Oral CGRP Shows Promising Results

Migraine is a complex neurological disorder, and in the U.S., migraine affects 39 million people, including children.1 Effective treatments are important to restore quality of life, address pain and discomfort, and relieve symptoms that go beyond a headache.

For decades, there have been few treatment advances for migraine, but that changed dramatically in 2018 with the introduction of a new class of drugs targeting the CGRP receptor. To date, the FDA has approved these drugs for the prevention of migraine. A new study evaluates another CGRP-receptor antagonist drug, rimegepant, and shows encouraging results for acute treatment of migraine, or as an “abortive” medication.

What is CGRP?

CGRP stands for calcitonin gene-related peptide. It is a vasoactive peptide, which means it affects the diameter of blood vessels, and it is involved in the dilation of cerebral and dural blood vessels.2 During a migraine or cluster headache, CGRP levels increase.2 By developing drugs that modulate CGRP responses, it is believed that migraine and cluster headache symptoms may be better controlled.

What did the studies show?

Rimegepant has been tested in 3 different phase III clinical trials to date. In each study, people were given either rimegepant or placebo. To be included in the trials, people had at least a one-year history of migraine, with 2-8 moderate to severe migraines a month.3 People in the studies received either 75mg of rimegepant or a placebo for a migraine, and the two main items being assessed were: freedom from pain, and freedom from the most bothersome migraine symptom other than pain.3 Both were self-reported by the participant 2 hours after the treatment was given.

Overall, the percentage of patients who were pain-free 2 hours after dosing was 19.6 percent in the rimegepant group, and 12.0 percent in the placebo group.3 The percentage of those free from their most bothersome symptom aside from pain 2 hours after dosing was 37.6 percent in the rimegepant group and 25.2 percent in the placebo group.3

These results are extremely promising and show rimegepant’s effectiveness compared to placebo in treating pain and other migraine symptoms.

What is rimegepant?

Rimegepant is a drug in a class known as gepants.4 Gepants target CGRP receptors, helping to relieve pain during migraines by blocking the CGRP pathway.4 Rimegepant is a pill taken orally, and since it is still an investigative medication, the full drug profile is not available. The most common side effects seen during the trials were nausea and urinary tract infection.4 As more studies are done on this drug, there is the possibility that more adverse effects will become apparent.

Why does this matter?

This new class of drugs is important since many people with migraine are treated with triptan drugs like rizatriptan, eletriptan, or sumatriptan. Since the early 1990’s, triptan drugs have been the most common treatment for migraines, slowing or stopping acute attacks by stimulating serotonin receptors, reducing inflammation and constricting blood vessels.4 However, triptans provide inconsistent and incomplete pain relief. Some people don’t tolerate these drugs, and those with cardiovascular disease or major risk factors for cardiovascular disease shouldn’t take those medications because of the effects on blood vessels.

Given the limitations of triptans, having a new class of drugs developed specifically for migraine is important. For those living with migraine, gepants or anti-CGRP drugs, bring the possibility of expanded migraine treatment options. Since 2018, several anti-CGRP drugs have been approved for the prevention of migraine. While more studies need to be done on rimegepant, these results are promising. Having a drug that uses the CGRP pathway to provide relief for acute migraine would be an important new option.

When will rimegepant be available?

It is widely believed that the FDA will make a decision on rimegepant in late 2019 or early 2020. Talk with your doctor about what they know about this potential future treatment, and whether it might be an option for you if or when it receives approval from the FDA.

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This article represents the opinions, thoughts, and experiences of the author; none of this content has been paid for by any advertiser. The Migraine.com team does not recommend or endorse any products or treatments discussed herein. Learn more about how we maintain editorial integrity here.

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