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

General Information of Drug (ID: DMUR64T)

Drug Name

Lesinurad Drug Info

Synonyms

LESINURAD; 878672-00-5; RDEA594; Zurampic; RDEA 594; UNII-09ERP08I3W; RDEA-594; 2-((5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetic acid; 09ERP08I3W; AK323774; C17H14BrN3O2S; 2-[[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl]thio]acetic acid; 2-[[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-1,2,4-triazol-3-yl]sulfanyl]acetic acid; 2-(5-Bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid

Indication

Disease Entry	ICD 11	Status	REF
Hyperuricaemia	5C55.Y	Approved	[1]

Cross-matching ID

PubChem CID: 53465279
ChEBI ID: CHEBI:90929
CAS Number: CAS 878672-00-5
TTD Drug ID: DMUR64T
VARIDT Drug ID: DR01130
INTEDE Drug ID: DR0926
ACDINA Drug ID: D00354

Molecule-Related Drug Atlas

Molecule Type:

DTT

DME

Drug Status:

Clinical Trial Drug(s)

Patented Agent(s)

Approved Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Urate anion exchanger 1 (URAT1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dotinurad	DM0UPQJ	Gout	FA25	Phase 3	[4]
URC102	DMY89BN	Gout	FA25	Phase 2	[5]
RDEA-684	DMNWYHD	Gout	FA25	Phase 2	[2]
RDEA3170	DM1TKG4	Hyperuricaemia	5C55.Y	Phase 2	[6]
AR882	DMFGYZ8	Gout	FA25	Phase 2	[7]
Sulfonamide derivative 11	DMJBR86	N. A.	N. A.	Patented	[8]
Cycloalkyl acid derivative 1	DMXMGSP	N. A.	N. A.	Patented	[8]
2-ethyl-3-(4-hydroxy) benzoyl benzofuran derivative 1	DMHYIAV	N. A.	N. A.	Patented	[8]
Tihoacetate derivative 1	DM6QHO0	N. A.	N. A.	Patented	[8]
Cycloalkyl acid derivative 2	DM09LY3	N. A.	N. A.	Patented	[8]
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Drug(s) Metabolized By Cytochrome P450 2C9 (CYP2C9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[9]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[10]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[11]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[12]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[13]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[12]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[14]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[15]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[16]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[17]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Urate anion exchanger 1 (URAT1)	TTA592U	S22AC_HUMAN	Modulator	[2]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2C9 (CYP2C9)^{Main DME}	DE5IED8	CP2C9_HUMAN	Substrate	[3]

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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: 7673).
2	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. (Target id: 1031).
3	FDA Label of Lesinurad. The 2020 official website of the U.S. Food and Drug Administration.
4	Dotinurad: a novel selective urate reabsorption inhibitor for the treatment of hyperuricemia and gout. Expert Opin Pharmacother. 2021 Aug;22(11):1397-1406.
5	Clinical pipeline report, company report or official report of Chugai Pharmaceutical (2013).
6	The pathophysiology of hyperuricaemia and its possible relationship to cardiovascular disease, morbidity and mortality. BMC Nephrol. 2013; 14: 164.
7	Clinical pipeline report, company report or official report of Arthrosi Therapeutics
8	Urate transporter URAT1 inhibitors: a patent review (2012 - 2015).Expert Opin Ther Pat. 2016 Jul 30:1-10.
9	Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9.
10	Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
11	Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98.
12	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
13	Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
14	Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
15	New insights into the structural features and functional relevance of human cytochrome P450 2C9. Part I. Curr Drug Metab. 2009 Dec;10(10):1075-126.
16	A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
17	A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.