• 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

UBRELVY is the first acute treatment for migraine that blocks CGRP5-7*

CGRP plays a key role in migraine attacks, binding to CGRP receptors to cause pain, inflammation, and vasodilation1,8-10

MIGRAINE PATHOPHYSIOLOGY CGRP is released, causing meningeal vessel expansion and pain signaling1,9,10

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 circulate1,3,9,10

BARBITURATES This class of drug acts by potentiating GABA-induced increase in chloride conductance. They enhance GABA binding to GABA A receptors11

NSAIDs The main effect of nonsteroidal anti-inflammatory drugs is the blockade of the enzyme cyclooxygenase (COX) receptors12

*CGRP=calcitonin gene-related peptide.

Watch the UBRELVY (ubrogepant)
mechanism of action

UBRELVY Pharmacokinetic profile

Within 11 minutes:
time to reach pharmacologically available concentration13†
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 near dose-proportional pharmacokinetics within the range of 40 to 400 mg.5

Based on the inhibition of human capsaicin-induced dermal vasodilation (CIDV) model, a pharmacodynamic measure of CGRP blockade, EC90=13 ng/mL.13

See the efficacy results

References

1. Durham PL. CGRP-receptor antagonists—a fresh approach to migraine therapy? N Engl J Med. 2004;350(11):1073-1075. 2. Goadsby PJ, Edvinsson L, Ekman R. Vasoactive peptide release in the extracerebral circulation of humans during migraine headache. Ann Neurol. 1990;28(2):183-187. 3. Benemei S, Cortese F, Labastida-Ramírez A, et al. Triptans and CGRP blockade—impact on the cranial vasculature. J Headache Pain. 2017;18(1):103. doi:10.1186/s10194-017-0811-5. 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.; 2019. 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 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. 9. 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. 10. 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. 11. Silberstein SD, McCrory CD. Butalbital in the treatment of headache: history, pharmacology, and efficacy. Headache. 2001;41(10):953-967. 12. 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. 13. 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: 60th Annual Scientific Meeting of the American Headache Society; June 28-July 1, 2018; San Francisco, CA. Poster P103.