Ubrogepant, First Oral CGRP Receptor Antagonist or Gepant, Approved by FDA

American Headache Society shares breaking news regarding new treatments approved or cleared by the FDA.

On December 23, 2019, the FDA approved ubrogepant (UBRELVY™) for the acute treatment of migraine with or without aura in adults. This is the first oral CGRP receptor antagonist, or gepant, approved by the FDA.  

“With every FDA approval for a migraine-specific medication, our arsenal to fight this disease is rapidly expanding,” says Amaal Starling, MD, FAHS, assistant professor of neurology at the Mayo Clinic and member of the American Headache Society. “The FDA approval of ubrogepant is ground breaking because this is the first in class of oral CGRP antagonists approved for the treatment of migraine.” 

Four clinical studies (ACHIEVE I, ACHIEVE II, UBR-MD-04 and 3110-105-002) demonstrated the efficacy, safety and tolerability of orally-administered ubrogepant, followed by two pivotal Phase 3 clinical trials. Both 50 mg and 100 mg dose strengths demonstrated significantly greater rates of pain freedom and freedom from the most bothersome migraine-associated symptom (such as nausea, hypersensitivity to light, or hypersensitivity to sound) at two hours, compared with placebo.

Nausea was the most common adverse event reported in 1.7-4.1% of patients at various doses during the pivotal studies, compared to 1.6-2.0% of patients who received placebo. There were no serious adverse events within 48 hours of a dose. Additionally, the safety study (UBR-MD-04) reinforced the safety and tolerability of ubrogepant for both the 50 mg and 100 mg dose strengths. Research shows that ubrogepant was well tolerated with an adverse event profile similar to placebo, providing relief up to 24 hours.

CGRP is a protein known to be released during a migraine attack. Ubrogepant reduces CGRP activity, preventing CGRP from binding to its receptors. It works without constricting blood vessels unlike triptan medications. Additionally, ubrogepant is non-narcotic, not scheduled, and does not have addiction potential.

The efficacy, side effect profile, and low risk of medication overuse of this medication makes this an ideal option for patients with migraine for whom triptan medications don’t work, are poorly tolerated, or are contraindicated.

“Clinical trials have not only demonstrated efficacy of ubrogepant compared to placebo, but also there is no vasoconstriction of blood vessels unlike triptan medications. Given the mechanism of action, this is also an acute medication that does not have a risk of medication overuse unlike triptans or non-steroidal anti-inflammatory medications,” says Dr. Starling.

For more information about ubrogepant that can be used to inform treatment decisions, click here.

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