rimegepant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
calcitonin gene-related peptide receptor antagonists	5381	1289023-67-1

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rimegepant
rimegepant sulfate
BMS-927711
nurtec odt
BHV-3000
vydura

Rimegepant is a calcitonin gene-related peptide receptor antagonist

Molecular weight: 534.57
Formula: C28H28F2N6O3
CLOGP: 3.68
LIPINSKI: 1
HAC: 9
HDO: 2
TPSA: 113.68
ALOGS: -3.85
ROTB: 4

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
37.50	mg	O

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.06 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
April 25, 2022	EMA	BIOHAVEN PHARMACEUTICAL IRELAND DAC
Feb. 27, 2020	FDA	BIOHAVEN PHARM

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	186.17	26.59	180	1563	1044585	62442694
Migraine	53.56	26.59	34	1709	103312	63383967
Nausea	42.54	26.59	80	1663	854391	62632888

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	220.39	32.79	163	1183	1080750	78662292
Migraine	50.28	32.79	26	1320	87467	79655575

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N02CD06	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Calcitonin gene-related peptide (CGRP) antagonists
FDA EPC	N0000193917	Calcitonin Gene-related Peptide Receptor Antagonist
FDA MoA	N0000193918	Calcitonin Gene-related Peptide Receptor Antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Migraine	indication	37796009	DOID:6364
Prevention of migraine attacks	indication	408381007

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.51	acidic
pKa2	7.34	Basic
pKa3	2.79	Basic
pKa4	0.19	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 75MG BASE	NURTEC ODT	PFIZER	N212728	Feb. 27, 2020	RX	TABLET, ORALLY DISINTEGRATING	ORAL	8314117	Feb. 22, 2031	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
EQ 75MG BASE	NURTEC ODT	PFIZER	N212728	Feb. 27, 2020	RX	TABLET, ORALLY DISINTEGRATING	ORAL	8314117	Feb. 22, 2031	PREVENTIVE TREATMENT OF EPISODIC MIGRAINE IN ADULTS
EQ 75MG BASE	NURTEC ODT	PFIZER	N212728	Feb. 27, 2020	RX	TABLET, ORALLY DISINTEGRATING	ORAL	11083724	March 25, 2039	ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS
EQ 75MG BASE	NURTEC ODT	PFIZER	N212728	Feb. 27, 2020	RX	TABLET, ORALLY DISINTEGRATING	ORAL	11083724	March 25, 2039	PREVENTIVE TREATMENT OF EPISODIC MIGRAINE IN ADULTS

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 75MG BASE	NURTEC ODT	PFIZER	N212728	Feb. 27, 2020	RX	TABLET, ORALLY DISINTEGRATING	ORAL	May 27, 2024	FOR THE PREVENTIVE TREATMENT OF EPISODIC MIGRAINE IN ADULTS
EQ 75MG BASE	NURTEC ODT	PFIZER	N212728	Feb. 27, 2020	RX	TABLET, ORALLY DISINTEGRATING	ORAL	Feb. 27, 2025	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Calcitonin gene-related peptide type 1 receptor	GPCR	Q16602	CALRL_HUMAN	ANTAGONIST	Ki	10.56		SCIENTIFIC LITERATURE	DRUG LABEL

External reference:

ID	Source
997WVV895X	UNII
1374024-48-2	SECONDARY_CAS_RN
C4519126	UMLSCUI
CHEMBL2178422	ChEMBL_ID
51049968	PUBCHEM_CID
DB12457	DRUGBANK_ID
CHEMBL2364629	ChEMBL_ID
9751	INN_ID
D10663	KEGG_DRUG
10704	IUPHAR_LIGAND_ID
018289	NDDF
018290	NDDF
860726001	SNOMEDCT_US
860757001	SNOMEDCT_US
897285009	SNOMEDCT_US
4039211	VANDF
2282307	RXNORM
331345	MMSL
38186	MMSL
d09516	MMSL
C578443	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NURTEC ODT	HUMAN PRESCRIPTION DRUG LABEL	1	72618-3000	TABLET, ORALLY DISINTEGRATING	75 mg	ORAL	NDA	32 sections
NURTEC ODT	HUMAN PRESCRIPTION DRUG LABEL	1	72618-3000	TABLET, ORALLY DISINTEGRATING	75 mg	ORAL	NDA	32 sections
NURTEC ODT	HUMAN PRESCRIPTION DRUG LABEL	1	72618-3000	TABLET, ORALLY DISINTEGRATING	75 mg	ORAL	NDA	32 sections
NURTEC ODT	HUMAN PRESCRIPTION DRUG LABEL	1	72618-3000	TABLET, ORALLY DISINTEGRATING	75 mg	ORAL	NDA	32 sections
NURTEC ODT	HUMAN PRESCRIPTION DRUG LABEL	1	72618-3001	TABLET, ORALLY DISINTEGRATING	75 mg	ORAL	NDA	32 sections