Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT34ZAF)

DTT Name UDP-glucuronosyltransferase 1A1 (UGT1A1)
Synonyms UGT1A1; Bilirubin-specific UDPGT isozyme 1; hUG-BR1; UDP-glucuronosyltransferase 1-1; UDPGT 1-1; UGT1*1; UGT1-01; UGT1.1; UDP-glucuronosyltransferase 1A isoform 1
Gene Name UGT1A1
DTT Type
Clinical trial target
 [1]
UniProt ID
UD11_HUMAN
TTD ID
T93480
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 2.4.1.17
Sequence
MAVESQGGRPLVLGLLLCVLGPVVSHAGKILLIPVDGSHWLSMLGAIQQLQQRGHEIVVL
APDASLYIRDGAFYTLKTYPVPFQREDVKESFVSLGHNVFENDSFLQRVIKTYKKIKKDS
AMLLSGCSHLLHNKELMASLAESSFDVMLTDPFLPCSPIVAQYLSLPTVFFLHALPCSLE
FEATQCPNPFSYVPRPLSSHSDHMTFLQRVKNMLIAFSQNFLCDVVYSPYATLASEFLQR
EVTVQDLLSSASVWLFRSDFVKDYPRPIMPNMVFVGGINCLHQNPLSQEFEAYINASGEH
GIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQNDL
LGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMTS
EDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAHD
LTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
Function
UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile. Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds. Catalyzes the glucuronidation of endogenous estrogen hormones such as estradiol, estrone and estriol. Involved in the glucuronidation of bilirubin, a degradation product occurring in the normal catabolic pathway that breaks down heme in vertebrates. Also catalyzes the glucuronidation the isoflavones genistein, daidzein, glycitein, formononetin, biochanin A and prunetin, which are phytoestrogens with anticancer and cardiovascular properties. Involved in the glucuronidation of the AGTR1 angiotensin receptor antagonist losartan, a drug which can inhibit the effect of angiotensin II. Involved in the biotransformation of 7-ethyl-10-hydroxycamptothecin (SN-38), the pharmacologically active metabolite of the anticancer drug irinotecan.
KEGG Pathway
Pentose and glucuronate interconversions (hsa00040 )
Ascorbate and aldarate metabolism (hsa00053 )
Steroid hormone biosynthesis (hsa00140 )
Retinol metabolism (hsa00830 )
Porphyrin metabolism (hsa00860 )
Metabolism of xenobiotics by cytochrome P450 (hsa00980 )
Drug metabolism - cytochrome P450 (hsa00982 )
Drug metabolism - other enzymes (hsa00983 )
Metabolic pathways (hsa01100 )
Biosynthesis of cofactors (hsa01240 )
Bile secretion (hsa04976 )
Chemical carcinogenesis - DNA adducts (hsa05204 )
Chemical carcinogenesis - receptor activation (hsa05207 )
Reactome Pathway
Heme degradation (R-HSA-189483 )
Defective UGT1A1 causes hyperbilirubinemia (R-HSA-5579002 )
Aspirin ADME (R-HSA-9749641 )
Paracetamol ADME (R-HSA-9753281 )
Glucuronidation (R-HSA-156588 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AT-342 DMSOQ6E Crigler-Najjar syndrome 5C58.00 Phase 1/2 [1]
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The Drug-Metabolizing Enzyme (DME) Role of This DTT

DTT DME Name UDP-glucuronosyltransferase 1A1 (UGT1A1) DME Info
Gene Name UGT1A1
102 Approved Drug(s) Metabolized by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Abacavir DMMN36E Human immunodeficiency virus infection 1C62 Approved [2]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [3]
Amitriptyline DMK7F9S Depression 6A70-6A7Z Approved [4]
Anastrozole DMNP60F Breast cancer 2C60-2C65 Approved [5]
ARRY-162 DM1P6FR Melanoma 2C30 Approved [6]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [7]
Atazanavir DMSYRBX Human immunodeficiency virus infection 1C62 Approved [8]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [9]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [10]
Bazedoxifene DMY85QW Hot flushes GA30 Approved [11]
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [12]
Candesartan DMRK8OT Chronic heart failure BD1Z Approved [13]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [14]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [15]
Chenodiol DMQ8JIK Cholelithiasis DC11 Approved [16]
Codeine DMJX6ZG Allergic rhinitis CA08.0 Approved [17]
Cyproheptadine DM92AH3 Allergic rhinitis CA08.0 Approved [18]
Darolutamide DMV7YFT Prostate cancer 2C82.0 Approved [19]
Deferasirox DM6ETS0 Beta thalassemia 3A50.2 Approved [20]
Dexibuprofen DMFYBD0 Ankylosing spondylitis FA92.0 Approved [21]
Diflunisal DM7EN8I Osteoarthritis FA00-FA05 Approved [22]
Digitoxin DMWVIGP Arrhythmia BC9Z Approved [23]
Dolutegravir DMCZGRE Human immunodeficiency virus infection 1C62 Approved [24]
Eltrombopag DMOGFIX Thrombocytopenia 3B64 Approved [25]
Elvitegravir DMG9B1U Human immunodeficiency virus infection 1C62 Approved [26]
Epinephrine DM3KJBC Acute asthma CA23 Approved [27]
Eslicarbazepine DMZREFQ Seizure disorder 8A6Z Approved [28]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [29]
Estradiol Acetate DM07U2A Hormone replacement therapy 8E01 Approved [29]
Estradiol Cypionate DM27Z5T Hormone replacement therapy 8E01 Approved [29]
Estradiol Valerate DM8MC6O Hormone replacement therapy 8E01 Approved [29]
Estriol DMOEM2I Hormone deficiency 5A61.1 Approved [30]
Ethanol DMDRQZU Chronic pain MG30 Approved [31]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [14]
Etodolac DM6WJO9 Osteoarthritis FA00-FA05 Approved [32]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [33]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [34]
Febuxostat DMDEXQ0 Hyperuricaemia 5C55.Y Approved [35]
Flurbiprofen DMGN4BY Osteoarthritis FA00-FA05 Approved [36]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [37]
Furosemide DMMQ8ZG Congestive heart failure BD10 Approved [14]
Fusidic Acid DMWVCF3 Acne vulgaris ED80 Approved [38]
Gemfibrozil DMD8Q3J Hyperlipidaemia 5C80 Approved [39]
Glibenclamide DM8JXPZ Diabetic complication 5A2Y Approved [40]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [14]
Hydrocodone bitartrate DMIAPBE N. A. N. A. Approved [41]
Hydromorphone DMHP21E Back pain ME84.Z Approved [42]
Hydroxyprogesterone DMIKQH5 Solid tumour/cancer 2A00-2F9Z Approved [43]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [4]
Indacaterol DMQJHR7 Chronic obstructive pulmonary disease CA22 Approved [44]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [45]
Indomethacin DMSC4A7 Bursitis Approved [21]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [46]
Ketoprofen DMRKXPT Bursitis Approved [47]
Labetalol DMK8U72 Hypertension BA00-BA04 Approved [48]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [14]
Levothyroxine DMHN027 Congenital hypothyroidism Approved [14]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [49]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [13]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [50]
MCI-186 DM8ZHP1 Amyotrophic lateral sclerosis 8B60.0 Approved [51]
Meprobamate DMHM93Y Anxiety Approved [52]
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [53]
Metronidazole DMTIVEN Abscess Approved [14]
Minoxidil DMA2Z4F Alopecia ED70 Approved [54]
MK-8228 DMOB58Q Cytomegalovirus Disease 1D82 Approved [55]
Morphine DMRMS0L Advanced cancer 2A00-2F9Z Approved [56]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [57]
Naltrexone DMUL45H Alcohol dependence 6C40.2 Approved [58]
Naproxen DMZ5RGV Bursitis Approved [59]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [4]
Niflumic Acid DMJ3I1Q Rheumatoid arthritis FA20 Approved [60]
Oxazepam DMXNZM4 Alcohol withdrawal delirium Approved [61]
Oxymetazoline DM8ZXT6 Arrhythmia BC9Z Approved [62]
Phenylbutazone DMAYL0T Chronic pain MG30 Approved [63]
Pirprofen DMMOFHT Dysmenorrhea GA34.3 Approved [64]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [65]
Posaconazole DMUL5EW Aspergillosis 1F20 Approved [66]
Probenecid DMMFWOJ Acute gonococcal cervicitis Approved [67]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [68]
Raloxifene DMDKF3M Osteoporosis FB83.0 Approved [14]
Raltegravir DMYURI6 Human immunodeficiency virus infection 1C62 Approved [69]
Repaglinide DM5SXUV Diabetic complication 5A2Y Approved [70]
Retigabine DMGNYIH Behcet disease 4A62 Approved [71]
Rilpivirine DMJ0QOW Human immunodeficiency virus infection 1C62 Approved [72]
Riluzole DMECBWN Amyotrophic lateral sclerosis 8B60.0 Approved [73]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [50]
Suprofen DMKXJZ7 Miosis LA11.62 Approved [21]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [74]
Telmisartan DMS3GX2 Hypertension BA00-BA04 Approved [75]
Tiagabine DMKSQG0 Epilepsy 8A60-8A68 Approved [76]
Tramadol DMRQD04 Osteoarthritis FA00-FA05 Approved [14]
Trimipramine DM1SC8M Major depressive disorder 6A70.3 Approved [77]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [78]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [79]
Vorinostat DMWMPD4 Adult acute monocytic leukemia Approved [80]
Warfarin DMJYCVW Atrial fibrillation BC81.3 Approved [81]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [82]
Zonisamide DM0DTF7 Alcohol dependence 6C40.2 Approved [76]
Dihydrotestosterone DM3S8XC Prostate hyperplasia GA90 Phase 4 [83]
Oleandomycin DMVAOME N. A. N. A. Phase 4 [84]
Silymarin DMXBYQR N. A. N. A. Phase 4 [85]
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⏷ Show the Full List of 102 Approved Drug(s)
20 Clinical Trial Drug(s) Metabolized by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ABT-492 DMJFD2I Bacterial infection 1A00-1C4Z Phase 3 [86]
Carisbamate DM4Y1SP Epilepsy 8A60-8A68 Phase 3 [87]
Curcumin DMQPH29 Solid tumour/cancer 2A00-2F9Z Phase 3 [88]
GSK1265744 DMT8J0I Human immunodeficiency virus infection 1C62 Phase 3 [89]
LCQ908 DMFLJHQ Familial chylomicronemia syndrome 5C80 Phase 3 [90]
MURAGLITAZAR DMG3NFZ N. A. N. A. Phase 3 [91]
Selinexor DMBD4K3 Multiple myeloma 2A83 Phase 3 [92]
PHENOL DM1QSM3 N. A. N. A. Phase 2/3 [93]
ABT-751 DMNG35S Solid tumour/cancer 2A00-2F9Z Phase 2 [94]
Afimoxifene DMFORDT Breast cancer 2C60-2C65 Phase 2 [95]
BCP-13498 DM2BO9W N. A. N. A. Phase 2 [96]
Cicletanine DMGTZLW Pulmonary arterial hypertension BB01.0 Phase 2 [97]
Flavopiridol DMKSUOI Acute myeloid leukaemia 2A60 Phase 2 [14]
LE-SN38 DMW50NF Colorectal cancer 2B91.Z Phase 2 [98]
PDX-101 DM6OC53 Plasma cell myeloma 2A83.1 Phase 2 [99]
Dapivirine DMJPSIL Human immunodeficiency virus infection 1C62 Phase 1/2 [100]
LM-94 DMW3QGJ N. A. N. A. Phase 1/2 [101]
Capravirine DM9ERH1 Human immunodeficiency virus infection 1C62 Phase 1 [102]
GS-9883 DMMF5IE N. A. N. A. Phase 1 [103]
TAS-103 DM5WDKY Solid tumour/cancer 2A00-2F9Z Phase 1 [104]
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⏷ Show the Full List of 20 Clinical Trial Drug(s)
1 Patented Agent(s) Metabolized by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
EUGENOL DM7US1H Discovery agent N.A. Patented [88]
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3 Discontinued Drug(s) Metabolized by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Phenolphthalein DM5SICT Constipation DD91.1 Withdrawn from market [105]
Gavestinel DM8IL1U Nerve injury ND56.4 Discontinued in Phase 2 [21]
VR-776 DMFQWNI Premature ejaculation HA03.0Z Discontinued in Phase 1 [77]
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5 Investigative Drug(s) Metabolized by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ACMC-1AKLT DMRQ70X N. A. N. A. Investigative [29]
Anthraflavic acid DMN1YFU N. A. N. A. Investigative [88]
Chrysin DM7V2LG Discovery agent N.A. Investigative [88]
Cis-4-hydroxytamoxifen DMRFTB5 N. A. N. A. Investigative [95]
phloretin DMYA50U Discovery agent N.A. Investigative [88]
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References

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2 A review of the pharmacokinetics of abacavir. Clin Pharmacokinet. 2008;47(6):351-71.
3 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
4 Liquid chromatography-tandem mass spectrometry method for measurement of nicotine N-glucuronide: a marker for human UGT2B10 inhibition. J Pharm Biomed Anal. 2011 Jul 15;55(5):964-71.
5 In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69.
6 Binimetinib - European Medicines Agency - European Union
7 Pharmacogenomics in aspirin intolerance. Curr Drug Metab. 2009 Nov;10(9):998-1008.
8 In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation. Drug Metab Dispos. 2005 Nov;33(11):1729-39.
9 Atorvastatin glucuronidation is minimally and nonselectively inhibited by the fibrates gemfibrozil, fenofibrate, and fenofibric acid. Drug Metab Dispos. 2007 Aug;35(8):1315-24.
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11 UGT1A1*28 polymorphism influences glucuronidation of bazedoxifene. Pharmazie. 2015 Feb;70(2):94-6.
12 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.
13 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.
14 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.
15 Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011 May;21(5):280-8.
16 Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Hepatology. 2006 Nov;44(5):1158-70.
17 Evaluation of 3'-azido-3'-deoxythymidine, morphine, and codeine as probe substrates for UDP-glucuronosyltransferase 2B7 (UGT2B7) in human liver microsomes: specificity and influence of the UGT2B7*2 polymorphism. Drug Metab Dispos. 2003 Sep;31(9):1125-33.
18 Effect of common exon variant (p.P364L) on drug glucuronidation by the human UDP-glucuronosyltransferase 1 family. Basic Clin Pharmacol Toxicol. 2011 Dec;109(6):486-93.
19 Drug-drug interaction potential of darolutamide: in vitro and clinical studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759.
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22 Differential effects of phenobarbital on ester and ether glucuronidation of diflunisal in rats. J Pharmacol Exp Ther. 1987 Sep;242(3):1013-8.
23 Use of a human liver microsome bank in drug glucuronidation studies. Toxicol In Vitro. 1991;5(5-6):559-62.
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28 Hepatic UDP-glucuronosyltransferase is responsible for eslicarbazepine glucuronidation. Drug Metab Dispos. 2011 Sep;39(9):1486-94.
29 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
30 Stimulation of microsomal uridine diphosphate glucuronyltransferase by glucuronic acid derivatives. Biochem J. 1974 Apr;139(1):243-9.
31 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
32 Stereoselective glucuronidation and hydroxylation of etodolac by UGT1A9 and CYP2C9 in man. Xenobiotica. 2004 May;34(5):449-61.
33 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
34 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
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36 Predominant contribution of UDP-glucuronosyltransferase 2B7 in the glucuronidation of racemic flurbiprofen in the human liver. Drug Metab Dispos. 2007 Jul;35(7):1182-7.
37 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.
38 Fusidic acid inhibits hepatic transporters and metabolic enzymes: potential cause of clinical drug-drug interaction observed with statin coadministration. Antimicrob Agents Chemother. 2016 Sep 23;60(10):5986-94.
39 The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos. 2007 Nov;35(11):2040-4.
40 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.
41 Pharmacokinetic drug interactions of morphine, codeine, and their derivatives: theory and clinical reality, Part II. Psychosomatics. 2003 Nov-Dec;44(6):515-20.
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43 The glucuronidation of Delta4-3-Keto C19- and C21-hydroxysteroids by human liver microsomal and recombinant UDP-glucuronosyltransferases (UGTs): 6alpha- and 21-hydroxyprogesterone are selective substrates for UGT2B7. Drug Metab Dispos. 2007 Mar;35(3):363-70.
44 Use of indacaterol for the treatment of COPD: a pharmacokinetic evaluation. Expert Opin Drug Metab Toxicol. 2014 Jan;10(1):129-37.
45 Inhibition of bilirubin metabolism induces moderate hyperbilirubinemia and attenuates ANG II-dependent hypertension in mice. Am J Physiol Regul Integr Comp Physiol. 2009 Sep;297(3):R738-43.
46 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.
47 Association between the UGT1A1*28 allele and hyperbilirubinemia in HIV-positive patients receiving atazanavir: a meta-analysis. Biosci Rep. 2019 May 2;39(5). pii: BSR20182105.
48 Regulation of UDP-glucuronosyltransferase (UGT) 1A1 by progesterone and its impact on labetalol elimination. Xenobiotica. 2008 Jan;38(1):62-75.
49 FDA Label of Liothyronine sodium. The 2020 official website of the U.S. Food and Drug Administration.
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51 A novel administration route for edaravone: I. Effects of metabolic inhibitors on skin permeability of edaravone. Int J Pharm. 2009 May 8;372(1-2):33-8.
52 Solid-phase synthesis of drug glucuronides by immobilized glucuronosyltransferase. J Med Chem. 1976 May;19(5):679-83.
53 Pharmacogenomics in drug-metabolizing enzymes catalyzing anticancer drugs for personalized cancer chemotherapy. Curr Drug Metab. 2007 Aug;8(6):554-62.
54 Human udp-glucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid. Drug Metab Dispos. 2004 Apr;32(4):413-23.
55 Pharmacogenetic analysis of OATP1B1, UGT1A1, and BCRP variants in relation to the pharmacokinetics of letermovir in previously conducted clinical studies. J Clin Pharmacol. 2019 Sep;59(9):1236-1243.
56 Contribution of UDP-glucuronosyltransferase 1A1 and 1A8 to morphine-6-glucuronidation and its kinetic properties. Drug Metab Dispos. 2008 Apr;36(4):688-94.
57 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
58 In vivo chronic exposure to heroin or naltrexone selectively inhibits liver microsome formation of estradiol-3-glucuronide in the rat. Biochem Pharmacol. 2008 Sep 1;76(5):672-9.
59 Influence of mutations associated with Gilbert and Crigler-Najjar type II syndromes on the glucuronidation kinetics of bilirubin and other UDP-glucuronosyltransferase 1A substrates. Pharmacogenet Genomics. 2007 Dec;17(12):1017-29.
60 Identification of human UDP-glucuronosyltransferase responsible for the glucuronidation of niflumic acid in human liver. Pharm Res. 2006 Jul;23(7):1502-8.
61 Evidence for oxazepam as an in vivo probe of UGT2B15: oxazepam clearance is reduced by UGT2B15 D85Y polymorphism but unaffected by UGT2B17 deletion. Br J Clin Pharmacol. 2009 Nov;68(5):721-30.
62 Identification and characterization of oxymetazoline glucuronidation in human liver microsomes: evidence for the involvement of UGT1A9. J Pharm Sci. 2011 Feb;100(2):784-93.
63 Identification of human UDP-glucuronosyltransferase isoform(s) responsible for the C-glucuronidation of phenylbutazone. Arch Biochem Biophys. 2006 Oct 1;454(1):72-9.
64 Glucuronidation of 2-arylpropionic acids pirprofen, flurbiprofen, and ibuprofen by liver microsomes. Drug Metab Dispos. 1990 Sep-Oct;18(5):692-7.
65 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.
66 Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of posaconazole (Noxafil). Drug Metab Dispos. 2004 Feb;32(2):267-71.
67 Modulation of 3'-azido-3'-deoxythymidine catabolism by probenecid and acetaminophen in freshly isolated rat hepatocytes. Biochem Pharmacol. 1991 Sep 12;42(7):1475-80.
68 Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
69 Successful tacrolimus treatment following renal transplant in a HIV-infected patient with raltegravir previously treated with a protease inhibitor based regimen. Drug Metabol Drug Interact. 2011;26(3):139-41.
70 Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism. Br J Clin Pharmacol. 2010 Dec;70(6):870-80.
71 N-Glucuronidation of the antiepileptic drug retigabine: results from studies with human volunteers, heterologously expressed human UGTs, human liver, kidney, and liver microsomal membranes of Crigler-Najjar type II. Metabolism. 2006 Jun;55(6):711-21.
72 Human biotransformation of the nonnucleoside reverse transcriptase inhibitor rilpivirine and a cross-species metabolism comparison. Antimicrob Agents Chemother. 2013 Oct;57(10):5067-79.
73 Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitro. J Pharmacol Exp Ther. 1997 Sep;282(3):1465-72.
74 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
75 The impact of pharmacogenetics of metabolic enzymes and transporters on the pharmacokinetics of telmisartan in healthy volunteers. Pharmacogenet Genomics. 2011 Sep;21(9):523-30.
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