CGRP

Gepants for the treatment of migraine

Introduction: Migraine is the most common of all neurological disorders. A breakthrough in migraine treatment emerged in the early nineties with the introduction of 5-HT1B/D receptor agonists called triptans. Triptans are used as the standard of care for acute migraine; however, they have significant limitations such as incomplete and inconsistent pain relief, high rates of headache recurrence, class- specific side effects and cardiovascular contraindications.

Rimegepant. calcitonin gene-related peptide (CGRP) receptor antagonist, treatment of migraine

Rimegepant is an oral calcitonin gene-related peptide
(CGRP) receptor antagonist and is currently under
development by Biohaven Pharmaceuticals for the acute
and preventive treatment of migraine. Among patients
with acute migraine, significant clinical efficacy has been
reported with a rimegepant single dose. The completed
pivotal phase II and III trials showed a beneficial action of
rimegepant in terms of pain freedom, pain relief, release
of migraine symptoms and lifestyle recovery. Moreover,

Fremanezumab for the preventive treatment of migraine in adults

Introduction: The Calcitonin Gene-Related Peptide (CGRP) has been implicated in migraine pathophysiology due to its role in neurogenic inflammation and transmission of trigeminovascular nociceptive signal. New molecules targeting CGRP and its receptor have been developed as migraine-specific preventative treatments. Fremanezumab (or TEV-48,125, LBR-101), a human monoclonal antibody against CGRP, has been recently approved for clinical use by FDA and EMA.

Ubrogepant for the treatment of migraine

Introduction: Migraine is a neurovascular disorder involving neurogenic inflammation and transmission of trigeminovascular nociceptive pathways mediated by Calcitonin Gene-Related Peptide (CGRP). Several small molecules antagonizing the CGRP receptor have been developed as migraine-specific acute medications. The CGRP receptor antagonist ubrogepant, also known as MK-1602, has been recently evaluated in phase III clinical trials for clinical efficacy and long-term safety as an abortive migraine treatment.

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