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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:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.09 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
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

Approvals:

Date	Agency	Company	Orphan
July 2, 1999	FDA

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
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
Muscle tension dysphonia	41.45	23.34	8	4917	206	63483891
Food intolerance	38.24	23.34	13	4912	3312	63480785
Pruritus	37.64	23.34	85	4840	361368	63122729
Skin plaque	36.04	23.34	16	4909	8304	63475793
Oral pruritus	34.57	23.34	11	4914	2280	63481817
Conjunctivitis allergic	34.40	23.34	9	4916	933	63483164
Vaccination complication	32.42	23.34	9	4916	1168	63482929
Eye inflammation	31.64	23.34	13	4912	5586	63478511
Skin reaction	29.94	23.34	17	4908	14832	63469265
Dysphoria	29.67	23.34	12	4913	4954	63479143
Scratch	29.64	23.34	13	4912	6552	63477545
Oropharyngeal discomfort	29.00	23.34	12	4913	5248	63478849
Skin warm	28.53	23.34	12	4913	5464	63478633
Immunisation reaction	27.81	23.34	7	4918	623	63483474
Haemorrhagic diathesis	27.52	23.34	11	4914	4404	63479693
Osteoporotic fracture	25.69	23.34	10	4915	3736	63480361
Visual impairment	25.37	23.34	32	4893	84414	63399683
Appetite disorder	25.19	23.34	12	4913	7309	63476788
Arthritis infective	23.46	23.34	11	4914	6467	63477630

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
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
Episcleritis	33.38	29.38	6	1558	184	34955183
Vertigo positional	29.66	29.38	7	1557	831	34954536

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
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
Dysphemia	32.06	20.69	11	5120	3473	79735784
Muscle tension dysphonia	31.72	20.69	6	5125	168	79739089
Oral pruritus	31.68	20.69	10	5121	2438	79736819
Angioedema	31.20	20.69	31	5100	76004	79663253
Food intolerance	30.99	20.69	11	5120	3837	79735420
Tendon disorder	30.85	20.69	13	5118	7173	79732084
Dacryostenosis acquired	30.03	20.69	7	5124	545	79738712
Scratch	28.95	20.69	13	5118	8350	79730907
Skin reaction	28.88	20.69	16	5115	16052	79723205
Application site oedema	28.81	20.69	5	5126	85	79739172
Dysphoria	28.77	20.69	11	5120	4723	79734534
Vaccination complication	26.84	20.69	7	5124	866	79738391
Appetite disorder	26.70	20.69	12	5119	7727	79731530
Osteoporotic fracture	26.30	20.69	10	5121	4230	79735027
Eye inflammation	25.54	20.69	11	5120	6402	79732855
Exostosis	25.51	20.69	15	5116	16843	79722414
Immunisation reaction	25.38	20.69	6	5125	496	79738761
Skin warm	25.18	20.69	11	5120	6621	79732636
Oropharyngeal discomfort	24.37	20.69	11	5120	7155	79732102
Asthma	23.92	20.69	36	5095	135059	79604198
Blood pressure increased	23.76	20.69	46	5085	211314	79527943
Visual impairment	23.02	20.69	29	5102	92102	79647155
Haemorrhagic diathesis	22.81	20.69	10	5121	6074	79733183
Osteoarthritis	22.64	20.69	28	5103	87281	79651976
pH body fluid increased	22.48	20.69	4	5127	79	79739178
Cardiac valve sclerosis	21.11	20.69	4	5127	113	79739144
Episcleritis	20.96	20.69	6	5125	1049	79738208

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
FDA EPC	N0000175519	Histamine-1 Receptor Inhibitor
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D018377	Neurotransmitter Agents
CHEBI has role	CHEBI:37955	H1 receptor antagonists
CHEBI has role	CHEBI:49167	anti-asthmatic drugs

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)

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

Bioactivity Summary:

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
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.49	DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.18	DRUG MATRIX
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.39	DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	7.02	WOMBAT-PK
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	6.58	WOMBAT-PK
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN		Ki	7.08	WOMBAT-PK
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	7.73	WOMBAT-PK
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	5.74	DRUG MATRIX
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	6.36	WOMBAT-PK
Histamine H1 receptor	GPCR		HRH1_CAVPO		Ki	9.51	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		IC50	5.60	CHEMBL

External reference:

ID	Source
4021170	VUID
N0000148619	NUI
D01332	KEGG_DRUG
34580-14-8	SECONDARY_CAS_RN
4021170	VANDF
4021171	VANDF
C0022642	UMLSCUI
CHEBI:92511	CHEBI
CHEMBL534	ChEMBL_ID
DB00920	DRUGBANK_ID
CHEMBL1633	ChEMBL_ID
D007665	MESH_DESCRIPTOR_UI
3827	PUBCHEM_CID
7206	IUPHAR_LIGAND_ID
3993	INN_ID
X49220T18G	UNII
11404	RXNORM
365752	MMSL
8247	MMSL
8249	MMSL
d04580	MMSL
003742	NDDF
003743	NDDF
116098000	SNOMEDCT_US
354038002	SNOMEDCT_US
372642003	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zaditor	HUMAN OTC DRUG LABEL	1	0065-4011	SOLUTION	0.25 mg	OPHTHALMIC	ANDA	13 sections
Zaditor	HUMAN OTC DRUG LABEL	1	0065-4011	SOLUTION	0.25 mg	OPHTHALMIC	ANDA	13 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	0363-0038	SOLUTION	0.35 mg	OPHTHALMIC	NDA	10 sections
EYE ITCH RELIEF	HUMAN OTC DRUG LABEL	1	0363-0610	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	ANDA	13 sections
Ketotifen Fumarate	HUMAN OTC DRUG LABEL	1	0363-9060	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	ANDA	13 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	0536-1096	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	14 sections
Ketotifen Fumarate	HUMAN OTC DRUG LABEL	1	0536-1252	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	NDA authorized generic	12 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	11673-064	SOLUTION	0.25 mg	OPHTHALMIC	NDA	9 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	11673-064	SOLUTION	0.25 mg	OPHTHALMIC	NDA	9 sections
LEADER EYE ITCH RELIEF DROPS	HUMAN OTC DRUG LABEL	1	11716-1163	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	OTC monograph final	20 sections
eye itch relief	HUMAN OTC DRUG LABEL	1	11822-4201	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
eye itch relief	HUMAN OTC DRUG LABEL	1	11822-4202	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
Ketotifen Fumarate	HUMAN OTC DRUG LABEL	1	17478-717	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Ketotifen Fumarate	HUMAN OTC DRUG LABEL	1	17478-717	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Ketotifen Fumarate	HUMAN OTC DRUG LABEL	1	17478-717	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	21130-601	SOLUTION	0.25 mg	OPHTHALMIC	NDA	11 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
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
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	30142-398	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	NDA	11 sections
Eye Itch	HUMAN OTC DRUG LABEL	1	30142-702	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	36800-097	SOLUTION/ DROPS	0.25 mg	OPHTHALMIC	NDA	10 sections
Eye Itch Relief	HUMAN OTC DRUG LABEL	1	37808-802	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections
Allergy Eye Drops	HUMAN OTC DRUG LABEL	1	37808-870	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
Itchy Eye	HUMAN OTC DRUG LABEL	1	41250-303	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	14 sections
Equate Eye Itch Relief	HUMAN OTC DRUG LABEL	1	49035-231	SOLUTION	0.25 mg	OPHTHALMIC	NDA	9 sections
eye itch relief	HUMAN OTC DRUG LABEL	1	49348-107	SOLUTION/ DROPS	0.35 mg	OPHTHALMIC	ANDA	13 sections