Rimegepant

Summary

Rimegepant (CHEMBL2178422) is an approved small molecule (ATC N02CD06); indicated across 7 conditions including temporomandibular joint disorder and sinusitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: N02CD06
• Indications: 7 conditions
• Clinical trials: 43
• Chemistry: 534.6 Da · C28H28F2N6O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2178422
Name	Rimegepant
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	51049968
ATC	N02CD06
Molecular formula	C28H28F2N6O3
Molecular weight	534.6
InChIKey	KRNAOFGYEFKHPB-ANJVHQHFSA-N

SMILES: C1C[C@H](C2=C(C=CC=N2)[C@H]([C@@H]1C3=C(C(=CC=C3)F)F)N)OC(=O)N4CCC(CC4)N5C6=C(NC5=O)N=CC=C6

IUPAC name: [(5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl] 4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate

Also known as: Bhv-3000, BMS-927711, Rimegepant, RIMEGEPANT

Parent form; salt/anhydrous children: CHEMBL2364629

Patent coverage: 210 distinct patent families (417 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 340 (82%) 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
	AMY1 receptor	Antagonist	8.1
	CGRP receptor	Antagonist	9.6

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

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CALCRL	10.57	Ki	0.03	nM	CHEMBL_ACT_12142831
CALCRL	9.85	EC50	0.14	nM	CHEMBL_ACT_12142828
ADRB2	5.5	EC50	3200	nM	CHEMBL_ACT_25751470

Target pathways

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

Indications & clinical

Indications

7 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
temporomandibular joint disorder	3	MONDO:0005473	EFO:0005279
sinusitis	3	MONDO:0005961	EFO:0007486
migraine disorder	3	MONDO:0005277	MONDO:0005277
trigeminal neuralgia	2	MONDO:0008599	EFO:1001219
psoriasis	2	MONDO:0005083	EFO:0000676
irritable bowel syndrome	2	MONDO:0005052	EFO:0000555

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 43.

Phase distribution

Phase	Trials
PHASE3	13
Not specified	11
PHASE4	9
PHASE2	8
PHASE2/PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06473597	PHASE4	RECRUITING	A Comparison of Nurtec ODT to Maxalt MLT-ODT in Adult ED Patients With Migraine Headache
NCT07301008	PHASE4	RECRUITING	Rimegepant as Preemptive Treatment for Predictable Trigger-Induced Migraine in Adult Patients in the US
NCT07609914	PHASE4	NOT_YET_RECRUITING	A Study to Learn About the Safety of Taking an Additional Dose of the Medicine Rimegepant in Adults With Migraine
NCT05127486	PHASE4	COMPLETED	A Study of Galcanezumab (LY2951742) in Adult Participants With Episodic Migraine
NCT05207865	PHASE4	COMPLETED	Safety and Tolerability Study of Daily Dosing Rimegepant in Episodic Migraine Prevention
NCT05211154	PHASE4	TERMINATED	Evaluation of the Efficacy of Diclofenac Potassium and Rimegepant for the Acute Treatment of Migraine
NCT05509400	PHASE4	COMPLETED	Efficacy and Tolerability of Rimegepant for the Acute Treatment of Migraine in Adults Unsuitable for Triptan Use
NCT05518123	PHASE4	COMPLETED	Efficacy and Tolerability of Rimegepant for the Prevention of Migraine in Adults With History of Inadequate Response to Oral Preventive Medications
NCT06985342	PHASE4	TERMINATED	Acute Migraine Treatment in the ED With Gepants
NCT04649242	PHASE3	RECRUITING	Randomized Study in Children and Adolescents With Migraine: Acute Treatment
NCT04743141	PHASE3	RECRUITING	Long-term Safety Study of Rimegepant in Pediatric Subjects for the Acute Treatment of Migraine
NCT05156398	PHASE3	RECRUITING	Efficacy and Safety Study of Rimegepant for the Preventative Treatment of Migraine in Pediatric Subjects
NCT06616194	PHASE3	RECRUITING	A Study to Learn About the Study Medicine Called Rimegepant in Adolescents With Frequent Migraine
NCT06641466	PHASE3	RECRUITING	A Study to Learn About the Study Medicine Called Rimegepant in Women When Used for Intermittent Prevention of Menstrual Migraine
NCT03235479	PHASE3	COMPLETED	Safety and Efficacy Study in Adult Subjects With Acute Migraines
NCT03237845	PHASE3	COMPLETED	Safety and Efficacy in Adult Subjects With Acute Migraines
NCT03266588	PHASE2/PHASE3	COMPLETED	Open Label Safety Study in Acute Treatment of Migraine
NCT03461757	PHASE3	COMPLETED	Trial in Adult Subjects With Acute Migraines
NCT03732638	PHASE2/PHASE3	COMPLETED	Efficacy and Safety Trial of Rimegepant for Migraine Prevention in Adults
NCT04574362	PHASE3	COMPLETED	Safety and Efficacy Trial of BHV3000 (Rimegepant) 75 mg for the Acute Treatment of Migraine
NCT05262517	PHASE3	TERMINATED	Safety and Efficacy of BHV-3000 (Rimegepant) Orally Disintegrating Tablet for Acute Treatment of Temporomandibular Disorders
NCT05399459	PHASE3	COMPLETED	Efficacy and Safety Study of Rimegepant for the Acute Treatment of Migraine in Japanese Subjects (Japan Only)
NCT05399485	PHASE3	COMPLETED	Efficacy and Safety Study of Rimegepant for Migraine Prevention in Japanese Subjects (Japan Only)
NCT05810038	PHASE3	COMPLETED	A Study to Learn About the Safety and Effects of Rimegepant to Prevent Migraine in Chinese Subjects.
NCT06748664	PHASE2	NOT_YET_RECRUITING	A Clinical Trial of Rimegepant for Vestibular Migraine Evaluation: Pre-experiment
NCT06992674	PHASE2	ACTIVE_NOT_RECRUITING	The R-E-V-I-V-A-L Study
NCT06999252	PHASE2	NOT_YET_RECRUITING	Rimegepant Combined With PD-1 in Liver Metastasis Colorectal Cancer Patients
NCT07613788	PHASE2	NOT_YET_RECRUITING	Rimegepant Plus Glofitamab and CD19 CAR-T Therapy in R/R LBCL
NCT01430442	PHASE2	COMPLETED	Dose Ranging Study of Rimegepant (BMS-927711) for the Acute Treatment of Migraine
NCT03941834	PHASE2	TERMINATED	Trial for Treatment Refractory Trigeminal Neuralgia
NCT04629950	PHASE2	COMPLETED	Rimegepant in Moderate Plaque-type Psoriasis
NCT05264714	PHASE2	COMPLETED	Cluster Headache Treatment With Rimegepant
NCT05046613	Not specified	RECRUITING	Observational Study to Assess Maternal, Fetal and Infant Outcomes Following Exposure to Rimegepant
NCT05198245	Not specified	ACTIVE_NOT_RECRUITING	Study of Pregnancy Outcomes in Women Exposed to Rimegepant During Pregnancy
NCT06212661	Not specified	ENROLLING_BY_INVITATION	Migraine Medication Effects on Urinary Symptoms
NCT06409832	Not specified	RECRUITING	RimegepAnt effectIvenesS and tolErability as Migraine Preventive Treatment
NCT06439628	Not specified	ACTIVE_NOT_RECRUITING	ARISE-A Chinese Real-world Study of Rimegepant for the Acute Treatment of Migraine
NCT06728345	Not specified	NOT_YET_RECRUITING	The Real-world Study of Rimegepant Treatment in Female Migraine Patients of China
NCT03934086	Not specified	NO_LONGER_AVAILABLE	An Open-label, Intermediate Size, Expanded Access Study of BHV-3000 in the Acute Treatment of Migraine
NCT05709106	Not specified	COMPLETED	A Prospective Real World Study of Rimegepant in the Treatment of Migraine

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).