Features and properties of zavegepant

Alternative names	BHV 3500; BMS-742413; BMS-742413-03; Vazegepant; Vazegepant - Pfizer; Zavegepant hydrochloride; ZAVZPRET
Class	Anti-infectives; antiallergics; antimigraines; indazoles; piperazines; piperidines; quinolines; small molecules
Mechanism of action	CGRP receptor antagonist
Route of administration	Intranasal, oral
Pharmacodynamics	Highly potent, selective, competitive CGRP receptor antagonist
	Demonstrated potent and full reversal of CGRP-induced dilation of ex vivo human intracranial arteries
	Does not prolong the corrected QT interval or have a clinically relevant effect on other ECG parameters
	Single doses of ≥ 10 mg produced an average Cmax associated with ≥ 90% inhibition of CGRP signalling
Pharmacokinetics (after an intranasal 10 mg dose)	Cmax reached at ≈ 30 mins after a single dose; absolute bioavailability ≈ 5%;
	Mean apparent volume of distribution ≈ 1774 L
	Effective half-life 6.55 h; mean apparent clearance 266 L/h
Adverse events (after a single dose)
Most frequent	Dysgeusia, nausea, nasal discomfort, vomiting
Rare	Hypersensitivity, including facial swelling and urticaria
ATC codes
WHO ATC code	J05A-X (other antivirals); N02C (antimigraine preparations); R03 (drugs for obstructive airway diseases)
EphMRA ATC code	J5 (antivirals for systemic use); N2C (anti-migraine preparations); R3 (anti-asthma and COPD products)
Chemical name	(R)-N(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl) piperazin-1-yl)-1-oxopropan-2-yl)4-(2-oxo-1,2-dihydroquinolin-3-yl) piperidine-1-carboxamide hydrochloride