- While research into the exact mechanism that causes migraine is ongoing, CGRP is known to play a role in migraine pain2
- CGRP acts at multiple sites along the trigeminovascular pathway, causing vasodilation, inflammation, and pain3
CGRP=calcitonin gene-related peptide.
UBRELVY is the first acute treatment for migraine that directly blocks CGRP5-7
CGRP plays a key role in migraine attacks, binding to CGRP receptors to cause pain, inflammation, and vasodilation1,2,8,9
UBRELVY works differently than older acute migraine treatments—see how each works against migraine2,5,8
MIGRAINE PATHOPHYSIOLOGY CGRP is released, causing meningeal vessel expansion and pain signaling1,2,9
UBRELVY Targets the CGRP receptor itself, blocking CGRP from attaching5
TRIPTANS 5HT1B/1D agonists that constrict blood vessels and prevent release of neuropeptides; those already released continue to circulate1-3,9
BARBITURATES This class of drug acts by potentiating GABA-induced increases in chloride conductance. They enhance GABA binding to GABA A receptors10
NSAIDs The main effect of nonsteroidal anti-inflammatory drugs is the blockade of cyclooxygenase (COX) receptors11
- Within 11 minutes:
- time to reach pharmacologically available concentration12*
- 12 hours:
- active concentration is maintained6
- 1.5 hours:
- time to peak plasma concentrations (Tmax)5
- 5-7 hours:
- elimination half-life5
The clinical significance of these data is not known.
UBRELVY displays dose-proportional pharmacokinetics within the recommended dose range.5
*Based on the inhibition of human capsaicin-induced dermal vasodilation model, a pharmacodynamic measure of CGRP blockade, EC90=13 ng/mL.12
1. Durham PL. CGRP-receptor antagonists—a fresh approach to migraine therapy? N Engl J Med. 2004;350(11):1073-1075. 2. Edvinsson L, Haanes KA, Warfvinge K, Krause DN. CGRP as the target of new migraine therapies—successful translation from bench to clinic. Nat Rev Neurol. 2018;14(6):338-350. 3. Benemei S, Cortese F, Labastida-Ramírez A, et al; School of Advanced Studies of the European Headache Federation (EHF-SAS). Triptans and CGRP blockade—impact on the cranial vasculature. J Headache Pain. 2017;18(1):103. 4. Schuster NM, Rapoport AM. New strategies for the treatment and prevention of primary headache disorders. Nat Rev Neurol. 2016;12(11):635-650. 5. UBRELVY [package insert]. Madison, NJ: Allergan USA, Inc.; 2021. 6. Data on file. Allergan. 7. Voss T, Lipton RB, Dodick DW, et al. A phase IIb randomized, double-blind, placebo-controlled trial of ubrogepant for the acute treatment of migraine. Cephalalgia. 2016;36(9):887-898. 8. Dodick DW, Lipton RB, Ailani J, et al. Ubrogepant for the treatment of migraine. N Engl J Med. 2019;381(23):2230-2241. 9. Goadsby PJ, Holland PR, Martins-Oliveira M, Hoffmann J, Schankin C, Akerman S. Pathophysiology of migraine: a disorder of sensory processing. Physiol Rev. 2017;97(2):553-622. 10. Silberstein SD, McCrory DC. Butalbital in the treatment of headache: history, pharmacology, and efficacy. Headache. 2001;41(10):953-967. 11. Pardutz A, Schoenen J. NSAIDs in the acute treatment of migraine: a review of clinical and experimental data. Pharmaceuticals (Basel). 2010;3(6):1966-1987. 12. Dodick DW, Goadsby PJ, Lu K, Jakata A, Szegedi A, Trugman JM. Ubrogepant achieves early pain relief for the acute treatment of migraine. Poster presented at: 61st Annual Scientific Meeting of the American Headache Society; July 11-14, 2019; Philadelphia, PA. Poster P103.