General Information of Drug (ID: DMIM5AP)

Drug Name
TAK-875 Drug Info
Synonyms
TAK-875; Fasiglifam; 1000413-72-8; TAK875; TAK 875; UNII-GLP1W4JXAH; GLP1W4JXAH; (S)-2-(6-((2',6'-Dimethyl-4'-(3-(methylsulfonyl)propoxy)-[1,1'-biphenyl]-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid; CHEMBL1829174; [(3s)-6-({2',6'-Dimethyl-4'-[3-(Methylsulfonyl)propoxy]biphenyl-3-Yl}methoxy)-2,3-Dihydro-1-Benzofuran-3-Yl]acetic Acid; 3-Benzofuranacetic acid, 6-[[2',6'-diMethyl-4'-[3-(Methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]Methoxy]-2,3-dihydro-, (3S)-; J-501277
Indication
Disease Entry ICD 11 Status REF
Type-2 diabetes 5A11 Phase 3 [1]
Cross-matching ID
PubChem CID
24857286
CAS Number
CAS 1000413-72-8
TTD Drug ID
DMIM5AP
INTEDE Drug ID
DR1882

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Clinical Trial Drug(s)
Preclinical Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fasiglifam hemihydrate DMTGYSO Type-2 diabetes 5A11 Phase 3 [7]
PBI-4050 DMPXK27 Idiopathic pulmonary fibrosis CB03.4 Phase 2 [8]
P-1736 DMEYQPN Diabetic complication 5A2Y Phase 2 [9]
JTT-851 DMED5J6 Type-2 diabetes 5A11 Phase 2 [10]
SHR0534 DMGFTAI Type 2 diabetes 5A11 Phase 1 [11]
LY-2881835 DM5EXJV Type-2 diabetes 5A11 Phase 1 [10]
P11187 DMXZOI0 Type-2 diabetes 5A11 Phase 1 [10]
CPL207-280CA DMFMGZR Type 2 diabetes 5A11 Phase 1 [11]
LY2922470 DMGLTE2 Type 2 diabetes 5A11 Phase 1 [12]
CNX-011-67 DM1H8D6 Type 2 diabetes 5A11 Preclinical [13]
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Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [14]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [17]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [18]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [19]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [20]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [21]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [15]
Verapamil DMA7PEW Angina pectoris BA40 Approved [22]
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Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [23]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [25]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [26]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [27]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [28]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [30]
Verapamil DMA7PEW Angina pectoris BA40 Approved [31]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [26]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [32]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [33]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [22]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [34]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [35]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [36]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [37]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [38]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [39]
Losartan DM72JXH Diabetic kidney disease GB61.Z Approved [22]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [40]
Methotrexate DM2TEOL Anterior urethra cancer Approved [41]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [42]
Calcipotriol DM03CP7 Psoriasis EA90 Approved [43]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [44]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [45]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [46]
Prednisone DM2HG4X Acute asthma CA23 Approved [47]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [48]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [49]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [50]
Quercetin DM3NC4M Obesity 5B81 Approved [51]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [52]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [53]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [54]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [55]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [56]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [57]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [58]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [59]
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Drug(s) Affected By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [60]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [61]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [61]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [62]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [60]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [61]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [63]
Gefitinib DM15F0X Colon adenocarcinoma Approved [60]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [64]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [60]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Clavulanate DM2FGRT Bacteremia 1A73 Approved [65]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [66]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [67]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [68]
Nefazodone DM4ZS8M Major depressive disorder 6A70.3 Approved [55]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [69]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [70]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [58]
Lindane DMB8CNL Infestations of lice and scabies 1G00.Z Approved [71]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [72]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lopinavir DMITQS0 Human immunodeficiency virus infection 1C62 Approved [73]
Sulfinpyrazone DMEV954 Gout FA25 Approved [74]
Probenecid DMMFWOJ Acute gonococcal cervicitis Approved [75]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [76]
Methotrexate DM2TEOL Anterior urethra cancer Approved [50]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [77]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [70]
Epirubicin DMPDW6T Solid tumour/cancer 2A00-2F9Z Approved [78]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [40]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [79]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Warfarin DMJYCVW Atrial fibrillation BC81.3 Approved [80]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [81]
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [82]
Trospium chloride DM32XZT Discovery agent N.A. Approved [83]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [70]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [84]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [85]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [70]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [86]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [87]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Testosterone DM7HUNW Hot flushes GA30 Approved [88]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [88]
Gefitinib DM15F0X Colon adenocarcinoma Approved [89]
Sunitinib DMCBJSR Acute undifferentiated leukemia Approved [90]
Rosuvastatin DMMIQ7G Arteriosclerosis BD40 Approved [91]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [92]
Methotrexate DM2TEOL Anterior urethra cancer Approved [93]
Quercetin DM3NC4M Obesity 5B81 Approved [51]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [94]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [95]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Enalapril DMNFUZR Congestive heart failure BD10 Approved [96]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [97]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [62]
Repaglinide DM5SXUV Diabetic complication 5A2Y Approved [98]
Methotrexate DM2TEOL Anterior urethra cancer Approved [99]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [100]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [101]
Ursodeoxycholic acid DMCUT21 Cholelithiasis DC11 Approved [101]
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [82]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [102]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Free fatty acid receptor 1 (GPR40) TTB8FUC FFAR1_HUMAN Modulator [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [3]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Substrate [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ATP-binding cassette sub-family C member 2 (ABCC2) OTJSIGV5 MRP2_HUMAN Gene/Protein Processing [4]
ATP-binding cassette sub-family C member 3 (ABCC3) OTC3IJV4 MRP3_HUMAN Gene/Protein Processing [5]
ATP-binding cassette sub-family C member 4 (ABCC4) OTO27PAL MRP4_HUMAN Gene/Protein Processing [5]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [5]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2) OTW8V2V1 ABCG2_HUMAN Gene/Protein Processing [6]
Hepatic sodium/bile acid cotransporter (SLC10A1) OTUJVMCL NTCP_HUMAN Gene/Protein Processing [4]
Solute carrier organic anion transporter family member 1B1 (SLCO1B1) OTNEN8QK SO1B1_HUMAN Gene/Protein Processing [6]
Solute carrier organic anion transporter family member 1B3 (SLCO1B3) OTOM3BUH SO1B3_HUMAN Gene/Protein Processing [6]

References

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2 Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial. Diabetes Obes Metab. 2015 Jul;17(7):675-81.
3 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.
4 Fasiglifam (TAK-875) Alters Bile Acid Homeostasis in Rats and Dogs: A Potential Cause of Drug Induced Liver Injury. Toxicol Sci. 2017 May 1;157(1):50-61. doi: 10.1093/toxsci/kfx018.
5 Fasiglifam (TAK-875): Mechanistic Investigation and Retrospective Identification of Hazards for Drug Induced Liver Injury. Toxicol Sci. 2018 Jun 1;163(2):374-384. doi: 10.1093/toxsci/kfx040.
6 Mechanistic investigations of the liver toxicity of the free fatty acid receptor 1 agonist fasiglifam (TAK875) and its primary metabolites. J Biochem Mol Toxicol. 2019 Aug;33(8):e22345. doi: 10.1002/jbt.22345. Epub 2019 May 8.
7 A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1. PLoS One. 2013 Oct 10;8(10):e76280.
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26 Drug Interactions Flockhart Table
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28 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
29 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
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31 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
32 Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
33 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.
34 UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7.
35 Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011 May;21(5):280-8.
36 Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
37 Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
38 Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.
39 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
40 Evaluation of drug transporters' significance for multidrug resistance in head and neck squamous cell carcinoma. Head Neck. 2011 Jul;33(7):959-68. doi: 10.1002/hed.21559. Epub 2010 Aug 24.
41 Gene expression profiling of leukemia T-cells resistant to methotrexate and 7-hydroxymethotrexate reveals alterations that preserve intracellular levels of folate and nucleotide biosynthesis. Biochem Pharmacol. 2009 Apr 15;77(8):1410-7.
42 Drug sensitivity and drug resistance profiles of human intrahepatic cholangiocarcinoma cell lines. World J Gastroenterol. 2005 May 14;11(18):2748-53. doi: 10.3748/wjg.v11.i18.2748.
43 Adaptive homeostasis of the vitamin D-vitamin D nuclear receptor axis in 8-methoxypsoralen-induced hepatotoxicity. Toxicol Appl Pharmacol. 2019 Jan 1;362:150-158. doi: 10.1016/j.taap.2018.11.002. Epub 2018 Nov 10.
44 Cannabidiol induces antioxidant pathways in keratinocytes by targeting BACH1. Redox Biol. 2020 Jan;28:101321. doi: 10.1016/j.redox.2019.101321. Epub 2019 Sep 5.
45 Estrogen regulation in human breast cancer cells of new downstream gene targets involved in estrogen metabolism, cell proliferation and cell transformation. J Mol Endocrinol. 2004 Apr;32(2):397-414.
46 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
47 Differential regulation of the human MRP2 and MRP3 gene expression by glucocorticoids. J Steroid Biochem Mol Biol. 2005 Aug;96(3-4):229-34. doi: 10.1016/j.jsbmb.2005.03.004.
48 Induction of multidrug resistance proteins MRP1 and MRP3 and gamma-glutamylcysteine synthetase gene expression by nonsteroidal anti-inflammatory drugs in human colon cancer cells. Biochem Biophys Res Commun. 2002 Feb 8;290(5):1427-33. doi: 10.1006/bbrc.2002.6367.
49 Activation of nuclear factor-kappa B pathway by simvastatin and RhoA silencing increases doxorubicin cytotoxicity in human colon cancer HT29 cells. Mol Pharmacol. 2008 Aug;74(2):476-84.
50 Methotrexate normalizes up-regulated folate pathway genes in rheumatoid arthritis. Arthritis Rheum. 2013 Nov;65(11):2791-802.
51 Activation of beta-catenin signalling by GSK-3 inhibition increases p-glycoprotein expression in brain endothelial cells. J Neurochem. 2008 Aug;106(4):1855-65. doi: 10.1111/j.1471-4159.2008.05537.x. Epub 2008 Jul 4.
52 ATP binding cassette multidrug transporters limit the anti-HIV activity of zidovudine and indinavir in infected human macrophages. Antivir Ther. 2004 Aug;9(4):519-28.
53 Selenium-dependent and -independent transport of arsenic by the human multidrug resistance protein 2 (MRP2/ABCC2): implications for the mutual detoxification of arsenic and selenium. Carcinogenesis. 2010 Aug;31(8):1450-5. doi: 10.1093/carcin/bgq125. Epub 2010 Jun 27.
54 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
55 Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
56 Hematopoietic stem cell differentiation affects expression and function of MRP4 (ABCC4), a transport protein for signaling molecules and drugs. Int J Cancer. 2009 May 15;124(10):2303-11. doi: 10.1002/ijc.24207.
57 Prolonged use of aspirin alters human and rat intestinal cells and thereby limits the absorption of clopidogrel. Clin Pharmacol Ther. 2011 Oct;90(4):612-9. doi: 10.1038/clpt.2011.163. Epub 2011 Sep 7.
58 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
59 Stem cell transcriptome responses and corresponding biomarkers that indicate the transition from adaptive responses to cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.
60 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
61 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
62 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
63 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
64 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
65 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
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68 Dysregulation of retinoic acid receptor diminishes hepatocyte permissiveness to hepatitis B virus infection through modulation of sodium taurocholate cotransporting polypeptide (NTCP) expression. J Biol Chem. 2015 Feb 27;290(9):5673-84. doi: 10.1074/jbc.M114.602540. Epub 2014 Dec 30.
69 Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes. Drug Metab Dispos. 2006 Oct;34(10):1756-63. doi: 10.1124/dmd.106.010033. Epub 2006 Jul 12.
70 Potency of individual bile acids to regulate bile acid synthesis and transport genes in primary human hepatocyte cultures. Toxicol Sci. 2014 Oct;141(2):538-46. doi: 10.1093/toxsci/kfu151. Epub 2014 Jul 23.
71 Regulation of hepatic drug transporter activity and expression by organochlorine pesticides. J Biochem Mol Toxicol. 2014 Mar;28(3):119-28.
72 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
73 Functional defect caused by the 4544G>A SNP in ABCC2: potential impact for drug cellular disposition. Pharmacogenet Genomics. 2011 Dec;21(12):884-93. doi: 10.1097/FPC.0b013e32834d672b.
74 Role of multidrug resistance protein 2 (MRP2, ABCC2) in alkylating agent detoxification: MRP2 potentiates glutathione S-transferase A1-1-mediated resistance to chlorambucil cytotoxicity. J Pharmacol Exp Ther. 2004 Jan;308(1):260-7. doi: 10.1124/jpet.103.057729. Epub 2003 Oct 20.
75 MRP2 (ABCC2) transports taxanes and confers paclitaxel resistance and both processes are stimulated by probenecid. Int J Cancer. 2005 Sep 20;116(5):824-9. doi: 10.1002/ijc.21013.
76 Association of genetic polymorphisms in SLCO1B3 and ABCC2 with docetaxel-induced leukopenia. Cancer Sci. 2008 May;99(5):967-72.
77 In vitro study of transporters involved in intestinal absorption of inorganic arsenic. Chem Res Toxicol. 2012 Feb 20;25(2):446-53. doi: 10.1021/tx200491f. Epub 2012 Jan 26.
78 Co-encapsulation of chrysophsin-1 and epirubicin in PEGylated liposomes circumvents multidrug resistance in HeLa cells. Chem Biol Interact. 2015 Dec 5;242:13-23. doi: 10.1016/j.cbi.2015.08.023. Epub 2015 Sep 1.
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80 Identification of two novel genes SLC15A2 and SLCO1B3 associated with maintenance dose variability of warfarin in a Chinese population. Sci Rep. 2017 Dec 12;7(1):17379. doi: 10.1038/s41598-017-17731-1.
81 Involvement of multiple efflux transporters in hepatic disposition of fexofenadine. Mol Pharmacol. 2008 May;73(5):1474-83.
82 Transcellular movement of hydroxyurea is mediated by specific solute carrier transporters. Exp Hematol. 2011 Apr;39(4):446-56.
83 Expression of drug transporters and drug metabolizing enzymes in the bladder urothelium in man and affinity of the bladder spasmolytic trospium chloride to transporters likely involved in its pharmacokinetics. Mol Pharm. 2015 Jan 5;12(1):171-8.
84 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
85 Rifampin Regulation of Drug Transporters Gene Expression and the Association of MicroRNAs in Human Hepatocytes. Front Pharmacol. 2016 Apr 26;7:111.
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87 Primary Human Hepatocyte Spheroids as Tools to Study the Hepatotoxic Potential of Non-Pharmaceutical Chemicals. Int J Mol Sci. 2021 Oct 12;22(20):11005. doi: 10.3390/ijms222011005.
88 Localization of breast cancer resistance protein (Bcrp) in endocrine organs and inhibition of its transport activity by steroid hormones. Cell Tissue Res. 2012 Aug;349(2):551-63. doi: 10.1007/s00441-012-1417-5. Epub 2012 May 13.
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90 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
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92 Ciprofloxacin mediates cancer stem cell phenotypes in lung cancer cells through caveolin-1-dependent mechanism. Chem Biol Interact. 2016 Apr 25;250:1-11.
93 Proteomic identification of differentially expressed proteins associated with the multiple drug resistance in methotrexate-resistant human breast cancer cells. Int J Oncol. 2014 Jul;45(1):448-58.
94 Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.
95 Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps. Cancer Biol Ther. 2005 Jul;4(7):747-52.
96 Effect of organic anion-transporting polypeptide 1B1 (OATP1B1) polymorphism on the single- and multiple-dose pharmacokinetics of enalapril in healthy Chinese adult men. Clin Ther. 2011 May;33(5):655-63. doi: 10.1016/j.clinthera.2011.04.018.
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98 Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics. Clin Pharmacol Ther. 2005 Jun;77(6):468-78. doi: 10.1016/j.clpt.2005.01.018.
99 SLC19A1, SLC46A1 and SLCO1B1 polymorphisms as predictors of methotrexate-related toxicity in Portuguese rheumatoid arthritis patients. Toxicol Sci. 2014 Nov;142(1):196-209. doi: 10.1093/toxsci/kfu162. Epub 2014 Aug 14.
100 SLCO1B1 variants and statin-induced myopathy--a genomewide study. N Engl J Med. 2008 Aug 21;359(8):789-99.
101 Transport of fluorescent chenodeoxycholic acid via the human organic anion transporters OATP1B1 and OATP1B3. J Lipid Res. 2006 Jun;47(6):1196-202.
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