. Varuby: EPAR-public assessment report 2017. http://www.ema.europa.eu/. Accessed 5 Jul 2017.

  14. Navari R, Nagy CK, Arora S, et al. Rolapitant for the prevention of nausea in patients receiving moderately or highly emetogenic chemotherapy [abstract no. 224]. J Clin Oncol. 2016;34(Suppl 26):224.

    Article  Google Scholar 

  15. Hesketh PJ, Schnadig ID, Schwartzberg LS, et al. Efficacy of the neurokinin-1 receptor antagonist rolapitant in preventing nausea and vomiting in patients receiving carboplatin-based chemotherapy. Cancer. 2016;122(15):2418–25.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  16. Navari R, Nagy C, Rapoport BL, et al. Rolapitant for the prevention of nausea in patients receiving cisplatin- or carboplatin based chemotherapy: alternative methods for evaluating nausea [abstract no. eP017]. Support Care Cancer. 2017;25(Suppl 2):S69.

    Google Scholar 

  17. Rapoport BL, Schwartzberg LS, Arora S, et al. Rolapitant for control of chemotherapy-induced nausea and vomiting (CINV) in patients with gynecologic cancer [abstract no. 10122]. J Clinic Oncol. 2016;34(Suppl. 26):223.

    Article  Google Scholar 

  18. Schwartzberg L, Navari R, Arora S, et al. Rolapitant for the prevention of chemotherapy-induced nausea and vomiting in breast cancer patients receiving multiple cycles of emetogenic chemotherapy [abstract no. P5-11-15]. Cancer Res. 2017;77(4 Suppl.).

  19. Navari R, Rapoport B, Arora S, et al. Rolapitant for control of chemotherapy induced nausea and vomiting (CINV) in patients with lung cancer [abstract no. PS084]. Support Care Cancer. 2016;24(Suppl 1):S51.

    Google Scholar 

  20. Navari R, Jordan K, Rapoport BL, et al. Efficacy of rolapitant for prevention of chemotherapy-induced nausea and vomiting (CINV) in patients with gastrointestinal and colorectal cancers [abstract no. 1440P]. Ann Oncol. 2016;27(Suppl. 6).

  21. Aapro M, Powers D, Arora S. Efficacy and safety of rolapitant in the prevention of chemotherapy-induced nausea and vomiting in patients aged <65 versus ≥65 years receiving multiple cycles of emetogenic chemotherapy [abstract no. P059]. J Geriatr Oncol. 2016;7/6(Suppl 1):S70.

  22. Rapoport B, Schwartzberg L, Chasen M, et al. Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy. Eur J Cancer. 2016;57:23–30.

    Article  CAS  PubMed  Google Scholar 

  23. 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;23(11):3281–8.

    Article  PubMed  Google Scholar 

  24. Barbour S, Smit T, Wang X, et al. Integrated safety analysis of rolapitant with coadministered drugs from phase II/III trials: an assessment of CYP2D6 or BCRP inhibition by rolapitant. Ann Oncol. 2017;28(6):1268–73

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  25. Herrstedt J, Roila F, Warr D, et al. 2016 Updated MASCC/ESMO consensus recommendations: prevention of nausea and vomiting following high emetic risk chemotherapy. Support Care Cancer. 2017;25(1):277–88.

    Article  PubMed  Google Scholar 

  26. Roila F, Warr D, Hesketh PJ, et al. 2016 updated MASCC/ESMO consensus recommendations: prevention of nausea and vomiting following moderately emetogenic chemotherapy. Support Care Cancer. 2017;25(1):289–94.

    Article  PubMed  Google Scholar 

  27. Rashad N, Abdel-Rahman O. Differential clinical pharmacology of rolapitant in delayed chemotherapy-induced nausea and vomiting (CINV). Drug Des Devel Ther. 2017;11:947–54.

    Article  PubMed  PubMed Central  Google Scholar 

  28. Abdel-Rahman O. Neurokinin-1 inhibitors in the prevention of nausea and vomiting from highly emetogenic chemotherapy: a network meta-analysis. Ther Adv Med Oncol. 2016;8(5):396–406.

    Article  PubMed  PubMed Central  Google Scholar 

  29. Harrow B, Sheinin M, German A, et al. Adoption of rolapitant, a novel NK-1 receptor antagonist for chemotherapy-induced nausea and vomiting (CINV), has a negligible budget impact for a typical US health plan [abstract no. C01]. In: AMCP Managed Care and Specialty Pharmacy Annual Meeting. 2016.

Download references

Acknowledgements

During the peer review process, the manufacturer of rolapitant was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

Author information

Authors and Affiliations

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

    Young-A Heo & Emma D. Deeks

Authors
  1. Young-A Heo
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Emma D. Deeks
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Young-A Heo.

Ethics declarations

Funding

The preparation of this review was not supported by any external funding.

Conflict of interest

Young-A Heo and Emma Deeks are salaried employees of Adis/Springer, are responsible for the article content and declare no relevant conflicts of interest.

Additional information about this Adis Drug Review can be found at http://www.medengine.com/Redeem/5ED8F0606A685C8C.

Additional information

The manuscript was reviewed by: J. Kolesar, Department of Pharmacy Practice & Science, University of Kentucky, Lexington, KY, USA; M. Markman, Eastern Regional Medical Center, Cancer Treatment Centers of America, Philadelphia, PA, USA; R. M. Navari, Division of Hematology Oncology, University of Alabama Birmingham School of Medicine, Birmingham, AL, USA; I. N. Olver, Sansom Institute for Health Research, University of South Australia, Adelaide, Australia.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Heo, YA., Deeks, E.D. Rolapitant: A Review in Chemotherapy-Induced Nausea and Vomiting. Drugs 77, 1687–1694 (2017). https://doi.org/10.1007/s40265-017-0816-z

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40265-017-0816-z

Search

Navigation