General Information of Drug (ID: DM74XKS)

Drug Name
Ketotifen Drug Info
Synonyms
Ketotifen [INN:BAN]; Ketotifene; Ketotifene [INN-French]; Ketotifeno; Ketotifeno [INN-Spanish]; Ketotifenum; Ketotifenum [INN-Latin]; HC 20-511; ZCVMWBYGMWKGHF-UHFFFAOYSA-N; Zaditor; ketotifen; 34580-13-7; 4,9-Dihydro-4-(1-methyl-4-piperidinylidene)-10H-benzo(4,5)cyclohepta(1,2-b)thiophen-10-one; 4-(1-methylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one; BRN 3983897; CHEMBL534; EINECS 252-099-7; HSDB 7283; UNII-X49220T18G
Indication
Disease Entry ICD 11 Status REF
Allergic conjunctivitis 9A60.02 Approved [1]
Cross-matching ID
PubChem CID
3827
ChEBI ID
CHEBI:92511
CAS Number
CAS 34580-13-7
TTD Drug ID
DM74XKS
INTEDE Drug ID
DR2514

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Drug(s) Targeting Histamine H1 receptor (H1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [5]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [6]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [2]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [7]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [8]
Diphenhydramine DMKQTBA Hyperemesis gravidarum Approved [2]
Doxepin DMPI98T Anxiety Approved [9]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [2]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [10]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [12]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [13]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [14]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [15]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [16]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [17]
Quercetin DM3NC4M Obesity 5B81 Approved [18]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [19]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [20]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [18]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [22]
Fructose DM43AN2 Vomiting MD90 Approved [23]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [24]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [25]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [26]
Riboflavin DM8YMWE Acne vulgaris ED80 Approved [27]
Leflunomide DMR8ONJ Arthritis FA20 Approved [28]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [27]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [29]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Substrate []
UDP-glucuronosyltransferase 1A4 (UGT1A4) DELOY3P UD14_HUMAN Substrate []
UDP-glucuronosyltransferase 2B10 (UGT2B10) DEI8NGH UDB10_HUMAN Substrate []
Short-chain dehydrogenase/reductase SDR19C1 (DHRS1) DE1LZID DHRS1_HUMAN Substrate [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PPARGC1A) OTHCDQ22 PRGC1_HUMAN Gene/Protein Processing [4]
Sterol regulatory element-binding protein 1 (SREBF1) OTWBRPAI SRBP1_HUMAN Gene/Protein Processing [4]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7206).
2 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
3 Initial characterization of human DHRS1 (SDR19C1), a member of the short-chain dehydrogenase/reductase superfamily. J Steroid Biochem Mol Biol. 2019 Jan;185:80-89.
4 Advantageous use of HepaRG cells for the screening and mechanistic study of drug-induced steatosis. Toxicol Appl Pharmacol. 2016 Jul 1;302:1-9. doi: 10.1016/j.taap.2016.04.007. Epub 2016 Apr 16.
5 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
6 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
7 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
8 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
9 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
10 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
11 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
12 Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
13 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
14 Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
15 Poly(ADP-Ribose) Polymerase Inhibitor PJ34 Attenuated Hepatic Triglyceride Accumulation in Alcoholic Fatty Liver Disease in Mice. J Pharmacol Exp Ther. 2018 Mar;364(3):452-461. doi: 10.1124/jpet.117.243105. Epub 2018 Jan 9.
16 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
17 Delta5 desaturase mRNA levels are increased by simvastatin via SREBP-1 at early stages, not via PPARalpha, in THP-1 cells. Eur J Pharmacol. 2007 Oct 1;571(2-3):97-105.
18 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
19 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
20 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
21 Inhibition of liver x receptor/retinoid X receptor-mediated transcription contributes to the proatherogenic effects of arsenic in macrophages in vitro. Arterioscler Thromb Vasc Biol. 2010 Jun;30(6):1228-36. doi: 10.1161/ATVBAHA.110.205500. Epub 2010 Mar 25.
22 Troglitazone induces cytotoxicity in part by promoting the degradation of peroxisome proliferator-activated receptor co-activator-1 protein. Br J Pharmacol. 2010 Oct;161(4):771-81. doi: 10.1111/j.1476-5381.2010.00900.x.
23 Effects of four-week high-fructose diet on gene expression in skeletal muscle of healthy men. Diabetes Metab. 2008 Feb;34(1):82-5. doi: 10.1016/j.diabet.2007.08.004. Epub 2007 Dec 11.
24 Glucosamine-induced endoplasmic reticulum stress affects GLUT4 expression via activating transcription factor 6 in rat and human skeletal muscle cells. Diabetologia. 2010 May;53(5):955-65. doi: 10.1007/s00125-010-1676-1. Epub 2010 Feb 18.
25 AMPK activator acadesine fails to alleviate isoniazid-caused mitochondrial instability in HepG2 cells. J Appl Toxicol. 2017 Oct;37(10):1219-1224. doi: 10.1002/jat.3483. Epub 2017 May 29.
26 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
27 A cardiac-specific robotized cellular assay identified families of human ligands as inducers of PGC-1 expression and mitochondrial biogenesis. PLoS One. 2012;7(10):e46753. doi: 10.1371/journal.pone.0046753. Epub 2012 Oct 3.
28 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
29 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.