Details of Drug-Metabolizing Enzyme (DME)

General Information of DME (ID: DME0041)
DME Name UDP-glucuronosyltransferase 1A3 (UGT1A3), Homo sapiens
Synonyms UDP-glucuronosyltransferase family 1 member A3; UDP-glucuronosyltransferase 1-C; UDP-glucuronosyltransferase 1-3; UDPGT 1-3; UGT-1C; UGT1*3; UGT1-03; UGT1.3; UGT1A3; UGT1C
Gene Name UGT1A3
UniProt ID
UD13_HUMAN
Gene ID
54659
EC Number    EC: 2.4.1.17     (Click to Show/Hide the Complete EC Tree)
Transferase
Glycosyltransferases
Hexosyltransferase
EC: 2.4.1.17
Lineage    Species: Homo sapiens     (Click to Show/Hide the Complete Species Lineage)
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Interactome
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       Interactions between Microbiome and DME (MICBIO)                       
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       Interactions between Xenobiotics and DME (XEOTIC)                      
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       Interactions between Host Protein and DME (HOSPPI)                     
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      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Sequence
MATGLQVPLPWLATGLLLLLSVQPWAESGKVLVVPIDGSHWLSMREVLRELHARGHQAVV
LTPEVNMHIKEENFFTLTTYAISWTQDEFDRHVLGHTQLYFETEHFLKKFFRSMAMLNNM
SLVYHRSCVELLHNEALIRHLNATSFDVVLTDPVNLCAAVLAKYLSIPTVFFLRNIPCDL
DFKGTQCPNPSSYIPRLLTTNSDHMTFMQRVKNMLYPLALSYICHAFSAPYASLASELFQ
REVSVVDILSHASVWLFRGDFVMDYPRPIMPNMVFIGGINCANRKPLSQEFEAYINASGE
HGIVVFSLGSMVSEIPEKKAMAIADALGKIPQTVLWRYTGTRPSNLANNTILVKWLPQND
LLGHPMTRAFITHAGSHGVYESICNGVPMVMMPLFGDQMDNAKRMETKGAGVTLNVLEMT
SEDLENALKAVINDKSYKENIMRLSSLHKDRPVEPLDLAVFWVEFVMRHKGAPHLRPAAH
DLTWYQYHSLDVIGFLLAVVLTVAFITFKCCAYGYRKCLGKKGRVKKAHKSKTH
Pathway Ascorbate and aldarate metabolism (hsa00053 )
Chemical carcinogenesis (hsa05204 )
Drug metabolism - cytochrome P450 (hsa00982 )
Drug metabolism - other enzymes (hsa00983 )
Metabolic pathways (hsa01100 )
Metabolism of xenobiotics by cytochrome P450 (hsa00980 )
Pentose and glucuronate interconversions (hsa00040 )
Porphyrin and chlorophyll metabolism (hsa00860 )
Retinol metabolism (hsa00830 )
Steroid hormone biosynthesis (hsa00140 )
Function This enzyme is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.
Full List of Drug(s) Metabolized by This DME
      Drugs Approved by FDA Click to Show/Hide the Full List of Drugs:        66 Drugs
Darolutamide
 Drug Info Approved Prostate cancer ICD11: 2C82 [1]
Dronabinol
 Drug Info Approved Anorexia nervosa ICD11: 6B80 [2]
Diclofenac sodium
 Drug Info Approved Osteoarthritis ICD11: FA00 [3]
Montelukast sodium
 Drug Info Approved Asthma ICD11: CA23 [2], [4]
Ethinyl estradiol
 Drug Info Approved Menopausal disorder ICD11: GA30 [5]
Irbesartan
 Drug Info Approved Essential hypertension ICD11: BA00 [2]
Pitavastatin
 Drug Info Approved Hypertriglyceridaemia ICD11: 5C80 [6]
Valproic acid
 Drug Info Approved Epilepsy ICD11: 8A60 [7]
Aprepitant
 Drug Info Approved Functional nausea/vomiting ICD11: DD90 [8]
Cyproheptadine
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [9]
Mirabegron
 Drug Info Approved Overactive bladder ICD11: GC50 [10]
Opicapone
 Drug Info Approved Parkinsonism ICD11: 8A00 [11]
Chenodeoxycholic acid
 Drug Info Approved Cholelithiasis ICD11: DC11 [12]
Axitinib
 Drug Info Approved Renal cell carcinoma ICD11: 2C90 [13]
Lasofoxifene
 Drug Info Approved Osteoporosis ICD11: FB83 [14]
Naproxen
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [15]
Repaglinide
 Drug Info Approved Diabetes mellitus ICD11: 5A10 [16]
Belinostat
 Drug Info Approved Anaplastic large cell lymphoma ICD11: 2A90 [17], [18]
Deferasirox
 Drug Info Approved Hyperphosphatemia ICD11: 5C64 [19]
Desvenlafaxine
 Drug Info Approved Major depressive disorder ICD11: 6A70-6A7Z [20]
Dolutegravir sodium
 Drug Info Approved Human immunodeficiency virus infection ICD11: 1C60 [21]
Dronedarone hydrochloride
 Drug Info Approved Atrial fibrillation ICD11: BC81 [22]
Etodolac
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [2]
Exjade
 Drug Info Approved Hyperphosphatemia ICD11: 5C64 [23]
Ibuprofen
 Drug Info Approved Anaesthesia ICD11: 8E22 [2]
Letermovir
 Drug Info Approved Cytomegalovirus infection ICD11: 1D82 [24]
Morphine
 Drug Info Approved Anaesthesia ICD11: 8E22 [9]
Morphine
 Drug Info Approved Anaesthesia ICD11: 8E22 [25], [26], [27]
Simvastatin
 Drug Info Approved Dyslipidaemia ICD11: 5C81 [28]
Anastrozole
 Drug Info Approved Breast cancer ICD11: 2C60 [29]
Atorvastatin calcium
 Drug Info Approved Dyslipidaemia ICD11: 5C81 [30]
Buprenorphine hydrochloride
 Drug Info Approved Anaesthesia ICD11: 8E22 [31]
Clofazimine
 Drug Info Approved Crohn disease ICD11: DD70 [32]
Etravirine
 Drug Info Approved Human immunodeficiency virus infection ICD11: 1C60 [33]
Gemfibrozil
 Drug Info Approved Hypertriglyceridaemia ICD11: 5C80 [34]
Nalbuphine
 Drug Info Approved Pain ICD11: MG30-MG3Z [35]
Nalmefene
 Drug Info Approved Opiate dependence ICD11: 6C43 [36]
Avapritinib
 Drug Info Approved Gastrointestinal stromal tumour ICD11: 2B5B [37]
Candesartan cilexetil
 Drug Info Approved Essential hypertension ICD11: BA00 [2]
Desloratadine
 Drug Info Approved Allergic rhinitis ICD11: CA08 [38]
Empagliflozin
 Drug Info Approved Diabetes mellitus ICD11: 5A10 [39]
Ezetimibe
 Drug Info Approved Hypertriglyceridaemia ICD11: 5C80 [40]
Ketotifen
 Drug Info Approved Conjunctivitis ICD11: 9A60 [41]
Ketotifen
 Drug Info Approved Conjunctivitis ICD11: 9A60 [42]
Lamotrigine
 Drug Info Approved Bipolar disorder ICD11: 6A60 [43]
Losartan potassium
 Drug Info Approved Essential hypertension ICD11: BA00 [2]
Lovastatin
 Drug Info Approved Hypertriglyceridaemia ICD11: 5C80 [28]
Pitavastatin calcium
 Drug Info Approved Hypertriglyceridaemia ICD11: 5C80 [44]
Troglitazone
 Drug Info Approved Diabetes mellitus ICD11: 5A10 [45]
Ambrisentan
 Drug Info Approved Pulmonary hypertension ICD11: BB01 [46]
Cerivastatin sodium
 Drug Info Approved Hypertriglyceridaemia ICD11: 5C80 [47]
Eltrombopag olamine
 Drug Info Approved Thrombocytopenia ICD11: 3B64 [48]
Elvitegravir
 Drug Info Approved Human immunodeficiency virus infection ICD11: 1C60 [49]
Flurbiprofen sodium
 Drug Info Approved Rheumatoid arthritis ICD11: FA20 [2]
Hesperidin
 Drug Info Approved Vascular purpura ICD11: 3B60 [50]
Hydromorphone
 Drug Info Approved Anaesthesia ICD11: 8E22 [51]
Loratadine
 Drug Info Approved Allergic rhinitis ICD11: CA08 [52]
Vorinostat
 Drug Info Approved Cutaneous T-cell lymphoma ICD11: 2B01 [53]
Baloxavir marboxil
 Drug Info Approved Influenza virus infection ICD11: 1E30 [54]
Baloxavir marboxil
 Drug Info Approved Influenza virus infection ICD11: 1E30 [55]
Enasidenib
 Drug Info Approved Acute myeloid leukaemia ICD11: 2A60 [56]
Fulvestrant
 Drug Info Approved Breast cancer ICD11: 2C60 [57]
Lorlatinib
 Drug Info Approved Lung cancer ICD11: 2C25 [58]
Telmisartan
 Drug Info Approved Essential hypertension ICD11: BA00 [59]
Telmisartan
 Drug Info Approved Essential hypertension ICD11: BA00 [60]
LAROPIPRANT
 Drug Info Phase 4 Atherosclerosis ICD11: BA80 [63]
      Drugs in Phase 4 Clinical Trial Click to Show/Hide the Full List of Drugs:          3 Drugs
Ethinylestradiol propanesulfonate
 Drug Info Phase 4 Prostate cancer ICD11: 2C82 [61], [62]
Retigabine
 Drug Info Phase 4 Epilepsy ICD11: 8A60 [64]
Dexibuprofen
 Drug Info Phase 4 Osteoarthritis ICD11: FA00 [2]
      Drugs in Phase 3 Clinical Trial Click to Show/Hide the Full List of Drugs:        15 Drugs
Selumetinib
 Drug Info Phase 3 Neurofibromatosis ICD11: LD2D [65]
ABL001
 Drug Info Phase 3 Chronic myelogenous leukaemia ICD11: 2A20 [66]
BMS-298585
 Drug Info Phase 3 Diabetes mellitus ICD11: 5A10 [67]
LAU-7b
 Drug Info Phase 3 Macular degeneration ICD11: 9B78 [68]
Heroin
 Drug Info Phase 3 Opiate dependence ICD11: 6C43 [69]
Losartan
 Drug Info Phase 3 Hypertension ICD11: BA00-BA04 [70]
TAK-875
 Drug Info Phase 3 Diabetes mellitus ICD11: 5A10 [71]
LCQ908-NXA
 Drug Info Phase 3 Hypertriglyceridaemia ICD11: 5C80 [72]
Fevipiprant
 Drug Info Phase 3 Asthma ICD11: CA23 [73]
Glinsuna
 Drug Info Phase 3 Diabetes mellitus ICD11: 5A10 [2]
Glinsuna
 Drug Info Phase 3 Diabetes mellitus ICD11: 5A10 [2], [74]
KAD-1229
 Drug Info Phase 3 Diabetes mellitus ICD11: 5A10 [2]
Ag-221
 Drug Info Phase 3 Acute myelogenous leukaemia ICD11: 2A41 [75]
Atorvastatin
 Drug Info Phase 3 Hypertriglyceridaemia ICD11: 5C80 [30]
CS-011
 Drug Info Phase 3 Diabetes mellitus ICD11: 5A10 [76]
      Drugs in Phase 2 Clinical Trial Click to Show/Hide the Full List of Drugs:        11 Drugs
PF-06463922
 Drug Info Phase 2 Lung cancer ICD11: 2C25 [77]
Puerarin
 Drug Info Phase 2 Alcohol dependence ICD11: 6C40 [78]
BAICALEIN
 Drug Info Phase 2 Influenza virus infection ICD11: 1E30-1E32 [79]
LJN452
 Drug Info Phase 2 Primary biliary cholangitis ICD11: DB96 [80]
S-297995
 Drug Info Phase 2 Opiate dependence ICD11: 6C43 [81]
PT2385
 Drug Info Phase 2 Von hippel-lindau disease ICD11: 5A75 [82]
AMG 232
 Drug Info Phase 2 Merkel cell carcinoma ICD11: 2C34 [83]
BIA 3-202
 Drug Info Phase 2 Parkinsonism ICD11: 8A00 [84]
BIIB074
 Drug Info Phase 2 Bipolar disorder ICD11: 6A60 [85]
MPC-4326
 Drug Info Phase 2 Human immunodeficiency virus infection ICD11: 1C60 [86]
Sitafloxacin
 Drug Info Phase 2 Escherichia coli infection ICD11: 1A03 [87]
      Drugs in Phase 1 Clinical Trial Click to Show/Hide the Full List of Drugs:          4 Drugs
CB-3304
 Drug Info Phase 1/2 Chronic lymphocytic leukaemia ICD11: 2A82 [88]
BRN-0183227
 Drug Info Phase 1 Acute coronary syndrome ICD11: BA4Z [89]
Norbuprenorphine
 Drug Info Phase 1 Human immunodeficiency virus infection ICD11: 1C60-1C62 [90]
OTSSP167
 Drug Info Phase 1 Myelodysplastic syndrome ICD11: 2A37 [91]
      Discontinued/withdrawn Drugs Click to Show/Hide the Full List of Drugs:          5 Drugs
Lexacalcitol
 Drug Info Discontinued in Phase 2 Solid tumour/cancer ICD11: 2A00-2F9Z [92], [93]
T-5224
 Drug Info Discontinued in Phase 2 Rheumatoid arthritis ICD11: FA20 [94]
GV-150526
 Drug Info Discontinued Cerebral stroke ICD11: 8B11 [2]
ML-3000
 Drug Info Discontinued Osteoarthritis ICD11: FA00 [95]
ML-3000
 Drug Info Discontinued Osteoarthritis ICD11: FA00 [2]
      Preclinical/investigative Agents Click to Show/Hide the Full List of Drugs:          1 Drugs
Hydroxyestrone
 Drug Info Investigative Discovery agent ICD: N.A. [96]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR009851 Ambrisentan Ambrisentan glucuronide Conjugation - Glucuronidation Ambrisentan [97]
MR005430 Avapritinib M499 Oxidation - Oxidationn deamination Avapritinib [37]
MR009888 Axitinib Axitinib Metabolite M7 Unclear - Unclear axitinib [13]
MR008613 BAICALEIN Baicalein-7-O-glucuronide Unclear - Unclear BAICALEIN [98]
MR014170 Baloxavir marboxil Baloxavir acid Unclear - Unclear Baloxavir marboxil [55]
MR008292 BIIB074 BIIB074 metabolite M13 Conjugation - N-carbamoyl glucuronidation BIIB074 [85]
MR000383 BMS-298585 BMS-298585 metabolite M13 Unclear - Unclear BMS-298585 [99], [100]
MR003858 Hesperetin Hesperetin-sulfo-O-glucuronide Unclear - Unclear BRN-0183227 [89]
MR000487 Norbuprenorphine Norbuprenorphine glucuronide Conjugation - Glucuronidation Buprenorphine hydrochloride [101], [102], [103]
MR000552 Candesartan Candesartan N2-glucuronide Conjugation - N-Glucuronidation Candesartan cilexetil [70]
MR006094 CB-3304 Glucuronic acid conjugates Conjugation - Conjugation CB-3304 [88]
MR002546 Chenodeoxycholic acid Chenodeoxycholic acid glucuronide Unclear - Unclear Chenodeoxycholic acid [12]
MR006564 Hydrated clofazimine Hydrated clofazimine glucuronidation Conjugation - Glucuronidation Clofazimine [32]
MR006560 Hydrolytic-deaminated clofazimine Hydrolytic-deaminated clofazimine glucuronide Conjugation - Glucuronidation Clofazimine [32]
MR006562 Hydroxylated clofazimine Hydroxylated clofazimine glucuronidation Conjugation - Glucuronidation Clofazimine [32]
MR007435 CYC-202 CYC-202 M6 Conjugation - Glucuronidation CYC-202 [104]
MR004135 Cyproheptadine Cyproheptadine N-glucuronide Conjugation - N-glucuronidation Cyproheptadine [105]
MR000755 Deferasirox Deferasirox metabolite M3 Conjugation - Glucuronidation Deferasirox [106]
MR000768 3-hydroxydesloratadine 3-hydroxydesloratadine O-glucuronide Conjugation - Glucuronidation Desloratadine [38]
MR002618 Diclofenac sodium Diclofenac acyl glucuronide Conjugation - Glucuronidation Diclofenac sodium [107]
MR006617 Dolutegravir sodium Ether glucuronide dolutegravir (M2) Conjugation - Glucuronidation Dolutegravir sodium [21]
MR006688 11-Nor-9-carboxy-delta-9-THC 11-nor-9-carboxy-delta-9-THC-glucuronide Conjugation - Glucuronidation Dronabinol [2]
MR006705 Phenol-dronedarone Phenol-dronedarone glucuronide Conjugation - Glucuronidation Dronedarone hydrochloride [22]
MR000907 Eltrombopag olamine Eltrombopag olamine glucuronide conjugate Conjugation - Glucuronidation Eltrombopag olamine [108]
MR009951 Elvitegravir Elvitegravir Metabolite M4 Conjugation - Glucuronidation Elvitegravir [49]
MR006862 Empagliflozin Empagliflozin-2-glucuronide Conjugation - O-glucuronidation Empagliflozin [109]
MR006868 AGI-16903 Unclear Unclear - Unclear Enasidenib [56]
MR000937 Ertugliflozin Ertugliflozin metabolite M4b Conjugation - Glucuronidation Ertugliflozin [110]
MR002720 Ethinyl estradiol N-desmethylzopiclone Conjugation - O-Glucuronidation Ethinyl estradiol [5]
MR007155 16alpha-methoxyethinylestradiol 16alpha-methoxyethinylestradiol-glucuronide Conjugation - O-glucuronidation Ethinylestradiol propanesulfonate [61], [62]
MR007143 2-methoxyethinylestradiol 2-methoxyethinylestradiol-glucuronide Conjugation - O-glucuronidation Ethinylestradiol propanesulfonate [61], [62]
MR007146 4-methoxyethinylestradiol 4-methoxyethinylestradiol-glucuronide Conjugation - O-glucuronidation Ethinylestradiol propanesulfonate [61], [62]
MR007149 6-methoxyethinylestradiol 6-methoxyethinylestradiol-glucuronide Conjugation - O-glucuronidation Ethinylestradiol propanesulfonate [61], [62]
MR007152 7-methoxyethinylestradiol 7-methoxyethinylestradiol-glucuronide Conjugation - O-glucuronidation Ethinylestradiol propanesulfonate [61], [62]
MR007157 Ethinylestradiol propanesulfonate Ethinylestradiol-glucuronide Conjugation - O-glucuronidation Ethinylestradiol propanesulfonate [61]
MR002737 Etodolac Etodolac acyl glucuronide Conjugation - Glucuronidation Etodolac [111]
MR000988 Etravirine metabolite M1 Etravirine metabolite M7 Conjugation - Glucuronidation Etravirine [112]
MR001008 Ezetimibe Ezetimibe-glucuronide Conjugation - Glucuronidation Ezetimibe [113], [114], [115], [116]
MR012009 Fevipiprant AG met Unclear - Unclear Fevipiprant [73], [117]
MR005044 Flurbiprofen sodium Flurbiprofen glucuronide Conjugation - Glucuronidation Flurbiprofen sodium [118]
MR001125 Gemfibrozil Gemfibrozil 1-beta-glucuronide metabolite Conjugation - O-Glucuronidation Gemfibrozil [119], [2], [120]
MR012935 Glinsuna Glinsuna Metabolite M1 Conjugation - Glucuronidation Glinsuna [2], [74]
MR005979 GV-150526 Gavestinel acyl glucuronid Conjugation - Glucuronidation GV-150526 [2]
MR013333 Morphine Morphine-3-glucuronide Conjugation - Glucuronidation Heroin [69]
MR013332 Morphine Morphine-6-glucuronide Conjugation - Glucuronidation Heroin [69]
MR005138 Hydromorphone Hydromorphone-3-glucuronide Conjugation - Glucuronidation Hydromorphone [121], [122], [51]
MR007047 Hydroxyestrone 2-hydroxyestrone 2-glucuronide Conjugation - O-glucuronidation Hydroxyestrone [96]
MR004643 Ibuprofen Ibuprofen glucuronide Conjugation - O-glucuronidation Ibuprofen [25], [2]
MR001221 Irbesartan Irbesartan derivative M8 Conjugation - N-Glucuronidation Irbesartan [123], [2]
MR003683 KAD-1229 Mitiglinide carboxyl-glucuronide Conjugation - Conjugation KAD-1229 [124]
MR001376 Ketotifen Ketotifen-N-glucuronide Conjugation - N-Glucuronidation Ketotifen [41], [42]
MR001410 Lamotrigine Lamotrigine-2-N-glucuronide Conjugation - Glucuronidation Lamotrigine [125], [126], [127]
MR001411 Lamotrigine Lamotrigine-5-N-glucuronide Conjugation - Glucuronidation Lamotrigine [125], [128], [127]
MR003709 LAU-7b 4-HPR glucuronide Unclear - Unclear LAU-7b [68]
MR003712 LCQ908-NXA M18.4 Conjugation - Glucuronidation LCQ908-NXA [72], [129]
MR001443 Letermovir Letermovir metabolite M1 Conjugation - O-Glucuronidation Letermovir [24]
MR008303 LJN452 LJN452 metabolite M22 Conjugation - Glucuronidation LJN452 [80]
MR006903 3-Hydroxydesloratadine 3-hydroxydesloratadine O-glucuronide Conjugation - Glucuronidation Loratadine [52]
MR006912 Lorlatinib Lorlatinib benzoic acid metabolite (M8) Oxidation - Oxidationn cleavage Lorlatinib [130]
MR013898 Losartan LOG Unclear - Unclear Losartan [70]
MR013899 Losartan LN1G Unclear - Unclear Losartan [70]
MR013900 Losartan LN2G Unclear - Unclear Losartan [70]
MR006915 Losartan potassium Losartan N2-glucuronide Conjugation - N-glucuronidation Losartan potassium [131]
MR006922 beta-hydroxy acid of lovastatin 6'-beta-Hydroxylovastatin Oxidation - Hydrolyzationn Lovastatin [28]
MR001651 17alpha-Ethinylestradiol N-desmethylzopiclone metabolite Conjugation - O-Glucuronidation Mestranol [61], [5], [132]
MR004783 Mirabegron Mirabegron M13 metabolite Conjugation - Glucuronidation Mirabegron [10]
MR007632 ML-3000 Licofelone acyl glucuronide (M1) Conjugation - Acyl glucuronidation ML-3000 [2]
MR004798 Montelukast sodium Montelukast metabolite M1 Conjugation - O-glucuronidation Montelukast sodium [2], [4]
MR004803 Montelukast sodium Montelukast ether glucuronide Unclear - Unclear Montelukast sodium [4]
MR004804 Morphine Morphine glucuronide Conjugation - Glucuronidation Morphine [25], [26], [27]
MR009658 MPC-4326 Mono-BVMG () Conjugation - Glucuronidation MPC-4326 [133]
MR009658 MPC-4326 Mono-BVMG () Conjugation - Glucuronidation MPC-4326 [86]
MR009659 MPC-4326 Mono-BVMG () Conjugation - Glucuronidation MPC-4326 [86]
MR009660 MPC-4326 Di-BVMG Conjugation - Glucuronidation MPC-4326 [86]
MR008827 Nalbuphine Nalbuphine-3-beta-D-glucuronide Conjugation - Glucuronidation Nalbuphine [35]
MR010774 Nalmefene Nalmefene 3-O-glucuronide Conjugation - O-glucuronidation Nalmefene [134]
MR004873 O-Desmethylnaproxen O-Desmethylnaproxen acyl glucuronide Conjugation - Glucuronidation Naproxen [2]
MR001735 Niclosamide Niclosamide-2-O-glucuronide metabolite Conjugation - Glucuronidation Niclosamide [135]
MR013758 Norbuprenorphine Norbuprenorphine metabolite M1 Unclear - Unclear Norbuprenorphine [31]
MR013702 Opicapone BIA 9-1106 Conjugation - Glucuronidation Opicapone [136]
MR008449 OTSSP167 OTS167-G Unclear - Unclear OTSSP167 [91]
MR011750 PF-06463922 PF-06895751 (M8) Unclear - Unclear PF-06463922 [77]
MR002069 Pitavastatin Pitavastatin glucuronide Conjugation - Glucuronidation Pitavastatin calcium [137]
MR013649 PT2385 M10 PT2385 M1 Multi-steps Reaction - Hydroxylation; Glucuronide conjugation PT2385 [82]
MR013647 PT2385 M2 PT2385 M11 Multi-steps Reaction - Hydroxylation; Glucuronide conjugation PT2385 [82]
MR013643 PT2385 M7 PT2385 M12 Multi-steps Reaction - Oxidative Defluorination; Glucuronide conjugation PT2385 [82]
MR008594 Puerarin Puerarin-7-O-glucuronide Conjugation - Glucuronidation Puerarin [78]
MR013054 Repaglinide Repaglinide M7 Conjugation - Glucuronidation Repaglinide [16]
MR005236 Retigabine Retigabine-N2-glucuronide Conjugation - Glucuronidation Retigabine [138], [64], [139]
MR005237 Retigabine Retigabine-N4-glucuronide Conjugation - Glucuronidation Retigabine [138], [64], [139]
MR011495 S-297995 Naidemedine-3-G Conjugation - Glucuronide conjugation S-297995 [140]
MR013437 Simvastatin Unclear Unclear - Unclear Simvastatin [141]
MR008323 Sitafloxacin Sitafloxacin metabolite M1 Conjugation - Glucuronidation Sitafloxacin [87]
MR009352 T-5224 T-5224 G3 Conjugation - Hydroxyl O-glucosidation T-5224 [94]
MR006476 TAK-875 T-167642 Unclear - Unclear TAK-875 [71]
MR006473 TAK-875 Metabolite M-I TAK-875 Metabolite M-I-G Conjugation - Conjugation TAK-875 [71]
MR002375 Telmisartan Telmisartan glucuronide Conjugation - Glucuronidation Telmisartan [59]
MR002497 Valproic acid Valproic acid beta-O-glucuronide metabolite Oxidation - Dehydrogenation Valproic acid [2]
⏷ Show the Full List of 98 MR(s)
References
1 Drug-drug interaction potential of darolutamide: in vitro and clinical studies. Eur J Drug Metab Pharmacokinet. 2019 Dec;44(6):747-759.
2 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.
3 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
4 In vitro metabolism of montelukast by cytochrome P450s and UDP-glucuronosyltransferases. Drug Metab Dispos. 2015 Dec;43(12):1905-16.
5 Human bilirubin UDP-glucuronosyltransferase catalyzes the glucuronidation of ethinylestradiol Mol Pharmacol. 1993 Apr;43(4):649-54.
6 DrugBank(Pharmacology-Metabolism):Pitavastatin
7 Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
8 In vitro glucuronidation of aprepitant: a moderate inhibitor of UGT2B7 Xenobiotica. 2015;45(11):990-8. doi: 10.3109/00498254.2015.1038743.
9 Glucuronidation of amines and other xenobiotics catalyzed by expressed human UDP-glucuronosyltransferase 1A3. Drug Metab Dispos. 1998 Jun;26(6):507-12.
10 Identification of Uridine 5'-Diphosphate-Glucuronosyltransferases Responsible for the Glucuronidation of Mirabegron, a Potent and Selective (3)-Adrenoceptor Agonist, in Human Liver Microsomes
11 Metabolism and disposition of opicapone in the rat and metabolic enzymes phenotyping
12 Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Hepatology. 2006 Nov;44(5):1158-70.
13 In Vitro Kinetic Characterization of Axitinib Metabolism
14 DrugBank(Pharmacology-Metabolism):Lasofoxifene
15 S-Naproxen and desmethylnaproxen glucuronidation by human liver microsomes and recombinant human UDP-glucuronosyltransferases (UGT): role of UGT2B7 in the elimination of naproxen. Br J Clin Pharmacol. 2005 Oct;60(4):423-33.
16 Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism. Br J Clin Pharmacol. 2010 Dec;70(6):870-80.
17 Glucuronidation by UGT1A1 is the dominant pathway of the metabolic disposition of belinostat in liver cancer patients. PLoS One. 2013;8(1):e54522.
18 In vitro characterization of belinostat glucuronidation: demonstration of both UGT1A1 and UGT2B7 as the main contributing isozymes
19 Deferasirox pharmacogenetic influence on pharmacokinetic, efficacy and toxicity in a cohort of pediatric patients. Pharmacogenomics. 2017 Apr;18(6):539-554.
20 Impact of polymorphisms in CYP and UGT enzymes and ABC and SLCO1B1 transporters on the pharmacokinetics and safety of desvenlafaxine
21 Metabolism, excretion, and mass balance of the HIV-1 integrase inhibitor dolutegravir in humans
22 DrugBank(Pharmacology-Metabolism):Dronedarone hydrochloride
23 LABEL:Exjade
24 LABEL:PREVYMIS- letermovir tablet, film coated PREVYMIS- letermovir injection, solution
25 Pharmacogenomics knowledge for personalized medicine Clin Pharmacol Ther. 2012 Oct;92(4):414-7. doi: 10.1038/clpt.2012.96.
26 Metabolism and pharmacokinetics of morphine in neonates: A review
27 Morphine metabolism, transport and brain disposition
28 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
29 In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69.
30 UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7.
31 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.
32 Characterization of Clofazimine Metabolism in Human Liver Microsomal Incubation In Vitro
33 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.
34 Comprehensive pharmacogenomic study reveals an important role of UGT1A3 in montelukast pharmacokinetics. Clin Pharmacol Ther. 2018 Jul;104(1):158-168.
35 A dual system platform for drug metabolism: Nalbuphine as a model compound
36 Ema.europa:Nalmefene
37 FDA label:Avapritinib
38 A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement Drug Metab Dispos. 2015 Apr;43(4):523-33. doi: 10.1124/dmd.114.062620.
39 Empagliflozin (Jardiance): a novel SGLT2 inhibitor for the treatment of type-2 diabetes. P T. 2015 Jun;40(6):364-8.
40 Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.
41 N+-glucuronidation, a common pathway in human metabolism of drugs with a tertiary amine group Drug Metab Dispos. 1998 Sep;26(9):830-7.
42 Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos. 2013 Jul;41(7):1389-97.
43 Variation in glucuronidation of lamotrigine in human liver microsomes. Xenobiotica. 2009 May;39(5):355-63.
44 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
45 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
46 Clinical pharmacokinetics and drug-drug interactions of endothelin receptor antagonists in pulmonary arterial hypertension. J Clin Pharmacol. 2012 Dec;52(12):1784-805.
47 Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011 May;21(5):280-8.
48 Eltrombopag for use in children with immune thrombocytopenia Blood Adv. 2018 Feb 27;2(4):454-461. doi: 10.1182/bloodadvances.2017010660.
49 In vitro resistance selections using elvitegravir, raltegravir, and two metabolites of elvitegravir M1 and M4
50 U. S. FDA Label -Hesperidin
51 Opioid therapies and cytochrome p450 interactions. J Pain Symptom Manage. 2012 Dec;44(6 Suppl):S4-14.
52 Advances in high-resolution MS and hepatocyte models solve a long-standing metabolism challenge: the loratadine story. Bioanalysis. 2016 Aug;8(16):1645-62.
53 Uridine 5'-diphospho-glucuronosyltransferase genetic polymorphisms and response to cancer chemotherapy. Future Oncol. 2010 Apr;6(4):563-85.
54 FDA Label of Baloxavir marboxil. The 2020 official website of the U.S. Food and Drug Administration.
55 Pharmacokinetics and safety of a novel influenza treatment (baloxavir marboxil) in Korean subjects compared with Japanese subjects
56 FDA:Enasidenib
57 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.
58 FDA label of Lorlatinib. The 2020 official website of the U.S. Food and Drug Administration.
59 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.
60 In vitro glucuronidation of the angiotensin II receptor antagonist telmisartan in the cat: a comparison with other species
61 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.
62 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.
63 Metabolism of MK-0524, a prostaglandin D2 receptor 1 antagonist, in microsomes and hepatocytes from preclinical species and humans
64 Retigabine N-glucuronidation and its potential role in enterohepatic circulation. Drug Metab Dispos. 1999 May;27(5):605-12.
65 Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens
66 Pharmacokinetic drug interactions of asciminib with the sensitive cytochrome P450 probe substrates midazolam, warfarin, and repaglinide in healthy participants
67 Characterization of the UDP glucuronosyltransferase activity of human liver microsomes genotyped for the UGT1A1*28 polymorphism. Drug Metab Dispos. 2007 Dec;35(12):2270-80.
68 Characterization of the metabolism of fenretinide by human liver microsomes, cytochrome P450 enzymes and UDP-glucuronosyltransferases. Br J Pharmacol. 2011 Feb;162(4):989-99.
69 PharmGKB:Heroin
70 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.
71 Disposition and metabolism of the G protein-coupled receptor 40 agonist TAK-875 (fasiglifam) in rats, dogs, and humans. Xenobiotica. 2019 Apr;49(4):433-445.
72 Pradigastat disposition in humans: in vivo and in vitro investigations. Xenobiotica. 2017 Dec;47(12):1077-1089.
73 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.
74 Carboxyl-glucuronidation of mitiglinide by human UDP-glucuronosyltransferases. Biochem Pharmacol. 2007 Jun 1;73(11):1842-51.
75 DrugBank(Pharmacology-Metabolism):Ag-221
76 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.
77 The Effect of Modafinil on the Safety and Pharmacokinetics of Lorlatinib: A Phase I Study in Healthy Participants
78 UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for puerarin metabolism in human liver microsomes
79 Involvement of UDP-glucuronosyltransferases in the extensive liver and intestinal first-pass metabolism of flavonoid baicalein
80 Evaluation of the Absorption, Metabolism, and Excretion of a Single Oral 1-mg Dose of Tropifexor in Healthy Male Subjects and the Concentration Dependence of Tropifexor Metabolism
81 Naldemedine: First Global Approval
82 Metabolic Profiling of the Novel Hypoxia-Inducible Factor 2 Inhibitor PT2385 In Vivo and In Vitro
83 Pharmacokinetics and metabolism of AMG 232, a novel orally bioavailable inhibitor of the MDM2-p53 interaction, in rats, dogs and monkeys: in vitro-in vivo correlation
84 Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation
85 Evaluation of the Pharmacokinetic Interaction Between the Voltage- and Use-Dependent Nav1.7 Channel Blocker Vixotrigine and Carbamazepine in Healthy Volunteers
86 Bevirimat: a novel maturation inhibitor for the treatment of HIV-1 infection. Antivir Chem Chemother. 2008;19(3):107-13.
87 Acyl glucuronidation of fluoroquinolone antibiotics by the UDP-glucuronosyltransferase 1A subfamily in human liver microsomes
88 Metabolic map and bioactivation of the anti-tumour drug noscapine
89 Stratification of Volunteers According to Flavanone Metabolite Excretion and Phase II Metabolism Profile after Single Doses of 'Pera' Orange and 'Moro' Blood Orange Juices
90 Chemical and enzyme-assisted syntheses of norbuprenorphine-3--D-glucuronide
91 Glucuronidation of OTS167 in Humans Is Catalyzed by UDP-Glucuronosyltransferases UGT1A1, UGT1A3, UGT1A8, and UGT1A10
92 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.
93 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.
94 Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms
95 In vitro metabolism of 2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid (licofelone, ML3000), an inhibitor of cyclooxygenase-1 and -2 and 5-lipoxygenase. Drug Metab Dispos. 2008 May;36(5):894-903.
96 Structural and functional studies of UDP-glucuronosyltransferases. Drug Metab Rev. 1999 Nov;31(4):817-99.
97 Effect of ketoconazole on the pharmacokinetic profile of ambrisentan. J Clin Pharmacol. 2009 Jun;49(6):719-24.
98 Hepatic metabolism and disposition of baicalein via the coupling of conjugation enzymes and transporters-in vitro and in vivo evidences
99 Involvement of multiple cytochrome P450 and UDP-glucuronosyltransferase enzymes in the in vitro metabolism of muraglitazar. Drug Metab Dispos. 2007 Jan;35(1):139-49.
100 Glucuronidation as a major metabolic clearance pathway of 14c-labeled muraglitazar in humans: metabolic profiles in subjects with or without bile collection Drug Metab Dispos. 2006 Mar;34(3):427-39. doi: 10.1124/dmd.105.007617.
101 In vitro metabolism study of buprenorphine: evidence for new metabolic pathways. Drug Metab Dispos. 2005 May;33(5):689-95.
102 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.
103 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.
104 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.
105 Human metabolism of cyproheptadine
106 Pharmacokinetics, metabolism, and disposition of deferasirox in beta-thalassemic patients with transfusion-dependent iron overload who are at pharmacokinetic steady state Drug Metab Dispos. 2010 May;38(5):808-16. doi: 10.1124/dmd.109.030833.
107 DrugBank(Pharmacology-Metabolism)Diclofenac sodium
108 Eltrombopag for use in children with immune thrombocytopenia. Blood Adv. 2018 Feb 27;2(4):454-461.
109 Pharmacokinetics, Pharmacodynamics and Clinical Use of SGLT2 Inhibitors in Patients with Type 2 Diabetes Mellitus and Chronic Kidney Disease
110 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.
111 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.
112 Clinical pharmacokinetics and pharmacodynamics of etravirine. Clin Pharmacokinet. 2009;48(9):561-74.
113 Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
114 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.
115 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.
116 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.
117 Fevipiprant has a low risk of influencing co-medication pharmacokinetics: Impact on simvastatin and rosuvastatin in different SLCO1B1 genotypes
118 DrugBank(Pharmacology-Metabolism):Flurbiprofen
119 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.
120 The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos. 2007 Nov;35(11):2040-4.
121 Hydromorphone
122 Opioid pharmacokinetic drug-drug interactions. Am J Manag Care. 2011 Sep;17 Suppl 11:S276-87.
123 Biotransformation of irbesartan in man Drug Metab Dispos. 1998 May;26(5):408-17.
124 Mitiglinide: a rapid- and short-acting non-sulfonylurea insulinotropic agent for the treatment of type 2 diabetic patients
125 Pharmacokinetics, toxicology and safety of lamotrigine in epilepsy Expert Opin Drug Metab Toxicol. 2006 Dec;2(6):1009-18. doi: 10.1517/17425255.2.6.1009.
126 Simultaneous determination of plasma lamotrigine, lamotrigine N2-glucuronide and lamotrigine N2-oxide by UHPLC-MS/MS in epileptic patients. J Pharm Biomed Anal. 2022 Oct 25;220:115017. doi: 10.1016/j.jpba.2022.115017.
127 UDP-glucuronosyltransferase 1A4-mediated N2-glucuronidation is the major metabolic pathway of lamotrigine in chimeric NOG-TKm30 mice with humanised-livers. Xenobiotica. 2021 Oct;51(10):1146-1154. doi: 10.1080/00498254.2021.1972492.
128 Studies on induction of lamotrigine metabolism in transgenic UGT1 mice. Xenobiotica. 2009 Nov;39(11):826-35.
129 #N/A
130 #N/A
131 Clinical pharmacokinetics of losartan. Clin Pharmacokinet. 2005;44(8):797-814.
132 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.
133 Glucuronidation of anti-HIV drug candidate bevirimat: identification of human UDP-glucuronosyltransferases and species differences
134 Isolation of a novel morphinan 3-O-diglucuronide metabolite from dog urine
135 Metabolism of the anthelmintic drug niclosamide by cytochrome P450 enzymes and UDP-glucuronosyltransferases: metabolite elucidation and main contributions from CYP1A2 and UGT1A1 Xenobiotica. 2016;46(1):1-13. doi: 10.3109/00498254.2015.1047812.
136 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
137 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.
138 Retigabine: the newer potential antiepileptic drug
139 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.
140 Absorption, distribution, metabolism, and excretion of radiolabeled naldemedine in healthy subjects
141 Simvastatin Tablet, Film-Coated

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