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

Stem definition	Drug id	CAS RN
serotonin (5-HT1) receptor agonists, sumatriptan derivatives	1251	158747-02-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: frovatriptan (R)-Frovatriptan frovatriptan succinate frovatriptan succinate hydrate SB 209509 VML251	Molecular weight: 243.31 Formula: C14H17N3O CLOGP: 0.72 LIPINSKI: 0 HAC: 4 HDO: 3 TPSA: 70.91 ALOGS: -3.30 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

frovatriptan
(R)-Frovatriptan
frovatriptan succinate
frovatriptan succinate hydrate
SB 209509
VML251

Molecular weight: 243.31
Formula: C14H17N3O
CLOGP: 0.72
LIPINSKI: 0
HAC: 4
HDO: 3
TPSA: 70.91
ALOGS: -3.30
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2.50	mg	O

ADMET properties:

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Property	Value	Reference
S (Water solubility)	72 mg/mL	Bocci G, Oprea TI, Benet LZ
EoM (Fraction excreted unchanged in urine)	6 %	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	3.60 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	27 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	24 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.85 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.44 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Nov. 8, 2001	FDA	ENDO PHARMS

FDA Adverse Event Reporting System (Female)

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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	180.13	34.22	61	2195	34002	63452764
Neovascularisation	174.97	34.22	31	2225	1114	63485652
Paradoxical drug reaction	135.14	34.22	31	2225	4121	63482645
Migraine	123.40	34.22	64	2192	103282	63383484
Anuria	101.14	34.22	31	2225	12520	63474246
Extrapyramidal disorder	99.41	34.22	31	2225	13253	63473513
Swollen tongue	73.56	34.22	32	2224	34768	63451998
Angioedema	69.70	34.22	34	2222	47931	63438835
Dysphonia	66.94	34.22	33	2223	47581	63439185
Swelling face	63.46	34.22	35	2221	63440	63423326

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FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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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
Neovascularisation	182.16	43.85	31	2036	1214	79741107
Drug ineffective for unapproved indication	166.97	43.85	59	2008	51179	79691142
Paradoxical drug reaction	127.97	43.85	31	2036	7154	79735167
Migraine	116.92	43.85	53	2014	87440	79654881
Anuria	95.13	43.85	31	2036	20932	79721389
Extrapyramidal disorder	92.74	43.85	31	2036	22648	79719673
Swollen tongue	70.39	43.85	30	2037	42540	79699781
Dysphonia	65.11	43.85	31	2036	56841	79685480
Swelling face	61.36	43.85	32	2035	71180	79671141
Dyspepsia	58.81	43.85	36	2031	108651	79633670

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02CC07	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Selective serotonin (5HT1) agonists
FDA EPC	N0000175765	Serotonin-1b and Serotonin-1d Receptor Agonist
FDA MoA	N0000175763	Serotonin 1b Receptor Agonists
FDA MoA	N0000175764	Serotonin 1d Receptor Agonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D017366	Serotonin Receptor Agonists

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

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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

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🐶 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:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN	AGONIST	Ki	7.99	CHEMBL	CHEMBL
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	AGONIST	Ki	8.36	CHEMBL	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.21	CHEMBL

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External reference:

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ID	Source
009509	NDDF
009510	NDDF
158930-17-7	SECONDARY_CAS_RN
16207	MMSL
228783	RXNORM
239641	MMSL
370214004	SNOMEDCT_US
4021297	VUID
4021297	VANDF
411990007	SNOMEDCT_US

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Pharmaceutical products:

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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
FROVA	HUMAN PRESCRIPTION DRUG LABEL	1	63481-025	TABLET, FILM COATED	2.50 mg	ORAL	NDA	25 sections
Frovatriptan	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3140	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	26 sections
Frovatriptan	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3140	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	26 sections
FROVATRIPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	50742-299	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	23 sections
FROVATRIPTAN	HUMAN PRESCRIPTION DRUG LABEL	1	50742-299	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	23 sections
Frovatriptan	HUMAN PRESCRIPTION DRUG LABEL	1	69238-1539	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	0603-3718	TABLET, FILM COATED	2.50 mg	ORAL	NDA	25 sections
frovatriptan succinate	HUMAN PRESCRIPTION DRUG LABEL	1	68462-694	TABLET, FILM COATED	2.50 mg	ORAL	ANDA	25 sections

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