Rimegepant: Treatment for Acute Migraine

Robert Cowan, MD, FAAN: Rimegepant is a very interesting molecule. The reason I say that is because while it is a unique agent in that it’s a CGRP antagonist unrelated to the triptans, it also has some very interesting features in that its adverse-effect profile is minimal. There are very few adverse effects associated with it. What makes it interesting to me is, based on long-term data, there is no medication overuse phenomenon. 

The medication overuse phenomenon is something we see when people take acute medication too often. What happens is the brain quickly starts to think that the medication is part of its normal chemistry, and when you don’t take it, your brain tells you there’s something wrong. The way it says that, of course, is with pain. We always have to limit how often a patient takes a triptan, for example, to no more than 10 days out of the month, which is roughly 2 days a week. That’s fine if you only have 1 or 2 headaches a week. But if you have 3 or 4 headaches a week, you’re in a very difficult position. The nice thing about rimegepant is that in its long-term data, there was no evidence that using the medication more often results in more migraine. In fact, they looked at every-other-day usage with the option of additional rescue and found that there was no escalation in headache frequency, severity, or duration with increased use of the medication. That’s very appealing.

The dosing of rimegepant is 75 mg, and it’s a pill you put under your tongue. It’s used once per day for the acute treatment of migraine. As with other acute treatments, there is no titration necessary. The 75-mg dose is the only dose available. 

Rimegepant is very well tolerated, and while its half-life is on the order of 8 to 12 hours, it seems to show a beneficial effect over 24 to 48 hours. That makes the recurrence of 1 headache less of an issue than it might be with a medication that has a shorter half-life.

As I mentioned earlier, we’re looking increasingly at most bothersome symptom as an important measure of the tolerability and efficacy of these medications. Rimegepant was able to differentiate at 2 hours, which was a secondary end point in the study, with respect to most bothersome symptoms.

One of the nice features of the CGRP antagonists in general is that they are very well tolerated and have very few drug interactions. They appear to be safe in combination with oral contraceptives and are very well tolerated.