General Information of Drug (ID: DMH21D9)

Drug Name
Ebastine Drug Info
Synonyms
ebastine; Kestine; Ebastel; Ebastin; Evastel; Kestin; Bactil; Ebastinum [Latin]; LAS W-090; Ebastina [Spanish]; Estivan; UNII-TQD7Q784P1; RP 64305; 1-(4-tert-butylphenyl)-4-[4-(diphenylmethoxy)piperidin-1-yl]butan-1-one; TQD7Q784P1; CHEMBL305660; 4-Diphenylmethoxy-1-(3-(4-tert-butylbenzoyl)propyl)piperidine; C32H39NO2; MFCD00865661; 1-[4-(1,1-Dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone; NCGC00164603-01; RP-64305; 4'-tert-Butyl-4-(4-(diphenylmethoxy)piperidino)butyrophenone
Cross-matching ID
PubChem CID
3191
ChEBI ID
CHEBI:31528
CAS Number
CAS 90729-43-4
TTD Drug ID
DMH21D9
VARIDT Drug ID
DR01688

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [1]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [8]
Methotrexate DM2TEOL Anterior urethra cancer Approved [9]
Folic Acid DMEMBJC Colorectal carcinoma Approved [10]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [9]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [9]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [11]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [9]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [12]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [13]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [14]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [17]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [18]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [19]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [20]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [21]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [15]
Verapamil DMA7PEW Angina pectoris BA40 Approved [22]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 4F2 (CYP4F2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [23]
Fingolimod DM5JVAN Multiple sclerosis 8A40 Approved [24]
Pafuramidine DMFKOR9 Malaria 1F40-1F45 Phase 3 [25]
Tocopherol DMBIJZ6 N. A. N. A. Phase 2 [26]
GSK618334 DMJPXZ4 Drug abuse 6C4G.1Z Phase 1 [27]
Arachidonic Acid DMUOQZD Discovery agent N.A. Investigative [28]
⏷ Show the Full List of 6 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2J2 (CYP2J2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Riociguat DMXBLMP Chronic thromboembolic pulmonary hypertension Approved [29]
Rivaroxaban DMQMBZ1 Deep vein thrombosis BD71 Approved [30]
Ergocalciferol DMHO0AR Hypoparathyroidism 5A50 Approved [31]
Vorapaxar DMA16BR Myocardial infarction BA41-BA43 Approved [32]
Vitamin D DMWQUC9 N. A. N. A. Approved [31]
Alfacalcidol DM1237M Hyperparathyroidism 5A51 Phase 4 [31]
MANIDIPINE DMJPGUA N. A. N. A. Phase 3 [33]
Carebastine DMUVMWZ Ocular allergy 4A81 Phase 3 [2]
Eperisone DM1SMAI Muscle spasm MB47.3 Phase 3 [34]
H3B-6545 DMIFCY2 Breast cancer 2C60-2C65 Phase 1/2 [35]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [33]
Quercetin DM3NC4M Obesity 5B81 Approved [51]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [52]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [53]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [54]
Nisoldipine DM7ISKJ Hypertension BA00-BA04 Approved [33]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [55]
Amlodipine DMBDAZV Angina pectoris BA40 Approved [33]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [56]
Gemfibrozil DMD8Q3J Hyperlipidaemia 5C80 Approved [57]
⏷ Show the Full List of 20 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bepridil DM0RKS4 Chronic/stable angina BA40.1 Approved [36]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [37]
Pergolide mesylate DM5GKOV N. A. N. A. Approved [38]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [39]
Decitabine DMQL8XJ Acute myelogenous leukaemia 2A41 Approved [40]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [41]
Carbamazepine DMZOLBI Epilepsy 8A60-8A68 Approved [39]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [42]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [42]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [43]
Quinidine DMLPICK N. A. N. A. Approved [44]
Verapamil DMA7PEW Angina pectoris BA40 Approved [45]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [46]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [46]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [47]
Propranolol DM79NTF Angina pectoris BA40 Approved [48]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [49]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [50]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [46]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [2]
Cytochrome P450 2J2 (CYP2J2) DERSX5P CP2J2_HUMAN Substrate [3]
Cytochrome P450 4F2 (CYP4F2) DE3GT9C CP4F2_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 2J2 (CYP2J2) OTJBTEH8 CP2J2_HUMAN Biotransformations [5]
Potassium voltage-gated channel subfamily A member 5 (KCNA5) OTHI2N71 KCNA5_HUMAN Gene/Protein Processing [6]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [7]

References

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5 Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole. Drug Metab Dispos. 2002 Nov;30(11):1240-5.
6 Comparative effects of nonsedating histamine H1 receptor antagonists, ebastine and terfenadine, on human Kv1.5 channels. Eur J Pharmacol. 1997 May 20;326(2-3):257-63. doi: 10.1016/s0014-2999(97)85421-0.
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10 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
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13 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
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16 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
17 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
18 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
19 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
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23 Cloning and characterization of CYP4F21: a prostaglandin E2 20-hydroxylase of ram seminal vesicles. Arch Biochem Biophys. 2001 May 1;389(1):123-9.
24 CYP4F enzymes are responsible for the elimination of fingolimod (FTY720), a novel treatment of relapsing multiple sclerosis. Drug Metab Dispos. 2011 Feb;39(2):191-8.
25 Human enteric microsomal CYP4F enzymes O-demethylate the antiparasitic prodrug pafuramidine. Drug Metab Dispos. 2007 Nov;35(11):2067-75.
26 Discovery, characterization, and significance of the cytochrome P450 omega-hydroxylase pathway of vitamin E catabolism. Ann N Y Acad Sci. 2004 Dec;1031:13-21.
27 Product information - Gilenya.
28 Role of cytochrome P450 enzymes in the bioactivation of polyunsaturated fatty acids. Biochim Biophys Acta. 2011 Jan;1814(1):210-22.
29 Riociguat (adempas): a novel agent for the treatment of pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension. P T. 2014 Nov;39(11):749-58.
30 Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar;103(3):572-85.
31 Characterization of rat and human CYP2J enzymes as Vitamin D 25-hydroxylases. Steroids. 2006 Oct;71(10):849-56.
32 Vorapaxar: the missing link in antiplatelet therapy! J Anaesthesiol Clin Pharmacol. 2017 Apr-Jun;33(2):269-270.
33 Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine. Chem Biol Interact. 2019 Jun 1;306:1-9.
34 Characterization of human cytochrome P450 enzymes involved in the biotransformation of eperisone. Xenobiotica. 2009 Jan;39(1):1-10.
35 Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERalpha covalent antagonist (SERCA). Cancer Chemother Pharmacol. 2019 Jan;83(1):151-160.
36 Inhibitory effect of bepridil on hKv1.5 channel current: comparison with amiodarone and E-4031. Eur J Pharmacol. 2001 Nov 2;430(2-3):149-57. doi: 10.1016/s0014-2999(01)01381-4.
37 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
38 Pergolide is an inhibitor of voltage-gated potassium channels, including Kv1.5, and causes pulmonary vasoconstriction. Circulation. 2005 Sep 6;112(10):1494-9. doi: 10.1161/CIRCULATIONAHA.105.556704. Epub 2005 Aug 29.
39 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
40 Acute hypersensitivity of pluripotent testicular cancer-derived embryonal carcinoma to low-dose 5-aza deoxycytidine is associated with global DNA Damage-associated p53 activation, anti-pluripotency and DNA demethylation. PLoS One. 2012;7(12):e53003. doi: 10.1371/journal.pone.0053003. Epub 2012 Dec 27.
41 Differential effects of estrogen and progesterone on potassium channels expressed in Xenopus oocytes. Steroids. 2008 Mar;73(3):272-9. doi: 10.1016/j.steroids.2007.10.010. Epub 2007 Nov 4.
42 Detection of potassium currents and regulation of multidrug resistance by potassium channels in human gastric cancer cells. Cell Biol Int. 2007 Jul;31(7):741-7. doi: 10.1016/j.cellbi.2007.01.008. Epub 2007 Jan 21.
43 Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
44 Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
45 Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
46 Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
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