Rimegepant (Nurtec ODT) now available for acute treatment of migraine

Pfizer is introducing Nurtec ODT (rimegepant 75 mg orally disintegrating tablets) for the acute treatment of migraine with or without aura in adults.1,2 Rimegepant is the second oral “gepant” for acute migraine to be marketed in Canada following ubrogepant tablets (Ubrelvy).3 A third oral gepant, atogepant (Qulipta), is available in tablet form for the prevention of episodic migraine (< 15 migraine days per month) in adults.4In the United States, Nurtec ODT is also approved for preventive treatment of episodic migraine. The recommended dosage is 75 mg orally every other day.5 This indication is not yet approved in Canada.1Rimegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist. It selectively binds with high affinity to human CGRP receptors and antagonizes CGRP receptor function. CGRP levels are elevated during a migraine attack and are associated with the release of vasoactive neuropeptides and vasodilation of the cerebral vasculature, which plays a role in the pathogenesis of migraine.1The recommended dosage of rimegepant for acute migraine is 75 mg, as needed, once daily. The maximum daily dose is 75 mg. No dosage adjustment is required in patients with mild, moderate or severe renal impairment, or in mild or moderate hepatic impairment, but the drug should be avoided in severe hepatic impairment. The safety of taking more than 15 doses in a 30-day period has not been established.1To administer rimegepant orally disintegrating tablets, instruct patients to use dry hands when opening the blister pack. After peeling back the foil covering of one blister, the tablet should be immediately placed on or under the tongue. The tablet will disintegrate in saliva so that it can be swallowed without additional liquid. Rimegepant tablets may be taken with or without food.1Nausea and dizziness are the most common adverse effects of rimegepant. Hypersensitivity reactions, including dyspnea and rash, occur in less than 1% of patients; these reactions may occur days after administration.1In terms of drug interactions, concomitant administration with strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, ritonavir) should be avoided. Caution is advised with moderate CYP3A4 inhibitors (e.g., diltiazem, erythromycin, fluconazole); when administered concomitantly with moderate CYP3A4 inhibitors, avoid taking another dose of rimegepant within 48 hours.1 Administration with strong CYP3A4 inducers (e.g., phenobarbital, rifampin, St John’s wort) or moderate CYP3A4 inducers (e.g., bosentan, efavirenz, modafinil) is not recommended. The effect of CYP3A4 induction may last for up to two weeks after discontinuation of the strong or moderate CYP3A4 inducer. A second dose of rimegepant should be avoided within 48 hours after concomitant administration with strong P-gp inhibitors (e.g., cyclosporine, verapamil, quinidine).1Medical Letter consultants note that an oral nonopioid analgesic (e.g., a nonsteroidal anti-inflammatory drug) may be sufficient for treatment of mild or moderate migraine headache without nausea or vomiting. An oral serotonin receptor agonist (“triptan”) such as sumatriptan is the drug of choice for treatment of moderate or severe migraine headache. About 30% of patients do not respond to an oral triptan, but these patients may respond to another triptan. Triptans are contraindicated for use in patients with vascular disease, as angina, myocardial infarction, cardiac arrhythmia and stroke have occurred rarely with triptan use.6,7Rimegepant and ubrogepant appear to have similar efficacy in acute migraine, but have not been directly compared to each other, or to triptans, in clinical studies. In clinical trials, about 10% more patients were headache-free two hours post-dose with rimegepant or ubrogepant compared to placebo. Both drugs begin to reduce migraine pain within 60 minutes. Rimegepant has as longer half-life (~11 hours) than ubrogepant (5–7 hours).6,7 An analysis of pooled data from three phase 3 clinical trials evaluated the efficacy of rimegepant versus placebo in the acute treatment of migraine based on patients’ historical and current experience with triptans. Results showed that rimegepant was effective in the acute treatment of migraine in participants with a history of an insufficient response to one triptan, or two or more triptans, as well as in current triptan users.8 Overall, oral CGRP receptor antagonists appear to be less effective than triptans in acute migraine, but they can be used in patients with vascular disease and do not appear to cause medication overuse headache.6,7,9 Triptan use for ≥ 10 days per month can lead to medication overuse headache.7ReferencesPfizer Canada ULC. Nurtec ODT (rimegepant orally disintegrating tablets) product monograph. Kirkland, QC; December 1, 2023. (accessed April 11, 2024).Pfizer Canada Inc. Nurtec ODT is now available in Canada for the treatment of acute migraine. Kirkland, QC; April 4, 2024. (accessed April 11, 2024). AbbVie Corp. Ubrelvy (ubrogepant tablets) product monograph. Saint-Laurent, QC; November 10, 2022. (accessed April 11, 2024).AbbVie Corp. Qulipta (atogepant tablets) product monograph. Saint-Laurent, QC; December 21, 2022. (accessed April 11, 2024). Pfizer Laboratories. Nurtec ODT (rimegepant sulfate tablet, orally disintegrating) prescribing information. New York, NY; February 2024. (accessed April 11, 2024).Anon. Rimegepant (Nurtec ODT) for acute treatment of migraine. Med Lett Drugs Ther 2020; 62:70-2. Anon. Drugs for migraine. Med Lett Drugs Ther 2024;65;89-96.Lipton RB, Blumenfeld A, Jensen CM, et al. Efficacy of rimegepant for the acute treatment of migraine based on triptan treatment experience: pooled results from three phase 3 randomized clinical trials. Cephalalgia 2023;43(2). (accessed April 11, 2024). Yang CP, Liang CS, Chang CM, et al. Comparison of new pharmacologic agents with triptans for treatment of migraine: a systematic review and meta-analysis. JAMA Netw Open 2021 Oct 1;4(10):e2128544. (accessed April 11, 2024).

Rimegepant (Nurtec ODT) now available for acute treatment of migraine

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