ketotifen ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
1530 34580-13-7

Description:

MoleculeDescription

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:

DoseUnitRoute
2 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.09 ยตM/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:

DateAgencyCompanyOrphan
July 2, 1999 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
Allergic conjunctivitis indication 473460002 DOID:11204




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.8 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 9.51 WOMBAT-PK CHEMBL
Histamine H4 receptor GPCR IC50 4.68 CHEMBL
D(1A) dopamine receptor GPCR Ki 6.36 DRUG MATRIX
Alpha-2A adrenergic receptor GPCR Ki 6.09 DRUG MATRIX
Multidrug resistance protein 1 Transporter WOMBAT-PK
5-hydroxytryptamine receptor 1A GPCR Ki 5.84 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 8.05 DRUG MATRIX
5-hydroxytryptamine receptor 2B GPCR Ki 7.54 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 7.08 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 6.28 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.49 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.18 DRUG MATRIX
Histamine H2 receptor GPCR Ki 5.39 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 7.02 WOMBAT-PK
Muscarinic acetylcholine receptor M3 GPCR Ki 6.58 WOMBAT-PK
Muscarinic acetylcholine receptor M4 GPCR Ki 7.08 WOMBAT-PK
Muscarinic acetylcholine receptor M5 GPCR Ki 7.73 WOMBAT-PK
Alpha-1D adrenergic receptor GPCR Ki 5.74 DRUG MATRIX
Muscarinic acetylcholine receptor M2 GPCR Ki 6.36 WOMBAT-PK
Histamine H1 receptor GPCR Ki 9.51 CHEMBL
5-hydroxytryptamine receptor 1A GPCR IC50 5.60 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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