Zavegepant

Summary

Zavegepant (CHEMBL2397415) is an approved small-molecule calcitonin gene-related peptide receptor antagonist (ATC N02CD08); indicated across 3 conditions including migraine disorder and severe acute respiratory syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02CD08
• Indications: 3 conditions
• Clinical trials: 13
• Chemistry: 638.8 Da · C36H46N8O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2397415
Name	Zavegepant
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	53472683
ChEBI	CHEBI:229643
ATC	N02CD08
Molecular formula	C36H46N8O3
Molecular weight	638.8
InChIKey	JJVAPHYEOZSKJZ-JGCGQSQUSA-N

SMILES: CC1=CC(=CC2=C1NN=C2)C[C@H](C(=O)N3CCN(CC3)C4CCN(CC4)C)NC(=O)N5CCC(CC5)C6=CC7=CC=CC=C7NC6=O

IUPAC name: N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-1-oxopropan-2-yl]-4-(2-oxo-1H-quinolin-3-yl)piperidine-1-carboxamide

ChEBI definition: A member of the class of ureas that is urea in which both amino groups are replaced by 4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidin-1-yl and {(2R)-3-(7-methyl-1H-indazol-5-yl)-1-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]-1-oxopropan-2-yl}amino groups. It is a calcitonin gene-related peptide receptor antagonist whose hydrochloride salt has been approved by the FDA for the acute treatment of migraine.

Pharmacological roles (ChEBI): calcitonin gene-related peptide receptor antagonist.

Also known as: BHV-3500, BMS-742413, Vazegepant, Zavegepant, ZAVEGEPANT

Parent form; salt/anhydrous children: CHEMBL4650220

Patent coverage: 134 distinct patent families (296 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 255 (86%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	CGRP receptor	Antagonist	10.64

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Cytochrome P450 3A4, Calcitonin gene-related peptide type 1 receptor.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CALCRL	10.64	Ki	0.02	nM	CHEMBL_ACT_13358851

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
migraine disorder	3	MONDO:0005277	MONDO:0005277
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
asthma	1	MONDO:0004979	MONDO:0004979

Clinical trials

Total trials: 13.

Phase distribution

Phase	Trials
PHASE2/PHASE3	4
PHASE1	4
PHASE3	3
PHASE4	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06401642	PHASE4	RECRUITING	Effectiveness and Tolerability of Zavegepant for Acute Migraine Treatment Among Those Using CGRP Targeting Preventive Medications
NCT06985342	PHASE4	TERMINATED	Acute Migraine Treatment in the ED With Gepants
NCT03872453	PHASE2/PHASE3	COMPLETED	Acute Treatment Trial in Adult Subjects With Migraines
NCT04346615	PHASE2/PHASE3	TERMINATED	Safety and Efficacy Trial of Zavegepant* Intranasal for Hospitalized Patients With COVID-19 Requiring Supplemental Oxygen
NCT04408794	PHASE2/PHASE3	COMPLETED	Long-term Safety Study of BHV-3500 (Zavegepant*) for the Acute Treatment of Migraine
NCT04571060	PHASE3	COMPLETED	Randomized Trial in Adult Participants With Acute Migraines
NCT04804033	PHASE2/PHASE3	TERMINATED	A Study to Evaluate the Efficacy and Safety of Oral Zavegepant in Migraine Prevention
NCT05989048	PHASE3	COMPLETED	A Study to Learn About Zavegepant as the Acute Treatment of Migraine in Asian Adults
NCT06103734	PHASE3	WITHDRAWN	A Study to Learn About Zavegepant as a Treatment for Multiple Migraine Attacks in Adult Participants
NCT06995729	PHASE1	RECRUITING	A Study to Learn About the Study Medicine Called Zavegepant (PF-07930207) in Children With a History of Migraine
NCT04987944	PHASE1	TERMINATED	Safety and Efficacy Active Drug vs. Placebo in Subjects With Asthma
NCT05960032	PHASE1	COMPLETED	A Study to Learn About the Study Medicine Called Zavegepant in Healthy Chinese Adult Participants
NCT06453356	PHASE1	COMPLETED	A Study to Learn How the Study Medicine Called Zavegepant is Taken Up Into Blood and Breast Milk of Healthy Breast-Feeding Women

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).