Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM6ETS0)

Drug Name

Deferasirox Drug Info

Synonyms

Deferasirox; Deferasirox (Exjade); Deferasiroxum; Deferasiroxum [INN-Latin]; Exjade; V8G4MOF2V9; 201530-41-8; 4-(3,5-Bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl)benzoic acid; 4-[3,5-Bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl]benzoic acid; 4-[3,5-bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid; Benzoic acid, 4-[3,5-bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]-; C21H15N3O4; CGP-72670; CHEBI:49005; DSSTox_CID_28522; DSSTox_RID_82794; ICL 670; ICL 670A; ICL-670; ICL-670A; ICL670; ICL670A; NCGC00181754-01; UNII-V8G4MOF2V9

Indication

Disease Entry	ICD 11	Status	REF
Beta thalassemia	3A50.2	Approved	[1]
Iron overload disease	5C64.10	Approved	[1]
Iron metabolism disease		Investigative	[1]

Cross-matching ID

PubChem CID: 214348
ChEBI ID: CHEBI:49005
CAS Number: C1CCC(C(C1)CN2CCN(CC2)C3=NSC4=CC=CC=C43)CN5C(=O)C6C7CCC(C7)C6C5=O
TTD Drug ID: DM6ETS0
INTEDE Drug ID: DR0429

Molecule-Related Drug Atlas

Molecule Type:

DME

DOT

Drug Status:

Approved Drug(s)

Download the Complete Related Drug List

Drug(s) Metabolized By UDP-glucuronosyltransferase 1A1 (UGT1A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[4]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[5]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[6]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[7]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[8]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[9]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[10]
Metronidazole	DMTIVEN	Abscess		Approved	[11]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[12]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[13]
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Drug(s) Metabolized By UDP-glucuronosyltransferase 1A3 (UGT1A3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[14]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[9]
Ibuprofen	DM8VCBE	Dysmenorrhea	GA34.3	Approved	[15]
Atorvastatin	DMF28YC	Acute coronary syndrome	BA41	Approved	[16]
Cerivastatin	DMXCM7H	Hyperlipidaemia	5C80	Approved	[17]
PITAVASTATIN CALCIUM	DM1UJO0	Dyslipidemia	5C80-5C81	Approved	[18]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[19]
Ezetimibe	DM7A8TW	Atherosclerosis	BD40	Approved	[20]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[21]
Losartan	DM72JXH	Diabetic kidney disease	GB61.Z	Approved	[15]
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Drug(s) Affected By DNA-directed RNA polymerase II subunit RPB1 (POLR2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selenium	DM25CGV	N. A.	N. A.	Approved	[22]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[23]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[24]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[25]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[26]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[27]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[28]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[29]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[30]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[31]
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Drug(s) Affected By Cyclin-dependent kinase 2 (CDK2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[32]
Mechlorethamine	DM0CVXA	Chronic myelogenous leukaemia	2A20.0	Approved	[33]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[34]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[35]
Selenium	DM25CGV	N. A.	N. A.	Approved	[36]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[37]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[38]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[39]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[40]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[41]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Substrate	[2]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Substrate	[2]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cyclin-dependent kinase 2 (CDK2)	OTB5DYYZ	CDK2_HUMAN	Gene/Protein Processing	[3]
DNA-directed RNA polymerase II subunit RPB1 (POLR2A)	OTHJQ1DZ	RPB1_HUMAN	Post-Translational Modifications	[3]

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References

1	Deferasirox FDA Label
2	Deferasirox pharmacogenetic influence on pharmacokinetic, efficacy and toxicity in a cohort of pediatric patients. Pharmacogenomics. 2017 Apr;18(6):539-554.
3	Iron chelators ICL670 and 311 inhibit HIV-1 transcription. Virology. 2007 Oct 25;367(2):324-33. doi: 10.1016/j.virol.2007.06.011. Epub 2007 Jul 13.
4	Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
5	Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
6	Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
7	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.
8	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.
9	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.
10	Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
11	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.
12	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.
13	Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.
14	Glucuronidation of nonsteroidal anti-inflammatory drugs: identifying the enzymes responsible in human liver microsomes. Drug Metab Dispos. 2005 Jul;33(7):1027-35.
15	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.
16	UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7.
17	Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011 May;21(5):280-8.
18	Pitavastatin: a review in hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168.
19	Troglitazone glucuronidation in human liver and intestine microsomes: high catalytic activity of UGT1A8 and UGT1A10. Drug Metab Dispos. 2002 Dec;30(12):1462-9.
20	Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers. Clin Pharmacol Ther. 2011 Apr;89(4):524-8.
21	Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
22	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.
23	Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
24	Phosphorylation of the RNA polymerase II largest subunit during heat shock and inhibition of transcription in HeLa cells. J Cell Physiol. 1994 Mar;158(3):417-26. doi: 10.1002/jcp.1041580305.
25	Quantitative phosphoproteomics reveal cellular responses from caffeine, coumarin and quercetin in treated HepG2 cells. Toxicol Appl Pharmacol. 2022 Aug 15;449:116110. doi: 10.1016/j.taap.2022.116110. Epub 2022 Jun 7.
26	Highly active combination of BRD4 antagonist and histone deacetylase inhibitor against human acute myelogenous leukemia cells. Mol Cancer Ther. 2014 May;13(5):1142-54.
27	Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
28	Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
29	Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
30	Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
31	The proapoptotic effect of zoledronic acid is independent of either the bone microenvironment or the intrinsic resistance to bortezomib of myeloma cells and is enhanced by the combination with arsenic trioxide. Exp Hematol. 2011 Jan;39(1):55-65.
32	Cannabidiol-induced transcriptomic changes and cellular senescence in human Sertoli cells. Toxicol Sci. 2023 Feb 17;191(2):227-238. doi: 10.1093/toxsci/kfac131.
33	G2 delay induced by nitrogen mustard in human cells affects cyclin A/cdk2 and cyclin B1/cdc2-kinase complexes differently. J Biol Chem. 1993 Apr 15;268(11):8298-308.
34	Estrogen receptor regulates E2F1 expression to mediate tamoxifen resistance. Mol Cancer Res. 2010 Mar;8(3):343-52. doi: 10.1158/1541-7786.MCR-09-0395. Epub 2010 Mar 9.
35	Down-regulation and decreased activity of cyclin-dependent kinase 2 in H2O2-induced premature senescence. Int J Biochem Cell Biol. 2003 Feb;35(2):246-54. doi: 10.1016/s1357-2725(02)00129-2.
36	Selenite and selenomethionine promote HL-60 cell cycle progression. J Nutr. 2002 Apr;132(4):674-9. doi: 10.1093/jn/132.4.674.
37	Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
38	Nonsteroidal anti-inflammatory drugs inhibit growth of human neuroendocrine tumor cells via G1 cell-cycle arrest. Int J Cancer. 2003 Dec 10;107(5):844-53. doi: 10.1002/ijc.11446.
39	Peripheral blood expression of nuclear factor-kappab-regulated genes is associated with rheumatoid arthritis disease activity and responds differentially to anti-tumor necrosis factor-alpha versus methotrexate. J Rheumatol. 2007 Sep;34(9):1817-22. Epub 2007 Aug 1.
40	Simvastatin inhibits cell growth and induces apoptosis and G0/G1 cell cycle arrest in hepatic cancer cells. Int J Mol Med. 2010 Nov;26(5):735-41. doi: 10.3892/ijmm_00000520.
41	Inhibition of prostate cancer cell colony formation by the flavonoid quercetin correlates with modulation of specific regulatory genes. Clin Diagn Lab Immunol. 2004 Jan;11(1):63-9. doi: 10.1128/cdli.11.1.63-69.2004.