General Information of Drug (ID: DM5SXUV)

Drug Name
Repaglinide Drug Info
Synonyms
Actulin; GlucoNorm; NovoNorm; Prandin; Repaglinida; Repaglinidum; Glaxo Wellcome brand of replaginide; Novo Nordisk brand of repaglinide; Repaglinide [USAN]; Novo Nordisk brand 2 of repaglinide; AG-EE 388; AG-EE 388 ZW; AG-EE 623 ZW; AGEE-623ZW; GlucoNorm (TN); NN-623; NovoNorm (TN); Prandin (TN); Repa-glinide; Repaglinida [INN-Spanish]; Repaglinidum [INN-Latin]; SMP-508; AG-EE-388; AG-EE-623 ZW; Prandin, GlucoNorm, NovoNorm, Repaglinide; Repaglinide (JAN/USP/INN); Repaglinide, (+-)-isomer; (+)-2-Ethoxy-alpha-(((S)-alpha-isobutyl-o-piperidinobenzyl)carbamoyl)-p-toluic acid; (S)-(+)-2-Ethoxy-4-[N-[1-(2-piperidinophenyl)-3-methyl-1-butyl]aminocarbonylmethyl]benzoic acid; (S)-2-Ethoxy-4-(2-((methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)-benzoic acid; (S)-2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)-phenyl)butyl)amino)-2-oxoethyl)-benzoic acid; 111GE012; 2-ethoxy-4-(2-((3-methyl-1-(2-(1-piperidinyl)phenyl)butyl)amino)-2-oxoethyl)benzoic acid; 2-ethoxy-4-(2-{[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino}-2-oxoethyl)benzoic acid; 2-ethoxy-4-[2-({(1S)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl}amino)-2-oxoethyl]benzoic acid; 2-ethoxy-4-[2-[[(1S)-3-methyl-1-(2-piperidin-1-ylphenyl)butyl]amino]-2-oxoethyl]benzoic acid; 2-ethoxy-N-(alpha-(2-methyl-1-propyl)-2-piperidinobenzyl)-4-carbamoylmethylbenzoic acid
Indication
Disease Entry ICD 11 Status REF
Diabetic complication 5A2Y Approved [1]
Therapeutic Class
Hypoglycemic Agents
Cross-matching ID
PubChem CID
65981
ChEBI ID
CHEBI:8805
CAS Number
CAS 135062-02-1
TTD Drug ID
DM5SXUV
VARIDT Drug ID
DR00446
INTEDE Drug ID
DR1404
ACDINA Drug ID
D00587

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Discontinued Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tolbutamide DM02AWV Advanced cancer 2A00-2F9Z Approved [11]
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [12]
Nicorandil DMIYJFV Angina pectoris BA40 Approved [13]
BTS-67582 DM54K2P Diabetic complication 5A2Y Discontinued in Phase 2 [14]
KRN-2391 DMZ1SEW Angina pectoris BA40 Discontinued in Phase 2 [15]
CCX915 DMHMST3 Multiple sclerosis 8A40 Discontinued in Phase 1 [16]
BMS-191095 DMKFXTD Angina pectoris BA40 Discontinued in Phase 1 [17]
⏷ Show the Full List of 7 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glibenclamide DM8JXPZ Diabetic complication 5A2Y Approved [18]
Tolbutamide DM02AWV Advanced cancer 2A00-2F9Z Approved [11]
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [12]
Acetohexamide DMR6N7H Diabetic complication 5A2Y Approved [19]
Gliclazide DMN6QO5 Diabetic complication 5A2Y Approved [20]
NN-414 DMRJEXM Type-1 diabetes 5A10 Phase 1 [21]
HBR-985 DMKDBFL Discovery agent N.A. Investigative [22]
NS-11757 DM98VMZ Atrial fibrillation BC81.3 Investigative [23]
⏷ Show the Full List of 8 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [24]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [27]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [26]
Pravastatin DM6A0X7 Adult acute monocytic leukemia Approved [28]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [29]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [30]
Cerivastatin DMXCM7H Hyperlipidaemia 5C80 Approved [31]
PITAVASTATIN CALCIUM DM1UJO0 Dyslipidemia 5C80-5C81 Approved [28]
⏷ Show the Full List of 10 Drug(s)
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 [32]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [33]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [34]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [35]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [36]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [37]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [38]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [39]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [33]
Verapamil DMA7PEW Angina pectoris BA40 Approved [40]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [41]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [42]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [43]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [44]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [45]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [46]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [47]
Metronidazole DMTIVEN Abscess Approved [48]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [49]
Ethanol DMDRQZU Chronic pain MG30 Approved [50]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2C8 (CYP2C8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [51]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [52]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [52]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [53]
Verapamil DMA7PEW Angina pectoris BA40 Approved [54]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [55]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [56]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [52]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [57]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [58]
⏷ 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 [59]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [60]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [61]
Methotrexate DM2TEOL Anterior urethra cancer Approved [62]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [63]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [64]
Ursodeoxycholic acid DMCUT21 Cholelithiasis DC11 Approved [64]
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [65]
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [66]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [67]
⏷ Show the Full List of 10 Drug(s)
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 [68]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [69]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [69]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [61]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [68]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [69]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [70]
Gefitinib DM15F0X Colon adenocarcinoma Approved [68]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [6]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [68]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-8 (CXCL8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [71]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [72]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [73]
Pantothenic acid DM091H2 Vitamin deficiency 5B55-5B71 Approved [74]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [75]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [76]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [77]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [78]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [79]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [77]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gefitinib DM15F0X Colon adenocarcinoma Approved [7]
Selenium DM25CGV N. A. N. A. Approved [80]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [7]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [81]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [82]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [83]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [84]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [85]
Saquinavir DMG814N Human immunodeficiency virus infection 1C62 Approved [7]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [86]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [83]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [87]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [88]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [89]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [90]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [91]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [92]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [86]
Benzoic Acid DMKB9FI Alopecia areata ED70.2 Approved [90]
Azathioprine DMMZSXQ Lupus nephritis 4A40.0Y Approved [93]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gefitinib DM15F0X Colon adenocarcinoma Approved [7]
Quercetin DM3NC4M Obesity 5B81 Approved [94]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [7]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [95]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [7]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [96]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [7]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [7]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [97]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [91]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
ATP-binding cassette transporter C8 (ABCC8) TTP835K ABCC8_HUMAN Blocker [2]
ATP-binding cassette transporter C9 (ABCC9) TTEF5MJ ABCC9_HUMAN Blocker [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [4]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [5]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [6]
HLA class I histocompatibility antigen, alpha chain F (HLA-F) OT76CM19 HLAF_HUMAN Gene/Protein Processing [7]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Gene/Protein Processing [8]
Major histocompatibility complex class I-related gene protein (MR1) OTZU3XX7 HMR1_HUMAN Gene/Protein Processing [7]
Solute carrier family 15 member 1 (SLC15A1) OT1P16B5 S15A1_HUMAN Gene/Protein Processing [9]
Solute carrier organic anion transporter family member 1B1 (SLCO1B1) OTNEN8QK SO1B1_HUMAN Regulation of Drug Effects [10]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6841).
2 Metformin/Repaglinide (PrandiMet) for type 2 diabetes. Med Lett Drugs Ther. 2009 Jun 1;51(1313):41-3.
3 Disease-Associated Changes in Drug Transporters May Impact the Pharmacokinetics and/or Toxicity of Drugs: A White Paper From the International Transporter Consortium. Clin Pharmacol Ther. 2018 Nov;104(5):900-915.
4 Drug-drug and food-drug pharmacokinetic interactions with new insulinotropic agents repaglinide and nateglinide. Clin Pharmacokinet. 2007;46(2):93-108.
5 Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism. Br J Clin Pharmacol. 2010 Dec;70(6):870-80.
6 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
7 Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. Chem Res Toxicol. 2015 May 18;28(5):927-34. doi: 10.1021/tx5005248. Epub 2015 Apr 3.
8 Toxicological evaluation of acyl glucuronides utilizing half-lives, peptide adducts, and immunostimulation assays. Toxicol In Vitro. 2015 Dec 25;30(1 Pt B):241-9.
9 In vitro and pharmacophore-based discovery of novel hPEPT1 inhibitors. Pharm Res. 2005 Apr;22(4):512-7. doi: 10.1007/s11095-005-2505-y. Epub 2005 Apr 7.
10 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.
11 Expression of an activating mutation in the gene encoding the KATP channel subunit Kir6.2 in mouse pancreatic beta cells recapitulates neonatal diabetes. J Clin Invest. 2009 Jan;119(1):80-90.
12 Mechanism of disopyramide-induced hypoglycaemia in a patient with Type 2 diabetes. Diabet Med. 2009 Jan;26(1):76-8.
13 A functional role of the C-terminal 42 amino acids of SUR2A and SUR2B in the physiology and pharmacology of cardiovascular ATP-sensitive K(+) chann... J Mol Cell Cardiol. 2005 Jul;39(1):1-6.
14 BTS-67582 (Knoll Pharmaceuticals Co). IDrugs. 1999 Apr;2(4):355-9.
15 Effects of KRN2391 on ionic currents in rabbit femoral arterial myocytes
16 Analysis of the differential modulation of sulphonylurea block of beta-cell and cardiac ATP-sensitive K+ (K(ATP)) channels by Mg-nucleotides. J Physiol. 2003 Feb 15;547(Pt 1):159-68.
17 The mitochondrial K(ATP) channel opener BMS-191095 reduces neuronal damage after transient focal cerebral ischemia in rats.J Cereb Blood Flow Metab.2007 Feb;27(2):348-55.
18 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
19 Diabetes and insulin secretion: the ATP-sensitive K+ channel (K ATP) connection.Diabetes.2005 Nov;54(11):3065-72.
20 Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes. 2001 Oct;50(10):2253-9.
21 Attenuation of hyperinsulinemia by NN414, a SUR1/Kir6.2 selective K-adenosine triphosphate channel opener, improves glucose tolerance and lipid profile in obese Zucker rats.Metabolism.2004 Apr;53(4):441-7.
22 Cardioselective K(ATP) channel blockers derived from a new series of m-anisamidoethylbenzenesulfonylthioureas. J Med Chem. 2001 Mar 29;44(7):1085-98.
23 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2944).
24 Preclinical Mouse Models To Study Human OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions in Vivo. Mol Pharm. 2015 Dec 7;12(12):4259-69.
25 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
26 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
27 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
28 The effect of SLCO1B1*15 on the disposition of pravastatin and pitavastatin is substrate dependent: the contribution of transporting activity changes by SLCO1B1*15. Pharmacogenet Genomics. 2008 May;18(5):424-33.
29 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
30 Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009 Jul;405(1-2):49-52.
31 FDA Drug Development and Drug Interactions
32 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
33 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
34 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
35 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
36 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
37 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
38 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
39 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
40 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.
41 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
42 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
43 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
44 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.
45 Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
46 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.
47 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
48 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.
49 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.
50 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
51 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
52 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
53 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
54 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
55 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
56 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
57 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
58 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
59 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.
60 Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug Metab Dispos. 2005 Apr;33(4):537-46.
61 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
62 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.
63 SLCO1B1 variants and statin-induced myopathy--a genomewide study. N Engl J Med. 2008 Aug 21;359(8):789-99.
64 Transport of fluorescent chenodeoxycholic acid via the human organic anion transporters OATP1B1 and OATP1B3. J Lipid Res. 2006 Jun;47(6):1196-202.
65 Transcellular movement of hydroxyurea is mediated by specific solute carrier transporters. Exp Hematol. 2011 Apr;39(4):446-56.
66 Severe toxicities after irinotecan-based chemotherapy in a patient with lung cancer: a homozygote for the SLCO1B1*15 allele. Ther Drug Monit. 2007 Oct;29(5):666-8. doi: 10.1097/FTD.0b013e3181357364.
67 Germline genetic variation in an organic anion transporter polypeptide associated with methotrexate pharmacokinetics and clinical effects. J Clin Oncol. 2009 Dec 10;27(35):5972-8.
68 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.
69 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
70 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.
71 Monomeric and oligomeric flavanols maintain the endogenous glucocorticoid response in human macrophages in pro-oxidant conditions in vitro. Chem Biol Interact. 2018 Aug 1;291:237-244.
72 Nicotine up-regulates IL-8 expression in human gingival epithelial cells following stimulation with IL-1 or P. gingivalis lipopolysaccharide via nicotinic acetylcholine receptor signalling. Arch Oral Biol. 2012 May;57(5):483-90. doi: 10.1016/j.archoralbio.2011.10.007. Epub 2011 Nov 25.
73 Ca(2+) Signaling and IL-8 Secretion in Human Testicular Peritubular Cells Involve the Cation Channel TRPV2. Int J Mol Sci. 2018 Sep 19;19(9):2829. doi: 10.3390/ijms19092829.
74 Calcium pantothenate modulates gene expression in proliferating human dermal fibroblasts. Exp Dermatol. 2009 Nov;18(11):969-78. doi: 10.1111/j.1600-0625.2009.00884.x. Epub 2009 Apr 8.
75 Nitrogen mustard prevents transport of Fra-1 into the nucleus to promote c-Fos- and FosB-dependent IL-8 induction in injured mouse epidermis. Toxicol Lett. 2020 Feb 1;319:256-263. doi: 10.1016/j.toxlet.2019.10.006. Epub 2019 Oct 19.
76 ERE-independent ERalpha target genes differentially expressed in human breast tumors. Mol Cell Endocrinol. 2005 Dec 21;245(1-2):53-9. doi: 10.1016/j.mce.2005.10.003. Epub 2005 Nov 17.
77 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
78 Gypenosides protect retinal pigment epithelium cells from oxidative stress. Food Chem Toxicol. 2018 Feb;112:76-85.
79 Nitric oxide synthase inhibitors attenuate ozone-induced airway inflammation in guinea pigs. Possible role of interleukin-8. Am J Respir Crit Care Med. 2000 Jan;161(1):249-56. doi: 10.1164/ajrccm.161.1.9804096.
80 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
81 Retinoic acid-induced downmodulation of telomerase activity in human cancer cells. Exp Mol Pathol. 2005 Oct;79(2):108-17.
82 Effect of nephrotoxicants and hepatotoxicants on gene expression profile in human peripheral blood mononuclear cells. Biochem Biophys Res Commun. 2010 Oct 15;401(2):245-50. doi: 10.1016/j.bbrc.2010.09.039. Epub 2010 Sep 16.
83 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
84 Changes in gene expression profiles of multiple myeloma cells induced by arsenic trioxide (ATO): possible mechanisms to explain ATO resistance in vivo. Br J Haematol. 2005 Mar;128(5):636-44.
85 The neuroprotective action of the mood stabilizing drugs lithium chloride and sodium valproate is mediated through the up-regulation of the homeodomain protein Six1. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):124-34.
86 Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
87 Rifampin Regulation of Drug Transporters Gene Expression and the Association of MicroRNAs in Human Hepatocytes. Front Pharmacol. 2016 Apr 26;7:111.
88 Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
89 Enhancement effect of resveratrol on the intestinal absorption of bestatin by regulating PEPT1, MDR1 and MRP2 in vivo and in vitro. Int J Pharm. 2015 Nov 10;495(1):588-598. doi: 10.1016/j.ijpharm.2015.09.042. Epub 2015 Sep 21.
90 Affinity and translocation relationships via hPEPT1 of H-X aa-Ser-OH dipeptides: evaluation of H-Phe-Ser-OH as a pro-moiety for ibuprofen and benzoic acid prodrugs. Eur J Pharm Biopharm. 2011 Feb;77(2):327-31. doi: 10.1016/j.ejpb.2010.12.009. Epub 2010 Dec 13.
91 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.
92 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
93 Severe villus atrophy and chronic malabsorption induced by azathioprine. Gastroenterology. 2003 Jun;124(7):1950-7.
94 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
95 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
96 Genomic profiling uncovers a molecular pattern for toxicological characterization of mutagens and promutagens in vitro. Toxicol Sci. 2011 Jul;122(1):185-97.
97 Chronic occupational exposure to arsenic induces carcinogenic gene signaling networks and neoplastic transformation in human lung epithelial cells. Toxicol Appl Pharmacol. 2012 Jun 1;261(2):204-16.