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A Phase 1 Open‐Label Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of a Single Intranasal Dose of Zavegepant in Healthy Chinese Adults

Year: 2025

Type: article

Abstract: Zavegepant is the only calcitonin gene‐related peptide antagonist approved as a nasal spray in the United States for acute treatment of migraine in adults with or without aura. This Phase 1, open‐label study evaluated the pharmacokinetics, safety, and tolerability of a single intranasal dose of zavegepant 10 mg in 12 healthy Chinese adults. Blood samples were collected for pharmacokinetic assessment prior to dosing and from 5 min to 24 h post dose. Geometric mean values for the primary pharmacokinetic parameters were 53.53 ng h/mL for area under the plasma concentration–time curve (AUC) from time zero to infinity, 44.25 ng h/mL for AUC from time zero to time of last quantifiable concentration, and 20.32 ng/mL for maximum plasma concentration (C max ). Secondary parameters included time to C max (median, 0.58 h), apparent clearance (geometric mean, 186.8 L/h), apparent volume of distribution (geometric mean, 2943 L), and terminal half‐life (arithmetic mean, 11.0 h). Results were comparable to exposures observed previously in non‐Asian healthy participants following a single intranasal dose of zavegepant 10 mg. Zavegepant demonstrated a favorable safety profile, with no serious or severe adverse events and no clinically relevant findings regarding laboratory tests, vital signs, or electrocardiograms observed.

Source: Clinical Pharmacology in Drug Development

DOI: 10.1002/cpdd.1617