New Drug Monograph By: Madeline McMillan, PharmD Candidate 2022
Generic Name: atogepant Brand Name: QuliptaTM Classification: Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist FDA Approval: September 28, 2021 Indication1: Approved for the prevention of episodic migraine in adults. Contraindications: None. Pharmacology : Atogepant is a calcitonin gene-related peptide (CGRP) receptor antagonist. CGRP helps modulate pain transmission in the brainstem. During an acute migraine attack, CGRP levels are usually increased. 1,2
Pharmacokinetics1,2 Absorption Atogepant is orally absorbed and reaches peak plasma concentrations
within 1-2 hours. The absorption of atogepant is not significantly affected by food; therefore, it may be administered without regard to meals. Distribution Atogepant is approximately 95% protein bound. The volume of distribution after oral administration was approximately 292 L. Metabolism Atogepant is primarily metabolized by CYP3A4. Elimination Atogepant was excreted as 42% unchanged drug in the feces and 5% unchanged drug in the urine. The approximately elimination half-life of atogepant is 11 hours. Drug Interactions1 CYP3A4 inhibitors Concentrations of atogepant may be increased by CYP3A4 inhibitors. If atogepant must be administered in combination with a strong Page 28
CYP3A4 inhibitor, the daily dose should be reduced to 10 mg daily. For coadministration of atogepant with moderate or weak CYP3A4 inhibitors, dose reduction may not be necessary. CYP3A4 inducers Concentrations of atogepant may be reduced by CYP3A4 inducers. If administration of atogepant along with a strong CYP3A4 inhibitor is necessary, the recommended dose of atogepant is either 30 mg or 60 mg daily. OATP inhibitors Concentrations of atogepant may be increased by OATP inhibitors. The recommended dose of atogepant is 10 mg or 30 mg daily when being used in combination with an OATP inhibitor. Clinical Efficacy3,4 Goadsby and colleagues conducted a phase 2b/3 trial to assess the safety, tolerability, and efficacy of atogepant for the prevention of episodic migraines. Participants
