Details of Drug-Metabolizing Enzyme (DME)
Full List of Drug(s) Metabolized by This DME | |||||
---|---|---|---|---|---|
Drugs Approved by FDA | Click to Show/Hide the Full List of Drugs: 29 Drugs | ||||
Darolutamide |
Drug Info | Approved | Prostate cancer | ICD11: 2C82 | [1] |
Tamoxifen citrate |
Drug Info | Approved | Breast cancer | ICD11: 2C60 | [2] |
Fospropofol disodium |
Drug Info | Approved | Monitored anaesthesia care | ICD11: N.A. | [3] |
Mycophenolate mofetil |
Drug Info | Approved | Crohn disease | ICD11: DD70 | [4] |
Aprepitant |
Drug Info | Approved | Functional nausea/vomiting | ICD11: DD90 | [5] |
Mirabegron |
Drug Info | Approved | Overactive bladder | ICD11: GC50 | [6] |
Opicapone |
Drug Info | Approved | Parkinsonism | ICD11: 8A00 | [7] |
Formoterol |
Drug Info | Approved | Asthma | ICD11: CA23 | [8] |
Lasofoxifene |
Drug Info | Approved | Osteoporosis | ICD11: FB83 | [9] |
Morphine |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [10], [11], [12] |
Etravirine |
Drug Info | Approved | Human immunodeficiency virus infection | ICD11: 1C60 | [13] |
Intedanib |
Drug Info | Approved | Idiopathic pulmonary fibrosis | ICD11: CB03 | [14] |
Nalmefene |
Drug Info | Approved | Opiate dependence | ICD11: 6C43 | [15] |
Propofol |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [16] |
Raloxifene |
Drug Info | Approved | Osteoporosis | ICD11: FB83 | [17] |
Tramadol hydrochloride |
Drug Info | Approved | Neuropathic pain | ICD11: 8E43 | [18] |
Candesartan cilexetil |
Drug Info | Approved | Essential hypertension | ICD11: BA00 | [19] |
Empagliflozin |
Drug Info | Approved | Diabetes mellitus | ICD11: 5A10 | [20] |
Mycophenolic acid |
Drug Info | Approved | Crohn disease | ICD11: DD70 | [10], [21] |
Mycophenolic acid |
Drug Info | Approved | Crohn disease | ICD11: DD70 | [22] |
Troglitazone |
Drug Info | Approved | Diabetes mellitus | ICD11: 5A10 | [23] |
Bicalutamide |
Drug Info | Approved | Prostate cancer | ICD11: 2C82 | [24] |
Edaravone |
Drug Info | Approved | Cerebral stroke | ICD11: 8B11 | [25] |
Vorinostat |
Drug Info | Approved | Cutaneous T-cell lymphoma | ICD11: 2B01 | [26] |
Fulvestrant |
Drug Info | Approved | Breast cancer | ICD11: 2C60 | [27] |
Gaboxadol |
Drug Info | Approved | Insomnia | ICD11: 7A00-7A0Z | [28] |
Telmisartan |
Drug Info | Approved | Essential hypertension | ICD11: BA00 | [29] |
Telmisartan |
Drug Info | Approved | Essential hypertension | ICD11: BA00 | [30] |
LAROPIPRANT |
Drug Info | Phase 4 | Atherosclerosis | ICD11: BA80 | [31] |
Drugs in Phase 4 Clinical Trial | Click to Show/Hide the Full List of Drugs: 1 Drugs | ||||
Bazedoxifene |
Drug Info | Phase 4 | Schizophrenia | ICD11: 6A20 | [32] |
Drugs in Phase 3 Clinical Trial | Click to Show/Hide the Full List of Drugs: 3 Drugs | ||||
AKB-6548 |
Drug Info | Phase 3 | Anaemia | ICD11: 3A90 | [33] |
Curcumin |
Drug Info | Phase 3 | Stomach cancer | ICD11: 2B72 | [34] |
Heroin |
Drug Info | Phase 3 | Opiate dependence | ICD11: 6C43 | [35] |
Drugs in Phase 2 Clinical Trial | Click to Show/Hide the Full List of Drugs: 8 Drugs | ||||
Puerarin |
Drug Info | Phase 2 | Alcohol dependence | ICD11: 6C40 | [36] |
BAICALEIN |
Drug Info | Phase 2 | Influenza virus infection | ICD11: 1E30-1E32 | [37] |
BIA 3-202 |
Drug Info | Phase 2 | Parkinsonism | ICD11: 8A00 | [38] |
(Z)-endoxifen |
Drug Info | Phase 2 | Breast cancer | ICD11: 2C60-2C6Y | [39] |
Endoxifen |
Drug Info | Phase 2 | Breast cancer | ICD11: 2C60-2C6Y | [39] |
ABT-751 |
Drug Info | Phase 2 | Breast cancer | ICD11: 2C60 | [40] |
AR-67 |
Drug Info | Phase 2 | Brain cancer | ICD11: 2A00 | [41] |
ICI-79,280 |
Drug Info | Phase 2 | Ductal carcinoma | ICD11: 2E65 | [42] |
Drugs in Phase 1 Clinical Trial | Click to Show/Hide the Full List of Drugs: 2 Drugs | ||||
BRN-0183227 |
Drug Info | Phase 1 | Acute coronary syndrome | ICD11: BA4Z | [43] |
OTSSP167 |
Drug Info | Phase 1 | Myelodysplastic syndrome | ICD11: 2A37 | [44] |
Discontinued/withdrawn Drugs | Click to Show/Hide the Full List of Drugs: 3 Drugs | ||||
Darexaban maleate |
Drug Info | Discontinued in Phase 3 | Acute coronary syndrome | ICD11: BA41-BA43 | [45] |
Lexacalcitol |
Drug Info | Discontinued in Phase 2 | Solid tumour/cancer | ICD11: 2A00-2F9Z | [46], [47] |
T-5224 |
Drug Info | Discontinued in Phase 2 | Rheumatoid arthritis | ICD11: FA20 | [48] |
Preclinical/investigative Agents | Click to Show/Hide the Full List of Drugs: 7 Drugs | ||||
Eugenol |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [34] |
Hydroxyestrone |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [49] |
Phloretin |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [34] |
Chrysin |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [34] |
Cis-4-hydroxytamoxifen |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [42] |
Hydroxyestradiol |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [49] |
Anthraflavic acid |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [34] |
Experimental Enzyme Kinetic Data of Drugs | Click to Show/Hide the Full List of Drugs: 7 Drugs | ||||
Curcumin |
Drug Info | Phase 3 | Stomach cancer | Km = 0.1 microM | [34] |
ICI-79,280 |
Drug Info | Phase 2 | Ductal carcinoma | Km = 0.004 microM | [42] |
Eugenol |
Drug Info | Investigative | Discovery agent | Km = 0.0084 microM | [34] |
Phloretin |
Drug Info | Investigative | Discovery agent | Km = 0.0068 microM | [34] |
Chrysin |
Drug Info | Investigative | Discovery agent | Km = 0.004 microM | [34] |
Cis-4-hydroxytamoxifen |
Drug Info | Investigative | Discovery agent | Km = 0.0074 microM | [42] |
Anthraflavic acid |
Drug Info | Investigative | Discovery agent | Km = 0.01 microM | [34] |
References | |||||
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1 | Drug-drug interaction potential of darolutamide: in vitro and clinical studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759. | ||||
2 | PharmGKB:Tamoxifen citrate | ||||
3 | Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects | ||||
4 | PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9. | ||||
5 | In vitro glucuronidation of aprepitant: a moderate inhibitor of UGT2B7 Xenobiotica. 2015;45(11):990-8. doi: 10.3109/00498254.2015.1038743. | ||||
6 | Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective (3)-Adrenoceptor Agonist, in Human Liver Microsomes | ||||
7 | Metabolism and disposition of opicapone in the rat and metabolic enzymes phenotyping | ||||
8 | FDA Approved Drug Products: Perforomist? inhalation solution | ||||
9 | DrugBank(Pharmacology-Metabolism):Lasofoxifene | ||||
10 | Pharmacogenomics knowledge for personalized medicine Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96. | ||||
11 | Metabolism and pharmacokinetics of morphine in neonates: A review | ||||
12 | Morphine metabolism, transport and brain disposition | ||||
13 | Biotransformation of the antiretroviral drug etravirine: metabolite identification, reaction phenotyping, and characterization of autoinduction of cytochrome P450-dependent metabolism. Drug Metab Dispos. 2012 Apr;40(4):803-14. | ||||
14 | Characterization of Enzymes Involved in Nintedanib Metabolism in Humans | ||||
15 | Ema.europa:Nalmefene | ||||
16 | Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development Curr Med Chem. 2009;16(27):3480-675. doi: 10.2174/092986709789057635. | ||||
17 | Raloxifene glucuronidation in liver and intestinal microsomes of humans and monkeys: contribution of UGT1A1, UGT1A8 and UGT1A9 | ||||
18 | DrugBank : Tramadol hydrochloride | ||||
19 | The human UDP-glucuronosyltransferase UGT1A3 is highly selective towards N2 in the tetrazole ring of losartan, candesartan, and zolarsartan Biochem Pharmacol. 2008 Sep 15;76(6):763-72. doi: 10.1016/j.bcp.2008.07.006. | ||||
20 | Empagliflozin (Jardiance): a novel SGLT2 inhibitor for the treatment of type-2 diabetes. P T. 2015 Jun;40(6):364-8. | ||||
21 | The main role of UGT1A9 in the hepatic metabolism of mycophenolic acid and the effects of naturally occurring variants | ||||
22 | Identification of the UDP-glucuronosyltransferase isoforms involved in mycophenolic acid phase II metabolism. Drug Metab Dispos. 2005 Jan;33(1):139-46. | ||||
23 | Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9. | ||||
24 | Enantiomer selective glucuronidation of the non-steroidal pure anti-androgen bicalutamide by human liver and kidney: role of the human UDP-glucuronosyltransferase (UGT)1A9 enzyme Basic Clin Pharmacol Toxicol. 2013 Aug;113(2):92-102. doi: 10.1111/bcpt.12071. | ||||
25 | LABEL:ADICAVA- edaravone injection RADICAVA ORS- edaravone kit | ||||
26 | Uridine 5'-diphospho-glucuronosyltransferase genetic polymorphisms and response to cancer chemotherapy. Future Oncol. 2010 Apr;6(4):563-85. | ||||
27 | Inactivation of the pure antiestrogen fulvestrant and other synthetic estrogen molecules by UDP-glucuronosyltransferase 1A enzymes expressed in breast tissue. Mol Pharmacol. 2006 Mar;69(3):908-20. | ||||
28 | Metabolism and renal elimination of gaboxadol in humans: role of UDP-glucuronosyltransferases and transporters | ||||
29 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin Drug Metab Dispos. 2012 Apr;40(4):825-35. doi: 10.1124/dmd.111.043984. | ||||
30 | In vitro glucuronidation of the angiotensin II receptor antagonist telmisartan in the cat: a comparison with other species | ||||
31 | Metabolism of MK-0524, a prostaglandin D2 receptor 1 antagonist, in microsomes and hepatocytes from preclinical species and humans | ||||
32 | UGT1A1*28 polymorphism influences glucuronidation of bazedoxifene Pharmazie. 2015 Feb;70(2):94-6. | ||||
33 | DrugBank(Pharmacology-Metabolism):AKB-6548 | ||||
34 | Differential and special properties of the major human UGT1-encoded gastrointestinal UDP-glucuronosyltransferases enhance potential to control chemical uptake. J Biol Chem. 2004 Jan 9;279(2):1429-41. | ||||
35 | PharmGKB:Heroin | ||||
36 | UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for puerarin metabolism in human liver microsomes | ||||
37 | Involvement of UDP-glucuronosyltransferases in the extensive liver and intestinal first-pass metabolism of flavonoid baicalein | ||||
38 | Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation | ||||
39 | Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen | ||||
40 | Preclinical discovery of candidate genes to guide pharmacogenetics during phase I development: the example of the novel anticancer agent ABT-751. Pharmacogenet Genomics. 2013 Jul;23(7):374-81. | ||||
41 | Metabolic pathways of the camptothecin analog AR-67 | ||||
42 | Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2006-14. | ||||
43 | Stratification of Volunteers According to Flavanone Metabolite Excretion and Phase II Metabolism Profile after Single Doses of 'Pera' Orange and 'Moro' Blood Orange Juices | ||||
44 | Glucuronidation of OTS167 in Humans Is Catalyzed by UDP-Glucuronosyltransferases UGT1A1, UGT1A3, UGT1A8, and UGT1A10 | ||||
45 | Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine | ||||
46 | Metabolism of 1,8-cineole by human cytochrome P450 enzymes: identification of a new hydroxylated metabolite. Biochim Biophys Acta. 2005 Apr 15;1722(3):304-11. doi: 10.1016/j.bbagen.2004.12.019. | ||||
47 | Performance comparison between multienzymes loaded single and dual electrodes for the simultaneous electrochemical detection of adenosine and metabolites in cancerous cells. Biosens Bioelectron. 2018 Jun 30;109:263-271. doi: 10.1016/j.bios.2018.03.031. | ||||
48 | Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms | ||||
49 | Structural and functional studies of UDP-glucuronosyltransferases. Drug Metab Rev. 1999 Nov;31(4):817-99. | ||||
50 | Metabolic profile, enzyme kinetics, and reaction phenotyping of -lapachone metabolism in human liver and intestine in vitro | ||||
51 | Hepatic metabolism and disposition of baicalein via the coupling of conjugation enzymes and transporters-in vitro and in vivo evidences | ||||
52 | UGT1A1*28 polymorphism influences glucuronidation of bazedoxifene. Pharmazie. 2015 Feb;70(2):94-6. | ||||
53 | Dailymed:Bicalutamide | ||||
54 | Absorption, metabolism and excretion of darexaban (YM150), a new direct factor Xa inhibitor in humans | ||||
55 | Pharmacokinetics, Pharmacodynamics and Clinical Use of SGLT2 Inhibitors in Patients with Type 2 Diabetes Mellitus and Chronic Kidney Disease | ||||
56 | Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet. 2009;48(9):561-74. | ||||
57 | Mass balance and metabolism of [(3)H]Formoterol in healthy men after combined i.v. and oral administration-mimicking inhalation Drug Metab Dispos. 1999 Oct;27(10):1104-16. | ||||
58 | DrugBank : Formoterol | ||||
59 | Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. | ||||
60 | Isolation of a novel morphinan 3-O-diglucuronide metabolite from dog urine | ||||
61 | Determination of raloxifene and its glucuronides in human urine by liquid chromatography-tandem mass spectrometry assay | ||||
62 | Pharmacokinetics of raloxifene and its clinical application | ||||
63 | Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albumin. Drug Metab Dispos. 2012 Apr;40(4):825-35. | ||||
64 | Clinical pharmacokinetics of troglitazone Clin Pharmacokinet. 1999 Aug;37(2):91-104. doi: 10.2165/00003088-199937020-00001. | ||||
65 | Stability studies of vorinostat and its two metabolites in human plasma, serum and urine |
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