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

Stem definition	Drug id	CAS RN
	1530	34580-13-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: HC 20-511 ketotifen ketotifen fumarate	A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis. Molecular weight: 309.43 Formula: C19H19NOS CLOGP: 3.59 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 20.31 ALOGS: -4.59 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

HC 20-511
ketotifen
ketotifen fumarate

A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.

Molecular weight: 309.43
Formula: C19H19NOS
CLOGP: 3.59
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 20.31
ALOGS: -4.59
ROTB: 0

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2	mg	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	60 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	10 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.09 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
July 2, 1999	FDA

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
Treatment failure	1095.86	23.34	448	4477	198595	63285502
Mastocytosis	89.74	23.34	18	4907	568	63483529
Urticaria	74.08	23.34	77	4848	165725	63318372
Perfume sensitivity	72.83	23.34	16	4909	789	63483308
Mast cell activation syndrome	72.43	23.34	16	4909	809	63483288
Angioedema	49.53	23.34	36	4889	47929	63436168
Mechanical urticaria	46.06	23.34	10	4915	466	63483631
Anaphylactic reaction	45.37	23.34	39	4886	66061	63418036
Dysphemia	45.19	23.34	14	4911	2661	63481436
Lipohypertrophy	42.73	23.34	10	4915	655	63483442

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FDA Adverse Event Reporting System (Male)

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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
Treatment failure	602.85	29.38	173	1391	46524	34908843
Mast cell activation syndrome	51.25	29.38	9	1555	241	34955126
Anaphylactic reaction	47.89	29.38	25	1539	32276	34923091
Tendon disorder	47.19	29.38	13	1551	2862	34952505
Exostosis	44.98	29.38	14	1550	4709	34950658
Ankle fracture	42.55	29.38	13	1551	4112	34951255
Foot deformity	41.33	29.38	13	1551	4524	34950843
Foot fracture	40.06	29.38	13	1551	4998	34950369
Application site eczema	39.27	29.38	5	1559	11	34955356
Application site oedema	35.21	29.38	5	1559	31	34955336

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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
Mastocytosis	88.28	20.69	17	5114	525	79738732
Urticaria	77.13	20.69	76	5055	185125	79554132
Perfume sensitivity	74.40	20.69	16	5115	863	79738394
Mast cell activation syndrome	66.02	20.69	14	5117	706	79738551
Anaphylactic reaction	58.19	20.69	46	5085	83697	79655560
Mechanical urticaria	54.65	20.69	11	5120	428	79738829
Pruritus	50.97	20.69	91	5040	394557	79344700
Lipohypertrophy	41.76	20.69	10	5121	874	79738383
Application site eczema	38.88	20.69	5	5126	7	79739250
Skin plaque	34.98	20.69	16	5115	10729	79728528

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R06AX17	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
ATC	S01GX08	SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:49167	anti-asthmatic drugs
FDA EPC	N0000175519	Histamine-1 Receptor Inhibitor
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D018494	Histamine Agents

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

Disease	Relation	SNOMED_ID	DOID
Allergic conjunctivitis	indication	473460002	DOID:11204

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.8	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 19MCG BASE	ACUVUE THERAVISION WITH KETOTIFEN	JOHNSON JOHNSON VISN	N022388	Feb. 25, 2022	DISCN	DRUG-ELUTING CONTACT LENS	OPHTHALMIC	Feb. 25, 2025	NEW PRODUCT

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	9.51	WOMBAT-PK	CHEMBL
Histamine H4 receptor	GPCR	Q9H3N8	HRH4_HUMAN		IC50	4.68	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	6.36	DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.09	DRUG MATRIX
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN				WOMBAT-PK
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.84	DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	8.05	DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	7.54	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.08	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.28	DRUG MATRIX

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External reference:

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ID	Source
003742	NDDF
003743	NDDF
11404	RXNORM
116098000	SNOMEDCT_US
34580-14-8	SECONDARY_CAS_RN
354038002	SNOMEDCT_US
365752	MMSL
372642003	SNOMEDCT_US
3827	PUBCHEM_CID
3993	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Alaway	HUMAN OTC DRUG LABEL	1	24208-601	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	NDA	12 sections
Alaway	HUMAN OTC DRUG LABEL	1	24208-601	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	NDA	12 sections
Alaway Preservative Free	HUMAN OTC DRUG LABEL	1	24208-600	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	10 sections
Alaway Preservative Free	HUMAN OTC DRUG LABEL	1	24208-600	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	10 sections
Allergy Eye Drops	HUMAN OTC DRUG LABEL	1	37808-870	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Equate Eye Itch Relief	HUMAN OTC DRUG LABEL	1	49035-231	SOLUTION	0.25 mg	OPHTHALMIC	NDA	9 sections
Eye Itch	HUMAN OTC DRUG LABEL	1	30142-702	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Eye Itch	HUMAN OTC DRUG LABEL	1	41250-302	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Eye Itch Releif	HUMAN OTC DRUG LABEL	1	11822-5533	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	NDA	12 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	0363-0038	SOLUTION	0.35 mg	OPHTHALMIC	NDA	10 sections

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