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: 82 Drugs | ||||
Bupropion |
Drug Info | Approved | Nicotine dependence | ICD11: 6C4A | [1] |
Tamoxifen citrate |
Drug Info | Approved | Breast cancer | ICD11: 2C60 | [2] |
Yn-968D1 |
Drug Info | Approved | Breast cancer | ICD11: 2C60-2C6Y | [3] |
Arbidol |
Drug Info | Approved | Virus infection | ICD11: 1A24-1D9Z | [4] |
Dabigatran etexilate |
Drug Info | Approved | Venous thromboembolism | ICD11: BD72 | [5] |
Diclofenac sodium |
Drug Info | Approved | Osteoarthritis | ICD11: FA00 | [6] |
Loxoprofen gel |
Drug Info | Approved | Inflammation | ICD11: 1A00-CA43 | [7] |
Naloxone |
Drug Info | Approved | Opiate dependence | ICD11: 6C43 | [8] |
Beta carotene |
Drug Info | Approved | Vitamin deficiency | ICD11: 5B55 | [9] |
Cannabidiol |
Drug Info | Approved | Lennox-Gastaut syndrome | ICD11: 8A62 | [10] |
Ethinyl estradiol |
Drug Info | Approved | Menopausal disorder | ICD11: GA30 | [11] |
Mycophenolate mofetil |
Drug Info | Approved | Crohn disease | ICD11: DD70 | [12] |
Pitavastatin |
Drug Info | Approved | Hypertriglyceridaemia | ICD11: 5C80 | [13] |
Silodosin |
Drug Info | Approved | Prostatic hyperplasia | ICD11: GA90 | [14] |
Valproic acid |
Drug Info | Approved | Epilepsy | ICD11: 8A60 | [15] |
Bempedoic acid |
Drug Info | Approved | Hypertriglyceridaemia | ICD11: 5C80 | [16] |
Ertugliflozin |
Drug Info | Approved | Diabetes mellitus | ICD11: 5A10 | [17] |
Labetalol |
Drug Info | Approved | Essential hypertension | ICD11: BA00 | [18] |
Mirabegron |
Drug Info | Approved | Overactive bladder | ICD11: GC50 | [19] |
Opicapone |
Drug Info | Approved | Parkinsonism | ICD11: 8A00 | [20] |
Ketorolac |
Drug Info | Approved | Rheumatoid arthritis | ICD11: FA20 | [21] |
Spironolactone |
Drug Info | Approved | Congestive heart failure | ICD11: BD10-BD1Z | [22] |
Suprofen |
Drug Info | Approved | Iris sphincter disorder | ICD11: 9B01 | [23] |
Vildagliptin |
Drug Info | Approved | Type-2 diabetes | ICD11: 5A11 | [24] |
Carvedilol |
Drug Info | Approved | Congestive heart failure | ICD11: BD10 | [25] |
Dextromethorphan hydrobromide |
Drug Info | Approved | Atherosclerosis | ICD11: BA80 | [23] |
Formoterol |
Drug Info | Approved | Asthma | ICD11: CA23 | [26] |
Naproxen |
Drug Info | Approved | Rheumatoid arthritis | ICD11: FA20 | [6] |
Rofecoxib |
Drug Info | Approved | Rheumatoid arthritis | ICD11: FA20 | [27] |
Belinostat |
Drug Info | Approved | Anaplastic large cell lymphoma | ICD11: 2A90 | [28], [29] |
Bromfenac |
Drug Info | Approved | Cataract | ICD11: 9B10 | [30] |
Carbamazepine |
Drug Info | Approved | Epilepsy | ICD11: 8A60 | [31] |
Cenobamate |
Drug Info | Approved | Focal seizure | ICD11: 8A68 | [32] |
Cenobamate |
Drug Info | Approved | Focal seizure | ICD11: 8A68 | [33] |
Codeine |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [34] |
Efavirenz |
Drug Info | Approved | Human immunodeficiency virus infection | ICD11: 1C60 | [35] |
Eslicarbazepine acetate |
Drug Info | Approved | Epilepsy | ICD11: 8A60 | [36] |
Etodolac |
Drug Info | Approved | Rheumatoid arthritis | ICD11: FA20 | [6] |
Ibuprofen |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [6] |
Indomethacin |
Drug Info | Approved | Rheumatoid arthritis | ICD11: FA20 | [37] |
Midazolam hydrochloride |
Drug Info | Approved | Anxiety disorder | ICD11: 6B00 | [38], [39], [40] |
Morphine |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [41] |
Morphine |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [42], [43], [44] |
Simvastatin |
Drug Info | Approved | Dyslipidaemia | ICD11: 5C81 | [45] |
Tapentadol |
Drug Info | Approved | Neuropathic pain | ICD11: 8E43 | [46] |
Varenicline |
Drug Info | Approved | Nicotine dependence | ICD11: 6C4A | [47] |
Abacavir |
Drug Info | Approved | Human immunodeficiency virus infection | ICD11: 1C60 | [48] |
Anastrozole |
Drug Info | Approved | Breast cancer | ICD11: 2C60 | [49] |
Buprenorphine hydrochloride |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [50] |
Gemfibrozil |
Drug Info | Approved | Hypertriglyceridaemia | ICD11: 5C80 | [51] |
Nalbuphine |
Drug Info | Approved | Pain | ICD11: MG30-MG3Z | [52] |
Nalmefene |
Drug Info | Approved | Opiate dependence | ICD11: 6C43 | [53] |
Tramadol hydrochloride |
Drug Info | Approved | Neuropathic pain | ICD11: 8E43 | [54] |
Dapagliflozin |
Drug Info | Approved | Diabetes mellitus | ICD11: 5A10 | [55] |
Empagliflozin |
Drug Info | Approved | Diabetes mellitus | ICD11: 5A10 | [56] |
Epirubicin |
Drug Info | Approved | Breast cancer | ICD11: 2C60 | [57] |
Ezetimibe |
Drug Info | Approved | Hypertriglyceridaemia | ICD11: 5C80 | [58] |
Losartan potassium |
Drug Info | Approved | Essential hypertension | ICD11: BA00 | [6] |
Lovastatin |
Drug Info | Approved | Hypertriglyceridaemia | ICD11: 5C80 | [45] |
Mycophenolic acid |
Drug Info | Approved | Crohn disease | ICD11: DD70 | [59] |
Mycophenolic acid |
Drug Info | Approved | Crohn disease | ICD11: DD70 | [60] |
Pitavastatin calcium |
Drug Info | Approved | Hypertriglyceridaemia | ICD11: 5C80 | [61] |
Troglitazone |
Drug Info | Approved | Diabetes mellitus | ICD11: 5A10 | [62] |
Zidovudine |
Drug Info | Approved | Human immunodeficiency virus infection | ICD11: 1C60 | [63] |
Ambrisentan |
Drug Info | Approved | Pulmonary hypertension | ICD11: BB01 | [64] |
Bicalutamide |
Drug Info | Approved | Prostate cancer | ICD11: 2C82 | [65] |
Clopidogrel bisulfate |
Drug Info | Approved | Acute coronary syndrome | ICD11: BA4Z | [66] |
Edaravone |
Drug Info | Approved | Cerebral stroke | ICD11: 8B11 | [67] |
Fenoprofen |
Drug Info | Approved | Rheumatoid arthritis | ICD11: FA20 | [68] |
Fluconazole |
Drug Info | Approved | Candidiasis | ICD11: 1F23 | [69] |
Flurbiprofen sodium |
Drug Info | Approved | Rheumatoid arthritis | ICD11: FA20 | [6] |
Hydromorphone |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [70] |
Oxazepam |
Drug Info | Approved | Anxiety disorder | ICD11: 6B00 | [71] |
Selexipag |
Drug Info | Approved | Pulmonary hypertension | ICD11: BB01 | [72] |
Vorinostat |
Drug Info | Approved | Cutaneous T-cell lymphoma | ICD11: 2B01 | [73] |
Artesunate |
Drug Info | Approved | Malaria | ICD11: 1F40-1F45 | [74], [75] |
Artesunate |
Drug Info | Approved | Malaria | ICD11: 1F40-1F45 | [74] |
Carprofen |
Drug Info | Approved | Anaesthesia | ICD11: 8E22 | [76] |
Letrozole |
Drug Info | Approved | Breast cancer | ICD11: 2C60 | [77] |
Lorazepam |
Drug Info | Approved | Anxiety disorder | ICD11: 6B00 | [15] |
Osilodrostat |
Drug Info | Approved | Cushing syndrome | ICD11: 5A70 | [78] |
LAROPIPRANT |
Drug Info | Phase 4 | Atherosclerosis | ICD11: BA80 | [83] |
Drugs in Phase 4 Clinical Trial | Click to Show/Hide the Full List of Drugs: 8 Drugs | ||||
Ethinylestradiol propanesulfonate |
Drug Info | Phase 4 | Prostate cancer | ICD11: 2C82 | [79], [80] |
Artenimol |
Drug Info | Phase 4 | Malaria | ICD11: 1F40 | [81] |
Acemetacin |
Drug Info | Phase 4 | Osteoarthritis | ICD11: FA00 | [82] |
Dihydrocodeine |
Drug Info | Phase 4 | Anaesthesia | ICD11: 8E22 | [84] |
Silymarin |
Drug Info | Phase 4 | Fatty liver disease | ICD11: DB92 | [85], [86] |
Zaltoprofen |
Drug Info | Phase 4 | Anaesthesia | ICD11: 8E22 | [6] |
Dexibuprofen |
Drug Info | Phase 4 | Osteoarthritis | ICD11: FA00 | [6] |
Denopamine |
Drug Info | Phase 4 | Congestive heart failure | ICD11: BD10 | [87] |
Drugs in Phase 3 Clinical Trial | Click to Show/Hide the Full List of Drugs: 11 Drugs | ||||
AKB-6548 |
Drug Info | Phase 3 | Anaemia | ICD11: 3A90 | [88] |
ABL001 |
Drug Info | Phase 3 | Chronic myelogenous leukaemia | ICD11: 2A20 | [89] |
Heroin |
Drug Info | Phase 3 | Opiate dependence | ICD11: 6C43 | [90] |
Losartan |
Drug Info | Phase 3 | Hypertension | ICD11: BA00-BA04 | [91] |
LCQ908-NXA |
Drug Info | Phase 3 | Hypertriglyceridaemia | ICD11: 5C80 | [92] |
Fevipiprant |
Drug Info | Phase 3 | Asthma | ICD11: CA23 | [93] |
Glinsuna |
Drug Info | Phase 3 | Diabetes mellitus | ICD11: 5A10 | [6], [94] |
KAD-1229 |
Drug Info | Phase 3 | Diabetes mellitus | ICD11: 5A10 | [95] |
Ag-221 |
Drug Info | Phase 3 | Acute myelogenous leukaemia | ICD11: 2A41 | [96] |
CS-011 |
Drug Info | Phase 3 | Diabetes mellitus | ICD11: 5A10 | [97] |
CS-600G |
Drug Info | Phase 3 | Epilepsy | ICD11: 8A60 | [7] |
Drugs in Phase 2 Clinical Trial | Click to Show/Hide the Full List of Drugs: 13 Drugs | ||||
UK-453,061 |
Drug Info | Phase 2 | Human immunodeficiency virus infection | ICD11: 1C60 | [98] |
LIK-066 |
Drug Info | Phase 2 | Heart failure | ICD11: BD10-BD1Z | [99] |
Ethanol |
Drug Info | Phase 2 | Diabetic nephropathy | ICD11: GB61 | [100] |
PT2385 |
Drug Info | Phase 2 | Von hippel-lindau disease | ICD11: 5A75 | [101] |
BIA 3-202 |
Drug Info | Phase 2 | Parkinsonism | ICD11: 8A00 | [102] |
(Z)-endoxifen |
Drug Info | Phase 2 | Breast cancer | ICD11: 2C60-2C6Y | [103] |
BIIB074 |
Drug Info | Phase 2 | Bipolar disorder | ICD11: 6A60 | [104] |
Endoxifen |
Drug Info | Phase 2 | Breast cancer | ICD11: 2C60-2C6Y | [103] |
MPC-4326 |
Drug Info | Phase 2 | Human immunodeficiency virus infection | ICD11: 1C60 | [105] |
ABT-751 |
Drug Info | Phase 2 | Breast cancer | ICD11: 2C60 | [106] |
ASA-404 |
Drug Info | Phase 2 | Prostate cancer | ICD11: 2C82 | [107] |
BN-1270 |
Drug Info | Phase 2 | Pulmonary hypertension | ICD11: BB01 | [108] |
Estetrol |
Drug Info | Phase 2 | Diabetes mellitus | ICD11: 5A10 | [109] |
Drugs in Phase 1 Clinical Trial | Click to Show/Hide the Full List of Drugs: 5 Drugs | ||||
CB-3304 |
Drug Info | Phase 1/2 | Chronic lymphocytic leukaemia | ICD11: 2A82 | [110] |
DA-1229 |
Drug Info | Phase 1 | Type-2 diabetes | ICD11: 5A11 | [111] |
BRN-3224996 |
Drug Info | Phase 1 | Allergy | ICD11: 4A80 | [112] |
GTPL-1666 |
Drug Info | Phase 1 | Cerebral vasospasm | ICD11: BA85 | [113] |
Norbuprenorphine |
Drug Info | Phase 1 | Human immunodeficiency virus infection | ICD11: 1C60-1C62 | [114] |
Discontinued/withdrawn Drugs | Click to Show/Hide the Full List of Drugs: 2 Drugs | ||||
BMS-204352 |
Drug Info | Discontinued in Phase 3 | Nerve injury | ICD11: ND56 | [115] |
ML-3000 |
Drug Info | Discontinued | Osteoarthritis | ICD11: FA00 | [6] |
Preclinical/investigative Agents | Click to Show/Hide the Full List of Drugs: 5 Drugs | ||||
Cotinine |
Drug Info | Investigative | Nicotine dependence | ICD11: 6C4A | [116] |
BRN-3548355 |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [117] |
Alpha-dihydroaldosterone |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [112] |
BRN-1999480 |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [118] |
Tetrahydroaldosterone |
Drug Info | Investigative | Discovery agent | ICD: N.A. | [112] |
Experimental Enzyme Kinetic Data of Drugs | Click to Show/Hide the Full List of Drugs: 4 Drugs | ||||
Zidovudine |
Drug Info | Approved | Human immunodeficiency virus infection | Km = 0.551 microM | [63] |
BRN-3224996 |
Drug Info | Phase 1 | Allergy | Km = 0.00036 microM | [112] |
Alpha-dihydroaldosterone |
Drug Info | Investigative | Discovery agent | Km = 0.00023 microM | [112] |
Tetrahydroaldosterone |
Drug Info | Investigative | Discovery agent | Km = 0.00197 microM | [112] |
References | |||||
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1 | DrugBank(Pharmacology-Metabolism)Bupropion | ||||
2 | Metabolism and transport of tamoxifen in relation to its effectiveness: new perspectives on an ongoing controversy. Future Oncol. 2014 Jan;10(1):107-22. | ||||
3 | Metabolism and pharmacokinetics of novel selective vascular endothelial growth factor receptor-2 inhibitor apatinib in humans | ||||
4 | DrugBank(Pharmacology-Metabolism):Arbidol | ||||
5 | Dabigatran acylglucuronide, the major human metabolite of dabigatran: in vitro formation, stability, and pharmacological activity. Drug Metab Dispos. 2010 Sep;38(9):1567-75. | ||||
6 | 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. | ||||
7 | Exploring the metabolism of loxoprofen in liver microsomes: the role of cytochrome P450 and UDP-glucuronosyltransferase in its biotransformation. Pharmaceutics. 2018 Aug 2;10(3). pii: E112. | ||||
8 | PBPK Modeling as a Tool for Predicting and Understanding Intestinal Metabolism of Uridine 5'-Diphospho-glucuronosyltransferase Substrates | ||||
9 | #NAME? | ||||
10 | Cytochrome P450-Catalyzed Metabolism of Cannabidiol to the Active Metabolite 7-Hydroxy-Cannabidiol Drug Metab Dispos. 2021 Oct;49(10):882-891. doi: 10.1124/dmd.120.000350. | ||||
11 | Human bilirubin UDP-glucuronosyltransferase catalyzes the glucuronidation of ethinylestradiol Mol Pharmacol. 1993 Apr;43(4):649-54. | ||||
12 | PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9. | ||||
13 | DrugBank(Pharmacology-Metabolism):Pitavastatin | ||||
14 | Pharmacokinetics and disposition of silodosin (KMD-3213). Yakugaku Zasshi. 2006 Mar;126 Spec no.:237-45. | ||||
15 | Pharmacokinetic and pharmacodynamic interaction of lorazepam and valproic acid in relation to UGT2B7 genetic polymorphism in healthy subjects. Clin Pharmacol Ther. 2008 Apr;83(4):595-600. | ||||
16 | DrugBank(Pharmacology-Metabolism):Bempedoic acid | ||||
17 | The effect of renal impairment on the pharmacokinetics and pharmacodynamics of ertugliflozin in subjects with type 2 diabetes mellitus. J Clin Pharmacol. 2017 Nov;57(11):1432-1443. | ||||
18 | Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination. Xenobiotica. 2008 Jan;38(1):62-75. | ||||
19 | Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective (3)-Adrenoceptor Agonist, in Human Liver Microsomes | ||||
20 | Metabolism and disposition of opicapone in the rat and metabolic enzymes phenotyping | ||||
21 | Body weight, gender and pregnancy affect enantiomer-specific ketorolac pharmacokinetics. Br J Clin Pharmacol. 2017 Sep;83(9):1966-1975. | ||||
22 | Spironolactone and canrenone inhibit UGT2B7-catalyzed human liver and kidney microsomal aldosterone 18beta-glucuronidation: a potential drug interaction | ||||
23 | 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. | ||||
24 | Dipeptidyl peptidase-4 greatly contributes to the hydrolysis of vildagliptin in human liver | ||||
25 | Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. | ||||
26 | FDA Approved Drug Products: Perforomist? inhalation solution | ||||
27 | Involvement of human UGT2B7 and 2B15 in rofecoxib metabolism | ||||
28 | Glucuronidation by UGT1A1 is the dominant pathway of the metabolic disposition of belinostat in liver cancer patients. PLoS One. 2013;8(1):e54522. | ||||
29 | In vitro characterization of belinostat glucuronidation: demonstration of both UGT1A1 and UGT2B7 as the main contributing isozymes | ||||
30 | Metabolite profiling and reaction phenotyping for the in vitro assessment of the bioactivation of bromfenac. Chem Res Toxicol. 2020 Jan 21;33(1):249-257. | ||||
31 | Association of carbamazepine major metabolism and transport pathway gene polymorphisms and pharmacokinetics in patients with epilepsy. Pharmacogenomics. 2013 Jan;14(1):35-45. | ||||
32 | FDA label of Cenobamate. The 2020 official website of the U.S. Food and Drug Administration. | ||||
33 | DrugBank(Pharmacology-Metabolism):Cenobamate | ||||
34 | Human UGT2B7 catalyzes morphine glucuronidation. Drug Metab Dispos. 1997 Jan;25(1):1-4. | ||||
35 | Biotransformation of Efavirenz and Proteomic Analysis of Cytochrome P450s and UDP-Glucuronosyltransferases in Mouse, Macaque, and Human Brain-Derived In Vitro Systems. Drug Metab Dispos. 2023 Apr;51(4):521-531. doi: 10.1124/dmd.122.001195. | ||||
36 | Pharmacokinetics and drug interactions of eslicarbazepine acetate Epilepsia. 2012 Jun;53(6):935-46. doi: 10.1111/j.1528-1167.2012.03519.x. | ||||
37 | Contribution of UDP-glucuronosyltransferases 1A9 and 2B7 to the glucuronidation of indomethacin in the human liver. Eur J Clin Pharmacol. 2007 Mar;63(3):289-96. | ||||
38 | The inhibition study of human UDP-glucuronosyltransferases with cytochrome P450 selective substrates and inhibitors | ||||
39 | Contribution of the N-glucuronidation pathway to the overall in vitro metabolic clearance of midazolam in humans | ||||
40 | The Oral Bioavailability and Metabolism of Midazolam in Stable Critically Ill Children: A Pharmacokinetic Microtracing Study | ||||
41 | Molecular cloning of the baboon UDP-glucuronosyltransferase 2B gene family and their activity in conjugating morphine. Drug Metab Dispos. 2010 Apr;38(4):545-53. | ||||
42 | Pharmacogenomics knowledge for personalized medicine Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96. | ||||
43 | Metabolism and pharmacokinetics of morphine in neonates: A review | ||||
44 | Morphine metabolism, transport and brain disposition | ||||
45 | Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106. | ||||
46 | Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008 Jan;2(1):67-75. | ||||
47 | Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro | ||||
48 | Product characteristics of Triumeq. | ||||
49 | In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. | ||||
50 | Contribution of the different UDP-glucuronosyltransferase (UGT) isoforms to buprenorphine and norbuprenorphine metabolism and relationship with the main UGT polymorphisms in a bank of human liver microsomes. Drug Metab Dispos. 2010 Jan;38(1):40-5. | ||||
51 | The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos. 2007 Nov;35(11):2040-4. | ||||
52 | A dual system platform for drug metabolism: Nalbuphine as a model compound | ||||
53 | Ema.europa:Nalmefene | ||||
54 | DrugBank : Tramadol hydrochloride | ||||
55 | Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. | ||||
56 | Empagliflozin (Jardiance): a novel SGLT2 inhibitor for the treatment of type-2 diabetes. P T. 2015 Jun;40(6):364-8. | ||||
57 | Epirubicin glucuronidation and UGT2B7 developmental expression. Drug Metab Dispos. 2006 Dec;34(12):2097-101. | ||||
58 | Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94. | ||||
59 | Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. Drug Metab Dispos. 2011 Mar;39(3):448-55. | ||||
60 | Effect of UGT polymorphisms on pharmacokinetics and adverse reactions of mycophenolic acid in kidney transplant patients | ||||
61 | Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. | ||||
62 | Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9. | ||||
63 | Determination of UDP-glucuronosyltransferase UGT2B7 activity in human liver microsomes by ultra-performance liquid chromatography with MS detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Jul 1;870(1):84-90. | ||||
64 | Clinical pharmacokinetics and drug-drug interactions of endothelin receptor antagonists in pulmonary arterial hypertension. J Clin Pharmacol. 2012 Dec;52(12):1784-805. | ||||
65 | 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. | ||||
66 | Physiologically Based Pharmacokinetic (PBPK) Modeling of Clopidogrel and Its Four Relevant Metabolites for CYP2B6, CYP2C8, CYP2C19, and CYP3A4 Drug-Drug-Gene Interaction Predictions | ||||
67 | LABEL:ADICAVA- edaravone injection RADICAVA ORS- edaravone kit | ||||
68 | Dataset of the first report of pharmacogenomics profiling in an outpatient spine setting | ||||
69 | The disposition and metabolism of [14C]fluconazole in humans Drug Metab Dispos. 1991 Jul-Aug;19(4):764-7. | ||||
70 | Opioid therapies and cytochrome p450 interactions. J Pain Symptom Manage. 2012 Dec;44(6 Suppl):S4-14. | ||||
71 | Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9. Drug Metab Dispos. 2002 Nov;30(11):1257-65. | ||||
72 | FDA LABEL:elexipag | ||||
73 | Age-dependent hepatic UDP-glucuronosyltransferase gene expression and activity in children. Front Pharmacol. 2016 Nov 16;7:437. | ||||
74 | Glucuronidation of dihydroartemisinin in vivo and by human liver microsomes and expressed UDP-glucuronosyltransferases | ||||
75 | LC-MS/MS method for the simultaneous quantification of artesunate and its metabolites dihydroartemisinin and dihydroartemisinin glucuronide in human plasma | ||||
76 | Enantioselective inhibition of carprofen towards UDP-glucuronosyltransferase (UGT) 2B7. Chirality. 2015 Mar;27(3):189-93. | ||||
77 | The letrozole phase 1 metabolite carbinol as a novel probe drug for UGT2B7 Drug Metab Dispos. 2013 Nov;41(11):1906-13. doi: 10.1124/dmd.113.053405. | ||||
78 | DrugBank(Pharmacology-Metabolism):Osilodrostat | ||||
79 | Genetic variation in the first-pass metabolism of ethinylestradiol, sex hormone binding globulin levels and venous thrombosis risk Eur J Intern Med. 2017 Jul;42:54-60. doi: 10.1016/j.ejim.2017.05.019. | ||||
80 | Metabolism of 17 alpha-ethinylestradiol by human liver microsomes in vitro: aromatic hydroxylation and irreversible protein binding of metabolites J Clin Endocrinol Metab. 1974 Dec;39(6):1072-80. doi: 10.1210/jcem-39-6-1072. | ||||
81 | Eurartesim - European Medicines Agency | ||||
82 | Seyffart G. (1992). Drug dosage in renal insufficiency (2nd ed.). Springer Science+Business Media Dordrecht. | ||||
83 | Metabolism of MK-0524, a prostaglandin D2 receptor 1 antagonist, in microsomes and hepatocytes from preclinical species and humans | ||||
84 | Adult and infant pharmacokinetic profiling of dihydrocodeine using physiologically based pharmacokinetic modeling. Biopharm Drug Dispos. 2019 Nov;40(9):350-357. | ||||
85 | Evidence for differences in regioselective and stereoselective glucuronidation of silybin diastereomers from milk thistle (Silybum marianum) by human UDP-glucuronosyltransferases | ||||
86 | Metabolism, Transport and Drug-Drug Interactions of Silymarin | ||||
87 | Regioselective glucuronidation of denopamine: marked species differences and identification of human udp-glucuronosyltransferase isoform. Drug Metab Dispos. 2005 Mar;33(3):403-12. | ||||
88 | DrugBank(Pharmacology-Metabolism):AKB-6548 | ||||
89 | Pharmacokinetics of asciminib in the presence of CYP3A or P-gp inhibitors, CYP3A inducers, and acid-reducing agents | ||||
90 | PharmGKB:Heroin | ||||
91 | 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. | ||||
92 | Pradigastat disposition in humans: in vivo and in vitro investigations. Xenobiotica. 2017 Dec;47(12):1077-1089. | ||||
93 | Clinical Investigation of Metabolic and Renal Clearance Pathways Contributing to the Elimination of Fevipiprant Using Probenecid as Perpetrator. Drug Metab Dispos. 2021 May;49(5):389-394. doi: 10.1124/dmd.120.000273. | ||||
94 | Carboxyl-glucuronidation of mitiglinide by human UDP-glucuronosyltransferases. Biochem Pharmacol. 2007 Jun 1;73(11):1842-51. | ||||
95 | Mitiglinide: a rapid- and short-acting non-sulfonylurea insulinotropic agent for the treatment of type 2 diabetic patients | ||||
96 | DrugBank(Pharmacology-Metabolism):Ag-221 | ||||
97 | In vitro metabolism of rivoglitazone, a novel peroxisome proliferator-activated receptor gama agonist, in rat, monkey, and human liver microsomes and freshly isolated hepatocytes. Drug Metab Dispos. 2011 Jul;39(7):1311-9. | ||||
98 | Excretion and metabolism of lersivirine (5-{[3,5-diethyl-1-(2-hydroxyethyl)(3,5-14C2)-1H-pyrazol-4-yl]oxy}benzene-1,3-dicarbonitrile), a next-generation non-nucleoside reverse transcriptase inhibitor, after administration of [14C]Lersivirine to healthy volunteers. Drug Metab Dispos. 2010 May;38(5):789-800. | ||||
99 | Pharmacokinetics, metabolism, and excretion of licogliflozin, a dual inhibitor of SGLT1/2, in rats, dogs, and humans | ||||
100 | Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32. | ||||
101 | Metabolic Profiling of the Novel Hypoxia-Inducible Factor 2 Inhibitor PT2385 In Vivo and In Vitro | ||||
102 | Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation | ||||
103 | Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen | ||||
104 | Evaluation of the Pharmacokinetic Interaction Between the Voltage- and Use-Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers | ||||
105 | Bevirimat: a novel maturation inhibitor for the treatment of HIV-1 infection. Antivir Chem Chemother. 2008;19(3):107-13. | ||||
106 | 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. | ||||
107 | 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. | ||||
108 | Induction and inhibition of cicletanine metabolism in cultured hepatocytes and liver microsomes from rats. Fundam Clin Pharmacol. 2000 Sep-Oct;14(5):509-18. | ||||
109 | Differential glucuronidation of bile acids, androgens and estrogens by human UGT1A3 and 2B7 | ||||
110 | Metabolic map and bioactivation of the anti-tumour drug noscapine | ||||
111 | In Vitro Metabolic Pathways of the New Anti-Diabetic Drug Evogliptin in Human Liver Preparations | ||||
112 | Human uridine diphosphate-glucuronosyltransferase UGT2B7 conjugates mineralocorticoid and glucocorticoid metabolites. Endocrinology. 2003 Jun;144(6):2659-68. | ||||
113 | Evaluation of the transport, in vitro metabolism and pharmacokinetics of Salvinorin A, a potent hallucinogen. Eur J Pharm Biopharm. 2009 Jun;72(2):471-7. | ||||
114 | Chemical and enzyme-assisted syntheses of norbuprenorphine-3--D-glucuronide | ||||
115 | Metabolism, pharmacokinetics, and protein covalent binding of radiolabeled MaxiPost (BMS-204352) in humans | ||||
116 | Interindividual variability in nicotine metabolism: C-oxidation and glucuronidation | ||||
117 | 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) metabolism-related enzymes gene polymorphisms, NNK metabolites levels and urothelial carcinoma | ||||
118 | Expression of UGT2B7, a UDP-glucuronosyltransferase implicated in the metabolism of 4-hydroxyestrone and all-trans retinoic acid, in normal human breast parenchyma and in invasive and in situ breast cancers | ||||
119 | Product characteristics of Triumeq | ||||
120 | Disposition of asciminib, a potent BCR-ABL1 tyrosine kinase inhibitor, in healthy male subjects | ||||
121 | DrugBank(Pharmacology-Metabolism)Acemetacin | ||||
122 | [Comparative metabolic studies on [14C]-labelled acemetacin and indometacin in rats (author's transl)] Arzneimittelforschung. 1980;30(8A):1384-91. | ||||
123 | Effect of ketoconazole on the pharmacokinetic profile of ambrisentan. J Clin Pharmacol. 2009 Jun;49(6):719-24. | ||||
124 | Pharmacokinetics, metabolism, and excretion of the antiviral drug arbidol in humans | ||||
125 | Metabolic profile, enzyme kinetics, and reaction phenotyping of -lapachone metabolism in human liver and intestine in vitro | ||||
126 | DrugBank(Pharmacology-Metabolism)Artenimol | ||||
127 | 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. | ||||
128 | Dailymed:Bicalutamide | ||||
129 | Amide N-glucuronidation of MaxiPost catalyzed by UDP-glucuronosyltransferase 2B7 in humans | ||||
130 | Metabolic disposition of 14C-bromfenac in healthy male volunteers J Clin Pharmacol. 1998 Aug;38(8):744-52. doi: 10.1002/j.1552-4604.1998.tb04815.x. | ||||
131 | In vitro metabolism study of buprenorphine: evidence for new metabolic pathways. Drug Metab Dispos. 2005 May;33(5):689-95. | ||||
132 | Interaction between buprenorphine and norbuprenorphine in neonatal opioid withdrawal syndrome. Drug Alcohol Depend. 2023 Jun 21;249:110832. doi: 10.1016/j.drugalcdep.2023.110832. | ||||
133 | Determination of buprenorphine, norbuprenorphine, naloxone, and their glucuronides in urine by liquid chromatography-tandem mass spectrometry. Drug Test Anal. 2021 Sep;13(9):1658-1667. doi: 10.1002/dta.3104. | ||||
134 | Glucuronidation of capsaicin by liver microsomes and expressed UGT enzymes: reaction kinetics, contribution of individual enzymes and marked species differences Expert Opin Drug Metab Toxicol. 2014 Oct;10(10):1325-36. doi: 10.1517/17425255.2014.954548. | ||||
135 | Carbamazepine and its metabolites in human perfused placenta and in maternal and cord blood Epilepsia. 1995 Mar;36(3):241-8. doi: 10.1111/j.1528-1157.1995.tb00991.x. | ||||
136 | The pharmacokinetics and metabolism of 14C-carprofen in man Biopharm Drug Dispos. 1982 Jan-Mar;3(1):29-38. doi: 10.1002/bdd.2510030105. | ||||
137 | Metabolism of carvedilol in dogs, rats, and mice Drug Metab Dispos. 1998 Oct;26(10):958-69. | ||||
138 | Mass Balance, Metabolism, and Excretion of Cenobamate, a New Antiepileptic Drug, After a Single Oral Administration in Healthy Male Subjects Eur J Drug Metab Pharmacokinet. 2020 Aug;45(4):513-522. doi: 10.1007/s13318-020-00615-7. | ||||
139 | Microsomal codeine N-demethylation: cosegregation with cytochrome P4503A4 activity | ||||
140 | Pharmacokinetics and metabolism of codeine in humans | ||||
141 | Pharmacogenetics of analgesic drugs | ||||
142 | Diclofenac does not interact with codeine metabolism in vivo: a study in healthy volunteers | ||||
143 | DrugBank(Pharmacology-Metabolism):Codeine | ||||
144 | Metabolism of the trisubstituted purine cyclin-dependent kinase inhibitor seliciclib (R-roscovitine) in vitro and in vivo. Drug Metab Dispos. 2008 Mar;36(3):561-70. | ||||
145 | #N/A | ||||
146 | Dabigatran Acylglucuronide, the Major Metabolite of Dabigatran, Shows a Weaker Anticoagulant Effect than Dabigatran | ||||
147 | LC-MS/MS analysis of dextromethorphan metabolism in human saliva and urine to determine CYP2D6 phenotype and individual variability in N-demethylation and glucuronidation J Chromatogr B Analyt Technol Biomed Life Sci. 2004 Dec 25;813(1-2):217-25. doi: 10.1016/j.jchromb.2004.09.040. | ||||
148 | Classics in Chemical Neuroscience: Dextromethorphan (DXM). ACS Chem Neurosci. 2023 Jun 21;14(12):2256-2270. doi: 10.1021/acschemneuro.3c00088. | ||||
149 | Physiologically based pharmacokinetic (PBPK) modeling of the role of CYP2D6 polymorphism for metabolic phenotyping with dextromethorphan. Front Pharmacol. 2022 Oct 24;13:1029073. doi: 10.3389/fphar.2022.1029073. | ||||
150 | Physiologically-based pharmacokinetic modeling of dextromethorphan to investigate interindividual variability within CYP2D6 activity score groups. CPT Pharmacometrics Syst Pharmacol. 2022 Apr;11(4):494-511. doi: 10.1002/psp4.12776. | ||||
151 | DrugBank(Pharmacology-Metabolism)Diclofenac sodium | ||||
152 | Pharmacokinetics of dihydrocodeine and its active metabolite after single and multiple oral dosing. Br J Clin Pharmacol. 1999 Sep;48(3):317-22. | ||||
153 | Pharmacokinetics, Pharmacodynamics and Clinical Use of SGLT2 Inhibitors in Patients with Type 2 Diabetes Mellitus and Chronic Kidney Disease | ||||
154 | Pharmacokinetics of epirubicin after intravenous administration: experimental and clinical aspects | ||||
155 | Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects Drug Metab Dispos. 2013 Feb;41(2):445-56. doi: 10.1124/dmd.112.049551. | ||||
156 | Bioequivalence Study of Ezetimibe Tablets After a Single Oral Dose of 10?mg in Healthy Japanese Subjects Under Fasting Conditions. Clin Pharmacol Drug Dev. 2023 Apr 6. doi: 10.1002/cpdd.1245. | ||||
157 | Pharmacokinetics and bioequivalence of Ezetimibe tablet versus Ezetrol?:an open-label, randomized, two-sequence crossover study in healthy Chinese subjects. BMC Pharmacol Toxicol. 2023 Feb 3;24(1):7. doi: 10.1186/s40360-023-00649-y. | ||||
158 | Investigation of the discriminatory ability of analytes for the bioequivalence assessment of ezetimibe: Parent drug, metabolite, total form, and combination of parent drug and total form. Eur J Pharm Sci. 2022 Jul 1;174:106192. doi: 10.1016/j.ejps.2022.106192. | ||||
159 | Fevipiprant has a low risk of influencing co-medication pharmacokinetics: Impact on simvastatin and rosuvastatin in different SLCO1B1 genotypes | ||||
160 | Investigation into UDP-glucuronosyltransferase (UGT) enzyme kinetics of imidazole- and triazole-containing antifungal drugs in human liver microsomes and recombinant UGT enzymes. Drug Metab Dispos. 2010 Jun;38(6):923-9. | ||||
161 | DrugBank(Pharmacology-Metabolism):Flurbiprofen | ||||
162 | 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. | ||||
163 | DrugBank : Formoterol | ||||
164 | Intracellular pharmacokinetics of gemcitabine, its deaminated metabolite 2',2'-difluorodeoxyuridine and their nucleotides Br J Clin Pharmacol. 2018 Jun;84(6):1279-1289. doi: 10.1111/bcp.13557. | ||||
165 | Hydromorphone | ||||
166 | Opioid pharmacokinetic drug-drug interactions. Am J Manag Care. 2011 Sep;17 Suppl 11:S276-87. | ||||
167 | Herb-drug interaction in the protective effect of Alpinia officinarum against gastric injury induced by indomethacin based on pharmacokinetic, tissue distribution and excretion studies in rats. J Pharm Anal. 2021 Apr;11(2):200-209. doi: 10.1016/j.jpha.2020.05.009. | ||||
168 | Identification and structural characterization of in vivo metabolites of ketorolac using liquid chromatography electrospray ionization tandem mass spectrometry (LC/ESI-MS/MS) J Mass Spectrom. 2012 Jul;47(7):919-31. doi: 10.1002/jms.3043. | ||||
169 | Pregnancy-Related Hormones Increase UGT1A1-Mediated Labetalol Metabolism in Human Hepatocytes Front Pharmacol. 2021 Apr 15;12:655320. doi: 10.3389/fphar.2021.655320. | ||||
170 | #N/A | ||||
171 | Effect of the UGT2B15 genotype on the pharmacokinetics, pharmacodynamics, and drug interactions of intravenous lorazepam in healthy volunteers. Clin Pharmacol Ther. 2005 Jun;77(6):486-94. | ||||
172 | Clinical pharmacokinetics of losartan. Clin Pharmacokinet. 2005;44(8):797-814. | ||||
173 | Identification of sulfonyl-loxoprofen as novel phase 2 conjugate in rat | ||||
174 | The potent inhibition of human cytosolic sulfotransferase 1A1 by 17-ethinylestradiol is due to interactions with isoleucine 89 on loop 1 Horm Mol Biol Clin Investig. 2014 Dec;20(3):81-90. doi: 10.1515/hmbci-2014-0028. | ||||
175 | Presence of morphine metabolites in human cerebrospinal fluid after intracerebroventricular administration of morphine | ||||
176 | Glucuronidation of anti-HIV drug candidate bevirimat: identification of human UDP-glucuronosyltransferases and species differences | ||||
177 | Identification of the UDP-glucuronosyltransferase isoforms involved in mycophenolic acid phase II metabolism. Drug Metab Dispos. 2005 Jan;33(1):139-46. | ||||
178 | Pharmacokinetics of mycophenolic acid and its phenolic-glucuronide and ACYl glucuronide metabolites in stable thoracic transplant recipients | ||||
179 | Isolation of a novel morphinan 3-O-diglucuronide metabolite from dog urine | ||||
180 | Optimization of Mass Spectrometry Imaging for Drug Metabolism and Distribution Studies in the Zebrafish Larvae Model: A Case Study with the Opioid Antagonist Naloxone | ||||
181 | Pharmacokinetics, pharmacodynamics and tolerability of opicapone, a novel catechol-O-methyltransferase inhibitor, in healthy subjects: prediction of slow enzyme-inhibitor complex dissociation of a short-living and very long-acting inhibitor | ||||
182 | Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: human UDP-glucuronosyltransferase enzymes involved in lactonization. Xenobiotica. 2003 Jan;33(1):27-41. | ||||
183 | In vivo metabolic investigation of silodosin using UHPLC-QTOF-MS/MS and in silico toxicological screening of its metabolites J Mass Spectrom. 2016 Oct;51(10):867-882. doi: 10.1002/jms.3795. | ||||
184 | Simvastatin Tablet, Film-Coated | ||||
185 | On the Molecular Basis Underlying the Metabolism of Tapentadol Through Sulfation Eur J Drug Metab Pharmacokinet. 2017 Oct;42(5):793-800. doi: 10.1007/s13318-016-0392-8. | ||||
186 | A case report on fatal intoxication by tapentadol: Study of distribution and metabolism Forensic Sci Int. 2021 Jul;324:110825. doi: 10.1016/j.forsciint.2021.110825. | ||||
187 | Absorption, metabolism, and excretion of [14C]vildagliptin, a novel dipeptidyl peptidase 4 inhibitor, in humans | ||||
188 | Disposition of vildagliptin, a novel dipeptidyl peptidase 4 inhibitor, in rats and dogs | ||||
189 | Stability studies of vorinostat and its two metabolites in human plasma, serum and urine | ||||
190 | Uridine 5'-diphospho-glucuronosyltransferase genetic polymorphisms and response to cancer chemotherapy. Future Oncol. 2010 Apr;6(4):563-85. | ||||
191 | Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. | ||||
192 | Metabolism and pharmacokinetics of the combination Zidovudine plus Lamivudine in the adult Erythrocebus patas monkey determined by liquid chromatography-tandem mass spectrometric analysis |
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