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Rimegepant: First Approval

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Abstract

The orally disintegrating tablet (ODT) formulation of rimegepant (NURTEC ODT®) is a small molecule, highly-selective, calcitonin gene-related peptide antagonist that was developed by Biohaven Pharmaceutical Holding Company Ltd as an acute treatment for migraine. A conventional tablet formulation of the drug is being investigated for the acute treatment (under FDA review in the USA) and prevention of migraine and the treatment of refractory trigeminal neuralgia. In February 2020, rimegepant ODT received its first global approval in the USA for the acute treatment of migraine (± aura) in adults. This article summarizes the milestones in the development of rimegepant leading to its first global approval for acute treatment of migraine (± aura) in adults.

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References

  1. Goadsby PJ. Primary headache disorders: five new things. Neurol Clin Pract. 2019;9(3):233–40.

    Article  Google Scholar 

  2. Chan C, Goadsby PJ. Recent advances in pharmacotherapy for episodic migraine. CNS Drugs. 2019;33(11):1053–71.

    Article  CAS  Google Scholar 

  3. Edvinsson L, Haanes KA, Warfvinge K, et al. CGRP as the target of new migraine therapies: successful translation from bench to clinic. Nat Rev Neurol. 2018;14(6):338–50.

    Article  CAS  Google Scholar 

  4. Edvinsson L. Rimegepant oral disintegrating tablet for migraine. Lancet. 2019;394(10200):711–2.

    Article  Google Scholar 

  5. US FDA. NURTEC ODT (rimegepant): NDA approval letter. 2020. https://www.fda.gov/. Accessed 2020.

  6. Biohaven Pharmaceuticals. NURTEC ODT (rimegepant) orally disintegrating tablets, for sublingual or oral use: US prescribing information. 2020. https://www.fda.gov/. Accessed 02 Mar 2020.

  7. Biohaven Pharmaceutical Holding Company. Biohaven Pharmaceuticals reports first quarter 2017 financial and business results [media release]. 16 Jul 2017. https://www.biohavenpharma.com.

  8. Biohaven Pharmaceutical Holding Company. Biohaven announces exclusive license with Catalent for Zydis® orally dissolving tablet with small molecule CGRP receptor antagonists [media release]. 21 Feb 2018. https://www.biohavenpharma.com.

  9. Biohaven Pharmaceutical Holding Company. Biohaven announces formation of BioShin, a wholly owned Asia-Pacific subsidiary [media release]. 28 Nov 2018. https://www.biohavenpharma.com.

  10. Tong G, Savant I, Jariwala N, et al. Phase I single and multiple dose study to evaluate the safety, tolerability, and pharmacokinetics of BMS-927711 in healthy subjects [poster]. J Headache Pain. 2012;14(Suppl 1):P118.

    Article  Google Scholar 

  11. Conway CM, Dubowchik GM, Croop R, et al. Phase 1 safety, tolerability and pharmacokinetics of single and multiple dose rimegepant as compared to the predicted clinically efficacious dose range [abstract no. P280LB plus poster]. Headache. 2019;59(1):206.

    Google Scholar 

  12. Conway CM, Dubowchik GM, Coric V. Rimegepant and BHV-3500, small molecule CGRP receptor antagonists, exhibit no active vasoconstrictive properties in ex vivo human coronary or cerebral arteries [abstract no. LBOR-08]. Headache. 2018;58(8):1295.

    Google Scholar 

  13. Conway CM, Croop R, Dubowchik GM, et al. Cardiovascular safety of rimegepant 75 mg in 3 randomized clinical trials and systematic evaluations from in vitro, ex vivo and in vivo nonclinical assays [abstract no. IHC-PO-365 plus poster]. Cephalalgia. 2019;39(1 Supp):200–1.

    Google Scholar 

  14. Croop R, Ivans A, Stock D, et al. A phase 1 study to evaluate the bioequivalence of oral tablet and orally dissolving tablet formulations of rimegepant in healthy adult subjects under fasting conditions [abstract no. PF116LB plus poster]. Headache. 2018;58(8):1303–4.

    Google Scholar 

  15. Croop R, Stringfellow J, Ivans A, et al. Rimegepant 75 mg exposure, safety, and tolerability are similar in elderly and nonelderly adults: a phase 1, open-label, parallel-group, single-dose study [abstract no. IHC-DP-021]. Cephalalgia. 2019;39(1):30.

    Google Scholar 

  16. Croop R, Stringfellow J, Ivans A, et al. Results of a phase 1, open-label, single-dose, parallel-group study of rimegepant 75 mg in subjects with hepatic impairment [abstract no. IHC-PO-364]. Cephalalgia. 2019;39(1):200.

    Google Scholar 

  17. Croop R, Goadsby PJ, Stock DA, et al. Efficacy, safety, and tolerability of rimegepant orally disintegrating tablet for the acute treatment of migraine: a randomised, phase 3, double-blind, placebo-controlled trial. Lancet. 2019;394:737–45.

    Article  CAS  Google Scholar 

  18. Marcus R, Goadsby PJ, Dodick D, et al. BMS-927711 for the acute treatment of migraine: a double-blind, randomized, placebo controlled, dose-ranging trial. Cephalalgia. 2014;34(2):114–25.

    Article  Google Scholar 

  19. Lipton RB, Croop R, Stock EG, et al. Rimegepant, an oral calcitonin gene-related peptide receptor antagonist, for migraine. N Engl J Med. 2019;381(2):142–9.

    Article  CAS  Google Scholar 

  20. Lipton RB, Conway CM, Stock EG, et al. Efficacy, safety, and tolerability of rimegepant 75 Mg, an oral CGRP receptor antagonist, for the acute treatment of migraine: results from a double-blind, randomized, placebo-controlled trial, study 301 [abstract no. PS123LB plus poster]. Headache. 2018;58(8):1336–7.

    Google Scholar 

  21. Blumenfeld AM, Buse D, Turner IM, et al. Rimegepant 75 mg is more effective than nonsteroidal anti-inflammatory drugs for the acute treatment of migraine: post hoc analysis of data from 2 phase 3 trials [abstract no. P246LB plus poster]. Headache. 2019;59(Suppl 1):182–3.

    Google Scholar 

  22. Lipton RB, Berman G, Kudrow D, et al. Long-term, open-label safety study of rimegepant 75 mg for the treatment of migraine (study 201): interim analysis of safety and exploratory efficacy [abstract no. P235LB plus poster]. Headache. 2019;59(Suppl 1):175.

    Google Scholar 

  23. Litalien G, Croop R, Stock E, et al. Acute treatment with rimegepant 75mg confers clinically relevant improvement in migraine-related disability: results from a one year, open-label safety study (BHV3000–201) [abstract no. IHC-OR-041 plus oral presentation]. Cephalalgia. 2019;39(1 Suppl):363.

    Google Scholar 

  24. Litalien G, Croop R, Stock E, et al. Acute migraine treatment with rimegepant 75 mg and health related quality of life in migraine: results from a long-term, open-label safety study (BHV-3000–201) [abstract no. IHC-LB-023 plus poster]. Cephalalgia. 2019;39(1 Suppl):393.

    Google Scholar 

  25. Pavlovic J, Dodick DW, Newman L, et al. A single dose of rimegepant demonstrates sustained efficacy and low rescue medication use in the acute treatment of migraine: results from 3 phase 3 trials [abstract no. P244LB plus poster]. Headache. 2019;59(Suppl 1):180–1.

    Google Scholar 

  26. Lipton RB, Tepper SJ, Friedman DI, et al. A single dose of rimegepant 75 mg provides pain relief and return to normal function: Results from 3 phase 3 trials in adults with migraine [abstract no. IHC-PO-135 plus poster]. Cephalalgia. 2019;39(1 Suppl):195.

    Google Scholar 

  27. Croop R, Coric V, Stock EG, et al. Rimegepant 75 mg demonstrates superiority to placebo on nausea freedom: results from a post hoc pooled analysis of 3 phase 3 trials in the acute treatment of migraine [P41 plus poster]. Headache. 2019;59(Suppl 1):51–2.

    Google Scholar 

  28. Buse D, Blumenfeld AM, Lipton RB, et al. Rimegepant 75 mg is effective for the acute treatment of migraine regardless of attack frequency: results from 3 phase 3 trials [abstract no. P236LB plus poster]. Headache. 2019;59(Suppl 1):175–6.

    Google Scholar 

  29. Dodick DW, Pavlovic J, Newman L, et al. Rimegepant is effective for the acute treatment of migraine in subjects taking concurrent preventive medication: results from 3 phase 3 trials [abstract no. P239LB plus poster]. Headache. 2019;59(Suppl 1):177.

    Google Scholar 

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    Lesley J. Scott

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  1. Lesley J. Scott
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Correspondence to Lesley J. Scott.

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

Conflict of interest

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 authors on the basis of scientific completeness and accuracy. Lesley Scott is a salaried employee of Adis International Ltd/Springer Nature, is responsible for the article content and declares no relevant conflicts of interest.

Additional information

Enhanced material for this AdisInsight Report can be found at https://doi.org/10.6084/m9.figshare.11987334.

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.

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Scott, L.J. Rimegepant: First Approval. Drugs 80, 741–746 (2020). https://doi.org/10.1007/s40265-020-01301-3

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