Details of Drug-Metabolizing Enzyme (DME)
| General Information of DME (ID: DMEN064) | |||||
|---|---|---|---|---|---|
| DME Name | UDP-glucuronyltransferase (UGT), . | ||||
| Gene Name | UGT | ||||
| Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME | |||||
| Full List of Drug(s) Metabolized by This DME | |||||
|---|---|---|---|---|---|
| Drugs Approved by FDA | Click to Show/Hide the Full List of Drugs: 11 Drugs | ||||
Erlotinib hydrochloride |
Drug Info | Approved | Lung cancer | ICD11: 2C25 | [1] |
Arbidol |
Drug Info | Approved | Virus infection | ICD11: 1A24-1D9Z | [2] |
Fostemsavir |
Drug Info | Approved | Human immunodeficiency virus infection | ICD11: 1C60-1C62 | [3] |
Desvenlafaxine |
Drug Info | Approved | Major depressive disorder | ICD11: 6A70-6A7Z | [4], [] |
Rilpivirine hydrochloride |
Drug Info | Approved | Human immunodeficiency virus infection | ICD11: 1C60 | [5] |
Levorphanol |
Drug Info | Approved | Pain | ICD11: MG30-MG3Z | [6] |
Oxycodone |
Drug Info | Approved | Pain | ICD11: MG30-MG3Z | [7] |
Troglitazone |
Drug Info | Approved | Diabetes mellitus | ICD11: 5A10 | [8] |
Osilodrostat |
Drug Info | Approved | Cushing syndrome | ICD11: 5A70 | [9] |
Migalastat |
Drug Info | Approved | Gaucher disease | ICD11: 5C56 | [10] |
3,4-Dihydroxycinnamic Acid |
Drug Info | Phase 4 | Thrombocytopenia | ICD11: 3B64 | [11] |
| Drugs in Phase 3 Clinical Trial | Click to Show/Hide the Full List of Drugs: 2 Drugs | ||||
SNS-595 |
Drug Info | Phase 3 | Acute myeloid leukaemia | ICD11: 2A60 | [12] |
Elagolix |
Drug Info | Phase 3 | Uterine leiomyoma | ICD11: 2E86 | [13] |
| Drugs in Phase 2 Clinical Trial | Click to Show/Hide the Full List of Drugs: 7 Drugs | ||||
Flupirtine |
Drug Info | Phase 2 | Cancer related pain | ICD11: MG30 | [14] |
Remogliflozin etabonate |
Drug Info | Phase 2 | Type-1/2 diabetes | ICD11: 5A10-5A11 | [15] |
BIA 3-202 |
Drug Info | Phase 2 | Parkinsonism | ICD11: 8A00 | [16] |
INX-189 |
Drug Info | Phase 2 | Hepatitis C virus infection | ICD11: 1E50-1E51 | [17] |
(Z)-endoxifen |
Drug Info | Phase 2 | Breast cancer | ICD11: 2C60-2C6Y | [18] |
Phenylbutyrate |
Drug Info | Phase 2 | Phenylketonuria | ICD11: 5C50 | [19] |
N-DESMETHYLCLOZAPINE |
Drug Info | Phase 2 | Schizophrenia | ICD11: 6A20 | [20] |
| Drugs in Phase 1 Clinical Trial | Click to Show/Hide the Full List of Drugs: 1 Drugs | ||||
STX 64 |
Drug Info | Phase 1 | Prostate cancer | ICD11: 2C82 | [21] |
| Discontinued/withdrawn Drugs | Click to Show/Hide the Full List of Drugs: 4 Drugs | ||||
Almokalant |
Drug Info | Discontinued in Phase 3 | Cardiac arrhythmias | ICD11: BC9Z | [22] |
R-ketoprofen |
Drug Info | Discontinued in Phase 2 | Discovery agent | ICD: N.A. | [23] |
Odapipam |
Drug Info | Discontinued in Phase 1 | Psychotic disorder | ICD11: 6A20-6A25 | [24] |
Berupipam |
Drug Info | Discontinued in Phase 1 | Psychotic disorder | ICD11: 6A20-6A25 | [24] |
| Preclinical/investigative Agents | Click to Show/Hide the Full List of Drugs: 1 Drugs | ||||
ACMC-1AKLT |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [25] |
| References | |||||
|---|---|---|---|---|---|
| 1 | Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. | ||||
| 2 | Glucuronidation of the broad-spectrum antiviral drug arbidol by UGT isoforms | ||||
| 3 | Pharmacokinetics of Temsavir, the Active Moiety of the HIV-1 Attachment Inhibitor Prodrug, Fostemsavir, Coadministered with Cobicistat, Etravirine, Darunavir/Cobicistat, or Darunavir/Ritonavir with or without Etravirine in Healthy Participants | ||||
| 4 | Influence of CYP2D6 genotype on the disposition of the enantiomers of venlafaxine and its major metabolites in postmortem femoral blood | ||||
| 5 | Human biotransformation of the nonnucleoside reverse transcriptase inhibitor rilpivirine and a cross-species metabolism comparison. Antimicrob Agents Chemother. 2013 Oct;57(10):5067-79. | ||||
| 6 | Metabolism and disposition of prescription opioids: a review. Forensic Sci Rev. 2015 Jul;27(2):115-45. | ||||
| 7 | Characterization of oxycodone in vitro metabolism by human cytochromes P450 and UDP-glucuronosyltransferases | ||||
| 8 | Comparative Pharmacokinetics and Safety of Imrecoxib, a Novel Selective Cyclooxygenase-2 Inhibitor, in Elderly Healthy Subjects. Drug Des Devel Ther. 2022 Nov 8;16:3865-3876. doi: 10.2147/DDDT.S387508. | ||||
| 9 | DrugBank(Pharmacology-Metabolism):Osilodrostat | ||||
| 10 | DrugBank(Pharmacology-Metabolism):Migalastat | ||||
| 11 | Absorption, disposition, metabolism, and excretion of [3-(14)C]caffeic acid in rats | ||||
| 12 | Metabolism of (+)-1,4-dihydro-7-(trans-3-methoxy-4-methylamino-1-pyrrolidinyl)-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid (voreloxin; formerly SNS-595), a novel replication-dependent DNA-damaging agent | ||||
| 13 | Quantitative Assessment of Elagolix Enzyme-Transporter Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling | ||||
| 14 | Investigation of the in vitro metabolism of the analgesic flupirtine | ||||
| 15 | Assessment of the drug interaction risk for remogliflozin etabonate, a sodium-dependent glucose cotransporter-2 inhibitor: evidence from in vitro, human mass balance, and ketoconazole interaction studies | ||||
| 16 | Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation | ||||
| 17 | In Vitro Metabolite Formation in Human Hepatocytes and Cardiomyocytes and Metabolism and Tissue Distribution in Monkeys of the 2'-C-Methylguanosine Prodrug BMS-986094 : Potential Role in Clinical Cardiovascular Toxicity | ||||
| 18 | Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen | ||||
| 19 | New secondary metabolites of phenylbutyrate in humans and rats | ||||
| 20 | Glucuronidation of the second-generation antipsychotic clozapine and its active metabolite N-desmethylclozapine. Potential importance of the UGT1A1 A(TA)?TAA and UGT1A4 L48V polymorphisms | ||||
| 21 | In vitro metabolism of irosustat, a novel steroid sulfatase inhibitor: interspecies comparison, metabolite identification, and metabolic enzyme identification | ||||
| 22 | Almokalant glucuronidation in human liver and kidney microsomes: evidence for the involvement of UGT1A9 and 2B7 | ||||
| 23 | Ketoprofen in horses: Metabolism, pharmacokinetics, and effects on inflammatory biomarkers | ||||
| 24 | Characterization of benzazepine UDP-glucuronosyl-transferases in laboratory animals and man | ||||
| 25 | Identification of UGT2B9*2 and UGT2B33 isolated from female rhesus monkey liver Arch Biochem Biophys. 2004 Jun 1;426(1):55-62. doi: 10.1016/j.abb.2004.03.035. | ||||
| 26 | An assessment of human liver-derived in vitro systems to predict the in vivo metabolism and clearance of almokalant | ||||
| 27 | Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors | ||||
| 28 | DrugBank(Pharmacology-Metabolism)Anastrozole | ||||
| 29 | Aromatic hydroxylation of salicylic acid and aspirin by human cytochromes P450. Eur J Pharm Sci. 2015 Jun 20;73:49-56. | ||||
| 30 | Polymorphisms of Aspirin-Metabolizing Enzymes CYP2C9, NAT2 and UGT1A6 in Aspirin-Intolerant Urticaria. Allergy Asthma Immunol Res. 2011 Oct;3(4):273-6. | ||||
| 31 | GDC-0810 Pharmacokinetics and Transporter-Mediated Drug Interaction Evaluation with an Endogenous Biomarker in the First-in-Human, Dose Escalation Study | ||||
| 32 | Predicting pharmacokinetics and drug interactions in patients from in vitro and in vivo models: the experience with 5,6-dimethylxanthenone-4-acetic acid (DMXAA), an anti-cancer drug eliminated mainly by conjugation. Drug Metab Rev. 2002 Nov;34(4):751-90. | ||||
| 33 | Preclinical factors affecting the interindividual variability in the clearance of the investigational anti-cancer drug 5,6-dimethylxanthenone-4-acetic acid. Biochem Pharmacol. 2003 Jun 1;65(11):1853-65. | ||||
| 34 | Hepatic metabolism and disposition of baicalein via the coupling of conjugation enzymes and transporters-in vitro and in vivo evidences | ||||
| 35 | Stereoselective pharmacokinetics of RS-8359, a selective and reversible MAO-A inhibitor, by species-dependent drug-metabolizing enzymes. Chirality. 2005 Mar;17(3):135-41. | ||||
| 36 | Evaluation of the Pharmacokinetic Interaction Between the Voltage- and Use-Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers | ||||
| 37 | Genistein: Dual Role in Women's Health | ||||
| 38 | FDA Label of Brexanolone | ||||
| 39 | Characterization of enzymes participating in carbonyl reduction of 4-methylnitrosamino-1-(3-pyridyl)-1-butanone (NNK) in human placenta. Chem Biol Interact. 2001 Jan 30;130-132(1-3):737-48. | ||||
| 40 | Quantitation of celecoxib and four of its metabolites in rat blood by UPLC-MS/MS clarifies their blood distribution patterns and provides more accurate pharmacokinetics profiles J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Sep 15;1001:202-11. doi: 10.1016/j.jchromb.2015.07.026. | ||||
| 41 | Celecoxib pathways: pharmacokinetics and pharmacodynamics. Pharmacogenet Genomics. 2012 Apr;22(4):310-8. | ||||
| 42 | Interaction of Chrysin and Its Main Conjugated Metabolites Chrysin-7-Sulfate and Chrysin-7-Glucuronide with Serum Albumin | ||||
| 43 | Comparative pharmacokinetic profile of cimicoxib in dogs and cats after IV administration | ||||
| 44 | Resveratrol Inhibits Key Steps of Steroid Metabolism in a Human Estrogen-Receptor Positive Breast Cancer Model: Impact on Cellular Proliferation Front Pharmacol. 2018 Jul 10;9:742. doi: 10.3389/fphar.2018.00742. | ||||
| 45 | 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. | ||||
| 46 | Differential effects of phenobarbital on ester and ether glucuronidation of diflunisal in rats. J Pharmacol Exp Ther. 1987 Sep;242(3):1013-8. | ||||
| 47 | Identification of a hydroxy metabolite of diflunisal in rat and human urine Xenobiotica. 1991 Nov;21(11):1521-33. doi: 10.3109/00498259109044402. | ||||
| 48 | Hydroxysteroid sulfotransferase and a specific UDP-glucuronosyltransferase are involved in the metabolism of digitoxin in man. Naunyn Schmiedebergs Arch Pharmacol. 1992 Aug;346(2):226-33. | ||||
| 49 | Metabolism of digoxin, digoxigenin digitoxosides and digoxigenin in human hepatocytes and liver microsomes Fundam Clin Pharmacol. 1991;5(7):567-82. doi: 10.1111/j.1472-8206.1991.tb00746.x. | ||||
| 50 | Non-invasive skin sampling detects systemically administered drugs in humans. PLoS One. 2022 Jul 26;17(7):e0271794. doi: 10.1371/journal.pone.0271794. | ||||
| 51 | FOODB:E-3A | ||||
| 52 | DrugBank(Pharmacology-Metabolism)Estradiol acetate | ||||
| 53 | DrugBank(Pharmacology-Metabolism):E-3A | ||||
| 54 | Comparative In vitro Metabolism of Enflicoxib in Dogs, Rats, and Humans: Main Metabolites and Proposed Metabolic Pathways | ||||
| 55 | Clinical pharmacokinetics and drug-drug interactions of Elbasvir/Grazoprevir. Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):509-531. | ||||
| 56 | The Activity of Members of the UDP-Glucuronosyltransferase Subfamilies UGT1A and UGT2B is Impaired in Patients with Liver Cirrhosis. Clin Pharmacokinet. 2023 Jun 16. doi: 10.1007/s40262-023-01261-3. | ||||
| 57 | FooDB:Estradiol acetate | ||||
| 58 | The metabolism of estradiol; oral compared to intravenous administration J Steroid Biochem. 1985 Dec;23(6A):1065-70. doi: 10.1016/0022-4731(85)90068-8. | ||||
| 59 | Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65. | ||||
| 60 | Pharmacokinetics, distribution, metabolism, and excretion of deferasirox and its iron complex in rats Drug Metab Dispos. 2008 Dec;36(12):2523-38. doi: 10.1124/dmd.108.022962. | ||||
| 61 | Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects | ||||
| 62 | 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. | ||||
| 63 | Techniques and technologies for the bioanalysis of Sativex?, metabolites and related compounds | ||||
| 64 | Hesperidin metabolite hesperetin-7-O-glucuronide, but not hesperetin-3'-O-glucuronide, exerts hypotensive, vasodilatory, and anti-inflammatory activities | ||||
| 65 | Involvement of phase II enzymes and efflux transporters in the metabolism and absorption of naringin, hesperidin and their aglycones in rats | ||||
| 66 | Potential industrial production of a well-soluble, alkaline-stable, and anti-inflammatory isoflavone glucoside from 8-hydroxydaidzein glucosylated by recombinant amylosucrase of Deinococcus geothermalis. Molecules. 2019 Jun 15;24(12). pii: E2236. | ||||
| 67 | Comparative in vitro metabolism of phospho-tyrosol-indomethacin by mice, rats and humans Biochem Pharmacol. 2013 Apr 15;85(8):1195-202. doi: 10.1016/j.bcp.2013.01.031. | ||||
| 68 | EMA Label: Cresemba, Isavuconazole - European Medicines Agency - Europa EU | ||||
| 69 | DrugBank(Pharmacology-Metabolism)Isavuconazonium | ||||
| 70 | Bioavailability of isoflavones J Chromatogr B Analyt Technol Biomed Life Sci. 2002 Sep 25;777(1-2):203-10. doi: 10.1016/s1570-0232(02)00347-1. | ||||
| 71 | Glucuronides are the main isoflavone metabolites in women J Nutr. 2003 Feb;133(2):399-404. doi: 10.1093/jn/133.2.399. | ||||
| 72 | Comprehensive Evaluation of Metabolism and the Contribution of the Hepatic First-Pass Effect in the Bioavailability of Glabridin in Rats. J Agric Food Chem. 2023 Feb 1;71(4):1944-1956. doi: 10.1021/acs.jafc.2c06460. | ||||
| 73 | Detoxication versus Bioactivation Pathways of Lapatinib In Vitro: UGT1A1 Catalyzes the Hepatic Glucuronidation of Debenzylated Lapatinib Drug Metab Dispos. 2021 Mar;49(3):233-244. doi: 10.1124/dmd.120.000236. | ||||
| 74 | Case Study 11: Considerations for Enzyme Mapping Experiments-Interaction Between the Aldehyde Oxidase Inhibitor Hydralazine and Glutathione. Methods Mol Biol. 2021;2342:809-823. doi: 10.1007/978-1-0716-1554-6_30. | ||||
| 75 | Pubchem:Lomefloxacin | ||||
| 76 | Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. | ||||
| 77 | DrugBank(Pharmacology-Metabolism):Methyldopate Hydrochloride | ||||
| 78 | Metabolomics of Methylphenidate and Ethylphenidate: Implications in Pharmacological and Toxicological Effects | ||||
| 79 | Absorption, disposition and metabolic pathway of amiselimod (MT-1303) in healthy volunteers in a mass balance study | ||||
| 80 | Differences in nevirapine biotransformation as a factor for its sex-dependent dimorphic profile of adverse drug reactions J Antimicrob Chemother. 2014 Feb;69(2):476-82. doi: 10.1093/jac/dkt359. | ||||
| 81 | Disposition and biotransformation of the antiretroviral drug nevirapine in humans Drug Metab Dispos. 1999 Aug;27(8):895-901. | ||||
| 82 | U. S. FDA Label -Nevirapine | ||||
| 83 | Human mass balance study and metabolite profiling of (14)C-niraparib, a novel poly(ADP-Ribose) polymerase (PARP)-1 and PARP-2 inhibitor, in patients with advanced cancer Invest New Drugs. 2017 Dec;35(6):751-765. doi: 10.1007/s10637-017-0451-2. | ||||
| 84 | P-Glycoprotein (ABCB1/MDR1) Controls Brain Penetration and Intestinal Disposition of the PARP1/2 Inhibitor Niraparib. Mol Pharm. 2021 Dec 6;18(12):4371-4384. doi: 10.1021/acs.molpharmaceut.1c00553. | ||||
| 85 | Normal-phase liquid chromatography-particle-beam mass spectrometry in drug metabolism studies of the dopamine receptor antagonist Odapipam and the muscarine M1 receptor agonist Xanomeline | ||||
| 86 | Simultaneous determination of parecoxib and its main metabolites valdecoxib and hydroxylated valdecoxib in mouse plasma with a sensitive LC-MS/MS method to elucidate the decreased drug metabolism of tumor bearing mice. J Pharm Biomed Anal. 2018 Sep 5;158:1-7. | ||||
| 87 | Comparison of pharmacokinetic profiles in hypoalbuminemia and healthy rats after parecoxib sodium injection?by LC-MS/MS. Bioanalysis. 2023 Feb;15(4):231-243. doi: 10.4155/bio-2022-0197. | ||||
| 88 | Disposition of a specific cyclooxygenase-2 inhibitor, valdecoxib, in human Drug Metab Dispos. 2002 Sep;30(9):1013-21. doi: 10.1124/dmd.30.9.1013. | ||||
| 89 | Metabolism and excretion of 1-hydroxymethylpyrene, the proximate metabolite of the carcinogen 1-methylpyrene, in rats. Toxicology. 2016 Jul 29;366-367:43-52. | ||||
| 90 | Effects of ketoconazole treatment on the pharmacokinetics of safinamide and its plasma metabolites in healthy adult subjects | ||||
| 91 | Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. | ||||
| 92 | In vitro metabolic profile and drug-drug interaction assessment of secnidazole, a high-dose 5-nitroimidazole antibiotic for the treatment of bacterial vaginosis Pharmacol Res Perspect. 2020 Aug;8(4):e00634. doi: 10.1002/prp2.634. | ||||
| 93 | Secnidazole. A review of its antimicrobial activity, pharmacokinetic properties and therapeutic use in the management of protozoal infections and bacterial vaginosis Drugs. 1996 Apr;51(4):621-38. doi: 10.2165/00003495-199651040-00007. | ||||
| 94 | DrugBank(Pharmacology-Metabolism)Sertraline hydrochloride | ||||
| 95 | FDA Approved Drug Products: Ultane (sevoflurane), volatile liquid for inhalation | ||||
| 96 | Stable isotope- and mass spectrometry-based metabolomics as tools in drug metabolism: a study expanding tempol pharmacology | ||||
| 97 | Elimination pathways of terbutaline | ||||
| 98 | Phase I dose escalation pharmacokinetics of O-(chloroacetylcarbamoyl) fumagillol (TNP-470) and its metabolites in AIDS patients with Kaposi's sarcoma | ||||
| 99 | A single dose mass balance study of the Hedgehog pathway inhibitor vismodegib (GDC-0449) in humans using accelerator mass spectrometry | ||||
| 100 | Absorption, distribution, metabolism, and excretion of [1?C]GDC-0449 (vismodegib), an orally active hedgehog pathway inhibitor, in rats and dogs: a unique metabolic pathway via pyridine ring opening | ||||
| 101 | Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor | ||||
| 102 | Identification of the cytochrome P450 and other enzymes involved in the in vitro oxidative metabolism of a novel antidepressant, Lu AA21004. Drug Metab Dispos. 2012 Jul;40(7):1357-65. | ||||
| 103 | Vortioxetine: clinical pharmacokinetics and drug interactions. Clin Pharmacokinet. 2018 Jun;57(6):673-686. | ||||
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