rimegepant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
calcitonin gene-related peptide receptor antagonists 5381 1289023-67-1

Description:

MoleculeDescription

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:

DoseUnitRoute
37.50 mg O

ADMET properties:

PropertyValueReference
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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK9,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MET,PDK1,PDK2,PDK4,PIK3CD,PRKDC 16
kinase-selectivity-class AXL,BRAF,CAMK2D,CDK9,GRK2,SIK2,STK33 7
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Feb. 27, 2020 FDA BIOHAVEN PHARM
April 25, 2022 EMA BIOHAVEN PHARMACEUTICAL IRELAND DAC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug ineffective 281.77 21.26 394 5575 1383904 89238574
Exposure during pregnancy 101.44 21.26 100 5869 238310 90384168
Migraine 84.93 21.26 82 5887 190310 90432168
Product administration interrupted 68.14 21.26 27 5942 12465 90610013
Nausea 50.83 21.26 174 5795 1110142 89512336
Gestational hypertension 49.86 21.26 15 5954 3047 90619431
Thyroid atrophy 45.65 21.26 9 5960 307 90622171
Postnatal growth restriction 43.01 21.26 7 5962 77 90622401
Intentional dose omission 40.82 21.26 21 5948 17762 90604716
Pre-eclampsia 37.32 21.26 17 5952 11031 90611447
Dermatitis atopic 35.37 21.26 21 5948 23451 90599027
Therapeutic product effect delayed 35.21 21.26 12 5957 3629 90618849
COVID-19 30.54 21.26 46 5923 168797 90453681
Illness 30.41 21.26 32 5937 81937 90540541
Foetal exposure during pregnancy 30.17 21.26 24 5945 42951 90579527
Headache 29.97 21.26 124 5845 862622 89759856
Off label use 28.36 21.26 145 5824 1102107 89520371
Live birth 26.04 21.26 29 5940 79078 90543400
Failed induction of labour 25.55 21.26 6 5963 471 90622007
Incorrect dose administered 24.39 21.26 28 5941 78902 90543576
Palpitations 24.36 21.26 37 5932 136691 90485787
Malabsorption 24.13 21.26 10 5959 5168 90617310
Vitamin B12 deficiency 23.66 21.26 11 5958 7475 90615003
Dizziness 23.06 21.26 88 5881 589196 90033282
Injection site pain 22.85 21.26 41 5928 173658 90448820
Drug effect less than expected 22.50 21.26 10 5959 6128 90616350
Somnolence 22.14 21.26 45 5924 209039 90413439

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Postnatal growth restriction 205.02 39.49 26 754 174 42620381
Foetal exposure during pregnancy 88.68 39.49 33 747 47278 42573277
Migraine 55.94 39.49 20 760 25394 42595161

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug ineffective 240.45 23.51 319 4785 1520221 109063974
Migraine 97.46 23.51 73 5031 171579 110412616
Postnatal growth restriction 52.48 23.51 7 5097 24 110584171
Headache 51.03 23.51 120 4984 882257 109701938
Thyroid atrophy 49.11 23.51 9 5095 298 110583897
Product administration interrupted 46.31 23.51 18 5086 11274 110572921
Nausea 30.58 23.51 125 4979 1235565 109348630
Dermatitis atopic 29.57 23.51 17 5087 25524 110558671
Anxiety 25.59 23.51 52 5052 345026 110239169
Malabsorption 25.49 23.51 10 5094 6415 110577780
Therapeutic product effect delayed 25.18 23.51 9 5095 4470 110579725
Pruritus 25.10 23.51 71 5033 581489 110002706
Vitamin B12 deficiency 24.30 23.51 11 5093 10044 110574151
Illness 24.11 23.51 24 5080 82147 110502048
Palpitations 23.98 23.51 33 5071 159179 110425016

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:53784 antispasmodic drug

Related Drugs by ATC class:

N02CD Calcitonin gene-related peptide (CGRP) antagonists 7 drugs
atogepanteptinezumaberenumabfremanezumabgalcanezumabubrogepantzavegepant

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 75MG BASE NURTEC ODT PFIZER N212728 Feb. 27, 2020 RX TABLET, ORALLY DISINTEGRATING ORAL 8314117 Feb. 27, 2034 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. 27, 2034 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)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Calcitonin gene-related peptide type 1 receptor GPCR ANTAGONIST Ki 10.56 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
997WVV895X UNII
1374024-48-2 SECONDARY_CAS_RN
4039211 VANDF
C4519126 UMLSCUI
CHEBI:754827 CHEBI
CHEMBL2178422 ChEMBL_ID
51049968 PUBCHEM_CID
DB12457 DRUGBANK_ID
CHEMBL2364629 ChEMBL_ID
9751 INN_ID
C578443 MESH_SUPPLEMENTAL_RECORD_UI
D10663 KEGG_DRUG
10704 IUPHAR_LIGAND_ID
860726001 SNOMEDCT_US
860757001 SNOMEDCT_US
897285009 SNOMEDCT_US
331345 MMSL
38186 MMSL
d09516 MMSL
018289 NDDF
018290 NDDF
2282307 RXNORM
997WVV895X INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NURTEC ODT HUMAN PRESCRIPTION DRUG LABEL 1 72618-3000 TABLET, ORALLY DISINTEGRATING 75 mg ORAL NDA 33 sections
NURTEC ODT HUMAN PRESCRIPTION DRUG LABEL 1 72618-3001 TABLET, ORALLY DISINTEGRATING 75 mg ORAL NDA 33 sections
NURTEC ODT HUMAN PRESCRIPTION DRUG LABEL 1 85766-096 TABLET, ORALLY DISINTEGRATING 75 mg ORAL NDA 33 sections