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Drugs of Today 2020-Jul

Ubrogepant to treat migraine

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A Dhir

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Migraine is the primary headache disorder affecting a significant population worldwide. Ubrogepant is an orally bioavailable calcitonin gene-related peptide (CGRP) receptor antagonist (gepant) approved by the U.S. Food and Drug Administration (FDA) for the acute treatment of migraine headaches with or without aura in adults. Ubrogepant is the first oral CGRP receptor antagonist approved for the acute treatment of migraine. CGRP is an important key mediator of migraine pain; CGRP levels have been shown to be significantly higher during a migraine attack. Two pivotal phase III clinical trials (ACHIEVE I and ACHIEVE II) demonstrated effectiveness and safety of ubrogepant in acute migraine attacks. Ubrogepant can be administered as 50- and 100-mg tablets, with a maximum dose of 200 mg within 48 h. Besides minimizing pain, the drug is equally effective in alleviating migraine-associated symptoms such as nausea, photophobia and sound sensitivity. Unlike other gepants, ubrogepant is free from hepatotoxicity at the therapeutic doses. In certain cases (1 in 5), a full relief of pain was achieved with a single dose of the drug. The molecule is not effective as a preventive migraine therapy. The present review discusses the background, preclinical and clinical pharmacology, indication and safety of ubrogepant for the treatment of migraine attacks.

Keywords: Antimigraine drugs; Aura; Calcitonin gene-related peptide (CGRP) antagonists; Gepants; Migraine headaches; Treatment of pain; Ubrogepant.

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