Other meanings of Ubrogepant
Pharmacology
Ubrogepant, sold under the brand name Ubrelvy, is a small-molecule medication used for the acute treatment of migraine with or without aura in adults. It belongs to the class of drugs known as gepants, which target the calcitonin gene-related peptide (CGRP) receptor. Approved by the U.S. Food and Drug Administration in December 2019, ubrogepant was the first oral CGRP receptor antagonist developed specifically for acute migraine, offering an alternative to triptans for patients who do not respond to or cannot tolerate those agents.
Ubrogepant is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor, a G protein-coupled receptor located on trigeminal neurons and cerebral vasculature. During a migraine attack, CGRP levels rise, causing vasodilation and neurogenic inflammation; ubrogepant blocks this signaling, thereby alleviating pain and associated symptoms without causing vasoconstriction, unlike triptans.1 The drug has a high oral bioavailability and a half-life of approximately 5–7 hours, allowing once-daily dosing as needed. It is metabolized primarily by CYP3A4, and co-administration with strong CYP3A4 inhibitors can increase plasma concentrations, requiring dose adjustments.2
In two pivotal phase 3 trials (ACHIEVE I and II), ubrogepant 50 mg and 100 mg demonstrated superior pain freedom and freedom from most bothersome symptoms (nausea, photophobia, or phonophobia) at two hours compared with placebo.3 The onset of meaningful relief occurred in a median of 1.5 hours, with sustained effects for up to 48 hours. Common adverse events include nausea, somnolence, and dry mouth, but the drug has a favorable cardiovascular profile, as it does not constrict blood vessels. However, it is contraindicated with strong CYP3A4 inhibitors and should be avoided during pregnancy due to potential fetal risk.4
Ubrogepant was developed by Allergan (now AbbVie) and received FDA approval on December 23, 2019, making it the first oral gepant for acute migraine treatment. It is available in 50 mg and 100 mg tablets, with a maximum recommended dose of 200 mg in 24 hours. Unlike triptans, which are contraindicated in patients with cardiovascular disease, ubrogepant can be used in such patients, offering a safer option. It is also approved in several other countries, including Canada and Australia, and is included in clinical guidelines as a first-line acute therapy for migraine.
Ubrogepant has been studied for potential preventive use in episodic migraine, though it is not currently approved for that indication.5 It also shows promise in treating migraine in patients with medication-overuse headache, as it does not interact with opioid receptors. A notable edge case: ubrogepant is not effective for cluster headaches, which involve different pathophysiological mechanisms. Additionally, its interaction with BCRP inhibitors can alter its absorption, and it may cause transient liver enzyme elevations in rare cases.6 The drug's development involved a unique patient-reported outcome measure, the Migraine Interictal Burden Scale, to assess quality of life between attacks.
Ubrogepant represents a significant advance in migraine therapy, offering a non-vasoconstrictive option with rapid onset and favorable safety profile.
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