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rimegepant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcitonin gene-related peptide receptor antagonists | 5381 | 1289023-67-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Rimegepant is a calcitonin gene-related peptide receptor antagonist
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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 27, 2020 | FDA | BIOHAVEN PHARM | |
| April 25, 2022 | EMA | BIOHAVEN PHARMACEUTICAL IRELAND DAC |
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 | 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 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 |
|---|---|---|---|---|---|---|
| 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 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 | 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:
| 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 |
| 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
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. 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Calcitonin gene-related peptide type 1 receptor | GPCR | ANTAGONIST | Ki | 10.56 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 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:
| 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 | 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 |