Collecting Drug-Drug Interaction Data on Rimegepant: Elyse Stock, MD


The chief medical officer of Biohaven Pharmaceuticals discussed the findings of an assessment of rimegepant (Nurtec ODT) exposure with concomitant administration of inhibitors of P-gp and BCRP transporters.

“Basically, what [the data] told us, is that we were able to tweeze out the effect that these strong inhibitors were having. What we saw—and what the takeaway is—is that with strong P-gp inhibition, like you see with cyclosporine and quinidine…you have a moderate increase in rimegepant exposure.”

Recently presented data at the 2021 American Headache Society (AHS) Annual Scientific Meeting, June 3-6, suggest that the exposure of rimegepant (Nurtec ODT; Biohaven) increases moderately when administered concomitantly with strong inhibitors of the P-glycoprotein (P-gp) transporter, and is impacted only minimally by the inhibition of the breast cancer resistance protein (BCRP) transporter. These data are clinically relevant for the migraine community, particularly in light of the recent May approval of rimegepant for the prevention of migraine, adding to its existing indication as an acute agent.

All told, the study was a single-center, open-label, randomized study in a planned total of 32 healthy subjects, conducted in 2 parts. Part 1 included a 2-period, 2-sequence, crossover study to evaluate the effect of cyclosporine (1 dose of 200 mg PO) on the pharmacokinetics of rimegepant 75 mg. Part 2 then followed with a 2-period, 2-sequence, crossover study to evaluate the effect of quinidine (1 dose of 600 mg PO) on the pharmacokinetics of the migraine therapy.

The data revealed that P-gp inhibitors—in this instance, cyclosporine and quinidine—increased rimegepant exposures by slightly more than 50% but less than 2-fold. This moderate effect, the authors noted, “may be generalizable to other strong P-gp inhibitors, such as amiodarone, carvedilol, dronedarone, lapatinib, propafenone, ranolazine, and verapamil.” Similarly, the results imply that BCRP inhibition has minimal influence on rimegepant exposure.

To find out more about the clinical implications of these data, as well as to gauge what the clinical community should know about the study and the possible further explorations of rimegepant’s drug-drug interactions, NeurologyLive spoke with Elyse Stock, MD, chief medical officer, Biohaven Pharmaceuticals.

For more coverage of AHS 2021, click here.

Bertz R, Anderson MS, Collins J, et al. Effect of Strong P-gp and BCRP Inhibition, Using Cyclosporine and Quinidine as Probes, on the Pharmacokinetics of Oral Rimegepant 75 mg in Healthy Subjects. Presented at 2021 AHS Annual Scientific Meeting; June 3-6. Abstract P222.
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