General Information of Drug (ID: DMCR1MV)

Drug Name
Itraconazole Drug Info
Synonyms
Canadiol; Hyphanox; ITCZ; ITZ; Intraconazole; Itraconazol; Itraconazolum; Itrizole; Oriconazole; Orungal; Prokanazol; Sempera; Spherazole; Sporal; Sporanos; Sporanox; Sporonox; Triasporn; Itraconazol [Spanish]; Itraconazole oral solution; Itraconazolum [Latin]; R 51211; Cis-Itraconazole; Itraconazole & Bovine Lactoferrin; Itraconazole & Nyotran; Itrizole (TN); R-51211; Sporanox (TN); Itraconazole & Nyotran(Liposomal Nystatin); Itraconazole (JAN/USAN); Oriconazole, R51211, Sporanox; Itraconazole [USAN:BAN:INN:JAN]; (+-)-1-sec-Butyl-4-(p-(4-(p-(((2R*,4S*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)-1-piperazinyl)phenyl)-delta(sup 2)-1,2,4-triazolin-5-one; (1)-cis-4-(4-(4-(4-((2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2,4-dihydro-2-sec-butyl-3H-1,2,4-triazol-3-one; 2-(butan-2-yl)-4-{4-[4-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-2,4-dihydro-3H-1,2,4-triazol-3-one; 2-butan-2-yl-4-[4-[4-[4-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one; 2-butan-2-yl-4-[4-[4-[4-[[(2S,4R)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one; 2-butan-2-yl-4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one; 3H-1,2,4-Triazol-3-one, 4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-pipera-zinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl); 4-(4-{4-[4-({[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl}oxy)phenyl]piperazin-1-yl}phenyl)-2-(1-methylpropyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
Indication
Disease Entry ICD 11 Status REF
Aspergillosis 1F20 Approved [1]
Blastomycosis 1F22 Approved [1]
Fungal infection 1F29-1F2F Approved [2]
Fusariosis Approved [1]
Histoplasmosis Approved [1]
Invasive candidiasis 1F23 Approved [1]
Mycoses 1F2Z Approved [1]
Candidemia 1F23.3Y Investigative [1]
Esophageal candidiasis Investigative [1]
Therapeutic Class
Antifungal Agents
Cross-matching ID
PubChem CID
55283
ChEBI ID
CHEMBL6076
CAS Number
CAS 84625-61-6
TTD Drug ID
DMCR1MV
VARIDT Drug ID
DR00687
INTEDE Drug ID
DR0895
ACDINA Drug ID
D00337

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
PF-04449913 DMSB068 Chronic myelomonocytic leukaemia 2A40 Approved [12]
Patidegib DM2NJYC Basal cell carcinoma 2C32 Phase 2 [13]
ENV-101 DMFOI3T Idiopathic pulmonary fibrosis CB03.4 Phase 2 [14]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [3]
Posaconazole DMUL5EW Aspergillosis 1F20 Approved [15]
Ketoconazole DMPZI3Q Blastomycosis 1F22 Approved [16]
Miconazole DMPMYE8 Cutaneous candidiasis 1F23.14 Approved [3]
Oxiconazole DME7KRM Tinea corporis 1F28.Y Approved [17]
Fluconazole DMOWZ6B Cryptococcal meningitis Approved [3]
Terconazole DMJ13KI Candidiasis 1F23 Approved [18]
Bifonazole DM3KN7V Fungal infection 1F29-1F2F Approved [19]
Tioconazole DMNYPGS Onychomycosis EE12.1 Approved [20]
Econazole DMFSWGH Cutaneous candidiasis 1F23.14 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [22]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [23]
Methotrexate DM2TEOL Anterior urethra cancer Approved [5]
Folic Acid DMEMBJC Colorectal carcinoma Approved [24]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [5]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [5]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [25]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [5]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [26]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [27]
⏷ 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 [28]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [29]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [30]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [31]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [32]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [33]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [34]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [35]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [29]
Verapamil DMA7PEW Angina pectoris BA40 Approved [36]
⏷ 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 [37]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [38]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [39]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [40]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [41]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [42]
Mycophenolate mofetil DMPQAGE Hepatosplenic T-cell lymphoma Approved [43]
Metronidazole DMTIVEN Abscess Approved [44]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [45]
Ethanol DMDRQZU Chronic pain MG30 Approved [46]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [47]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [48]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [49]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [50]
Cepharanthine DM9Y5JB N. A. N. A. Approved [51]
Clozapine DMFC71L Schizophrenia 6A20 Approved [52]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [53]
Trifluoperazine DMKBYWI Anxiety Approved [54]
Olanzapine DMPFN6Y Bipolar depression Approved [52]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [50]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [55]
Calcidiol DMN4CV5 Hypophosphatemia Approved [56]
Calcipotriol DM03CP7 Psoriasis EA90 Approved [57]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [58]
Quercetin DM3NC4M Obesity 5B81 Approved [59]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [60]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [61]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [62]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [63]
Testosterone DM7HUNW Hot flushes GA30 Approved [64]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [65]
Vidarabine DM0N85H Hepatosplenic T-cell lymphoma Approved [65]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [66]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [67]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [68]
Etidronic acid DM1XHYJ Bone Paget disease Approved [65]
Tiaprofenic acid DM23D7J Osteoarthritis FA00-FA05 Approved [65]
Bromperidol DM24XYQ Schizophrenia 6A20 Approved [65]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [69]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [70]
⏷ 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 [10]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [71]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [71]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [72]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [10]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [71]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [73]
Gefitinib DM15F0X Colon adenocarcinoma Approved [10]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [74]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [10]
⏷ 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
Candida Cytochrome P450 51 (Candi ERG11) TTTSOUD CP51_CANAL Modulator [3]
Hedgehog signaling pathway (HS pathway) TT4LXBC NOUNIPROTAC Inhibitor [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [6]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Substrate [7]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial (CYP24A1) OTG2T749 CP24A_HUMAN Gene/Protein Processing [8]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [9]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [10]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Gene/Protein Processing [11]

References

1 Itraconazole FDA Label
2 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076104.
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
6 Effects of itraconazole and tandospirone on the pharmacokinetics of perospirone. Ther Drug Monit. 2006 Feb;28(1):73-5.
7 Investigation into UDP-glucuronosyltransferase (UGT) enzyme kinetics of imidazole- and triazole-containing antifungal drugs in human liver microsomes and recombinant UGT enzymes. Drug Metab Dispos. 2010 Jun;38(6):923-9.
8 The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
9 Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
10 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.
11 Azole antimycotics differentially affect rifampicin-induced pregnane X receptor-mediated CYP3A4 gene expression. Drug Metab Dispos. 2008 Feb;36(2):339-48.
12 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
13 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
14 Development of taladegib as a sonic hedgehog signaling pathway inhibitor. Arch Pharm Res. 2017 Dec;40(12):1390-1393.
15 A new, broad-spectrum azole antifungal: posaconazole--mechanisms of action and resistance, spectrum of activity. Mycoses. 2006;49 Suppl 1:2-6.
16 Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302.
17 Antifungal agents: mechanisms of action. Trends Microbiol. 2003 Jun;11(6):272-9.
18 Mode of action of anti-Candida drugs: focus on terconazole and other ergosterol biosynthesis inhibitors. Am J Obstet Gynecol. 1991 Oct;165(4 Pt 2):1193-9.
19 Investigation of the role of cytochrome P450 2B4 active site residues in substrate metabolism based on crystal structures of the ligand-bound enzyme. Arch Biochem Biophys. 2006 Nov 1;455(1):61-7.
20 Biological spectra analysis: Linking biological activity profiles to molecular structure. Proc Natl Acad Sci U S A. 2005 Jan 11;102(2):261-6.
21 Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homolo... Antimicrob Agents Chemother. 2008 Oct;52(10):3597-603.
22 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
23 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
24 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
25 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
26 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
27 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
28 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.
29 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
30 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.
31 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
32 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.
33 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.
34 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
35 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.
36 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.
37 Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
38 Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
39 Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
40 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.
41 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.
42 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.
43 Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
44 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.
45 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.
46 Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
47 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
48 Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
49 Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
50 Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
51 Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
52 Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
53 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
54 Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.
55 DNA microarray analysis of vitamin D-induced gene expression in a human colon carcinoma cell line. Physiol Genomics. 2004 Apr 13;17(2):122-9. doi: 10.1152/physiolgenomics.00002.2003.
56 Retinoic acid via RARalpha inhibits the expression of 24-hydroxylase in human prostate stromal cells. Biochem Biophys Res Commun. 2005 Dec 30;338(4):1973-81. doi: 10.1016/j.bbrc.2005.10.178. Epub 2005 Nov 7.
57 Actions of Vitamin D3, analogs on human prostate cancer cell lines: comparison with 1,25-dihydroxyvitamin D3. Endocrinology. 1995 Jan;136(1):20-6.
58 Time series analysis of oxidative stress response patterns in HepG2: a toxicogenomics approach. Toxicology. 2013 Apr 5;306:24-34.
59 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.
60 Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61.
61 Possible involvement of pregnane X receptor-enhanced CYP24 expression in drug-induced osteomalacia. J Clin Invest. 2005 Jan;115(1):177-86.
62 19-Nor-1,25(OH)2D2 (a novel, noncalcemic vitamin D analogue), combined with arsenic trioxide, has potent antitumor activity against myeloid leukemia. Cancer Res. 2005 Mar 15;65(6):2488-97.
63 Similarities and differences between two modes of antagonism of the thyroid hormone receptor. ACS Chem Biol. 2011 Oct 21;6(10):1096-106.
64 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
65 Screening of a chemical library reveals novel PXR-activating pharmacologic compounds. Toxicol Lett. 2015 Jan 5;232(1):193-202. doi: 10.1016/j.toxlet.2014.10.009. Epub 2014 Oct 16.
66 Induction of PXR-mediated metabolism by beta-carotene. Biochim Biophys Acta. 2005 May 30;1740(2):162-9. doi: 10.1016/j.bbadis.2004.11.013. Epub 2004 Dec 8.
67 Lignans, bacteriocides and organochlorine compounds activate the human pregnane X receptor (PXR). Toxicol Appl Pharmacol. 2005 Dec 1;209(2):123-33. doi: 10.1016/j.taap.2005.03.015.
68 Identification and validation of novel human pregnane X receptor activators among prescribed drugs via ligand-based virtual screening. Drug Metab Dispos. 2011 Feb;39(2):337-44. doi: 10.1124/dmd.110.035808. Epub 2010 Nov 10.
69 Identification of HMG-CoA reductase inhibitors as activators for human, mouse and rat constitutive androstane receptor. Drug Metab Dispos. 2005 Jul;33(7):924-9.
70 Acetylated deoxycholic (DCA) and cholic (CA) acids are potent ligands of pregnane X (PXR) receptor. Toxicol Lett. 2017 Jan 4;265:86-96.
71 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
72 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
73 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.
74 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.