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frovatriptan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| serotonin (5-HT1) receptor agonists, sumatriptan derivatives | 1251 | 158747-02-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 6 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.44 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 27 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3.60 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.85 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 24 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 72 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | AAK1,ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK16,CDK5,CDK9,CHEK1,CLK2,CLK4,DDR1,DYRK1A,DYRK1B,DYRK2,EGFR,EIF2AK3,ERBB2,FLT3,GAK,GRK1,GRK2,GSK3B,HASPIN,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,KDR,KIT,LCK,LRRK2,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MARK4,MELK,MET,MINK1,NTRK1,NTRK2,NTRK3,NUAK1,PAK4,PDK1,PDK2,PDK4,PIK3CA,PIM2,PRKAA1,PRKAA2,PRKCD,PRKCZ,PRKDC,ROCK2,SGK1,SIK2,SIK3,SRC,STK17A,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TTK,ULK1,ULK2 | 97 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK4,CDK8,CDK9,CLK2,CLK4,DYRK1A,DYRK1B,DYRK2,EGFR,EIF2AK3,HASPIN,IKBKB,IRAK1,JAK2,MAP2K6,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK7,MARK4,MELK,PDK1,PIM3,PRKCD,ROCK1,ROCK2,SIK2,SIK3,STK33,STK4,SYK,TNK1,TTK,ULK1,ULK2 | 45 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 8, 2001 | FDA | ENDO PHARMS |
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 for unapproved indication | 581.06 | 52.53 | 177 | 3280 | 66467 | 90558523 |
| Swollen tongue | 535.89 | 52.53 | 153 | 3304 | 45803 | 90579187 |
| Dysphonia | 488.05 | 52.53 | 153 | 3304 | 62931 | 90562059 |
| Angioedema | 488.00 | 52.53 | 154 | 3303 | 64722 | 90560268 |
| Swelling face | 449.80 | 52.53 | 153 | 3304 | 81199 | 90543791 |
| Neovascularisation | 238.51 | 52.53 | 43 | 3414 | 1587 | 90623403 |
| Drug intolerance | 213.56 | 52.53 | 158 | 3299 | 447433 | 90177557 |
| Hypersensitivity | 206.85 | 52.53 | 156 | 3301 | 454521 | 90170469 |
| Headache | 201.69 | 52.53 | 202 | 3255 | 862544 | 89762446 |
| Paradoxical drug reaction | 184.34 | 52.53 | 43 | 3414 | 5723 | 90619267 |
| Off label use | 165.77 | 52.53 | 205 | 3252 | 1102047 | 89522943 |
| Anuria | 144.09 | 52.53 | 43 | 3414 | 14775 | 90610215 |
| Extrapyramidal disorder | 140.04 | 52.53 | 43 | 3414 | 16260 | 90608730 |
| Migraine | 117.57 | 52.53 | 79 | 3378 | 190313 | 90434677 |
| Product use in unapproved indication | 89.34 | 52.53 | 85 | 3372 | 336151 | 90288839 |
| Drug ineffective | 69.62 | 52.53 | 158 | 3299 | 1384140 | 89240850 |
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 for unapproved indication | 543.54 | 66.00 | 177 | 3215 | 102661 | 110483246 |
| Swollen tongue | 527.69 | 66.00 | 153 | 3239 | 60209 | 110525698 |
| Dysphonia | 493.04 | 66.00 | 153 | 3239 | 75776 | 110510131 |
| Swelling face | 463.61 | 66.00 | 153 | 3239 | 92168 | 110493739 |
| Angioedema | 457.86 | 66.00 | 154 | 3238 | 98346 | 110487561 |
| Drug intolerance | 258.87 | 66.00 | 158 | 3234 | 406354 | 110179553 |
| Hypersensitivity | 252.04 | 66.00 | 155 | 3237 | 403843 | 110182064 |
| Neovascularisation | 245.14 | 66.00 | 43 | 3349 | 1694 | 110584213 |
| Headache | 209.35 | 66.00 | 189 | 3203 | 882188 | 109703719 |
| Paradoxical drug reaction | 170.92 | 66.00 | 43 | 3349 | 9774 | 110576133 |
| Off label use | 148.06 | 66.00 | 203 | 3189 | 1499982 | 109085925 |
| Anuria | 132.31 | 66.00 | 43 | 3349 | 24298 | 110561609 |
| Extrapyramidal disorder | 125.11 | 66.00 | 43 | 3349 | 28824 | 110557083 |
| Migraine | 111.82 | 66.00 | 68 | 3324 | 171584 | 110414323 |
| Product use in unapproved indication | 79.01 | 66.00 | 82 | 3310 | 447295 | 110138612 |
| Drug ineffective | 72.29 | 66.00 | 149 | 3243 | 1520391 | 109065516 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02CC07 | NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Selective serotonin (5HT1) agonists |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| FDA MoA | N0000175763 | Serotonin 1b Receptor Agonists |
| FDA MoA | N0000175764 | Serotonin 1d Receptor Agonists |
| FDA EPC | N0000175765 | Serotonin-1b and Serotonin-1d Receptor Agonist |
| CHEBI has role | CHEBI:35480 | analgesic |
Related Drugs by ATC class:
N02CC Selective serotonin (5HT1) agonists 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Migraine | indication | 37796009 | DOID:6364 |
| Hypercholesterolemia | contraindication | 13644009 | |
| Coronary artery spasm | contraindication | 23687008 | DOID:11840 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Hemiplegic migraine | contraindication | 59292006 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Vascular insufficiency of intestine | contraindication | 82196007 | |
| Prinzmetal angina | contraindication | 87343002 | |
| Angina pectoris | contraindication | 194828000 | |
| Cerebrovascular accident | contraindication | 230690007 | |
| Transient ischemic attack | contraindication | 266257000 | DOID:224 |
| Raynaud's phenomenon | contraindication | 266261006 | |
| Serotonin syndrome | contraindication | 371089000 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Peripheral vascular disease | contraindication | 400047006 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Hypertensive urgency | contraindication | 443482000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.14 | acidic |
| pKa2 | 12.79 | acidic |
| pKa3 | 10.16 | Basic |
Orange Book patent data (new drug applications)
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1D | GPCR | AGONIST | Ki | 8.36 | CHEMBL | CHEMBL | |||
| 5-hydroxytryptamine receptor 1B | GPCR | AGONIST | Ki | 7.99 | CHEMBL | CHEMBL | |||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 7.21 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 7.44 | CHEMBL | |||||
| D(4) dopamine receptor | GPCR | Ki | 6.04 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1E | GPCR | Ki | 6.51 | CHEMBL | |||||
| Mu-type opioid receptor | GPCR | Ki | 6.73 | CHEMBL | |||||
| Transmembrane protein 97 | Enzyme | Ki | 5.49 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | Ki | 6.16 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021297 | VUID |
| N0000148734 | NUI |
| D04264 | KEGG_DRUG |
| 158930-17-7 | SECONDARY_CAS_RN |
| 4021297 | VANDF |
| C0754647 | UMLSCUI |
| CHEBI:134991 | CHEBI |
| CHEMBL1279 | ChEMBL_ID |
| DB00998 | DRUGBANK_ID |
| CHEMBL2138684 | ChEMBL_ID |
| C108128 | MESH_SUPPLEMENTAL_RECORD_UI |
| 77992 | PUBCHEM_CID |
| 7191 | IUPHAR_LIGAND_ID |
| 7661 | INN_ID |
| H82Q2D5WA7 | UNII |
| 228783 | RXNORM |
| 16207 | MMSL |
| 239641 | MMSL |
| d04776 | MMSL |
| 009509 | NDDF |
| 009510 | NDDF |
| 370214004 | SNOMEDCT_US |
| 411990007 | SNOMEDCT_US |
| 767324002 | SNOMEDCT_US |
| H82Q2D5WA7 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| FROVA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-396 | TABLET, FILM COATED | 2.50 mg | ORAL | NDA | 25 sections |
| FROVATRIPTAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50742-299 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 23 sections |
| frovatriptan succinate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68462-694 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
| Frovatriptan | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1539 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |
| FROVATRIPTAN SUCCINATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69315-157 | TABLET, FILM COATED | 2.50 mg | ORAL | ANDA | 25 sections |