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] , [2]

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:

Approved Drug(s)

Clinical Trial Drug(s)

Patented Agent(s)

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Drug(s) Metabolized By Cytochrome P450 2C9 (CYP2C9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Progesterone	DMUY35B	Premature labour	JB00	Approved	[5]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[6]
Estradiol	DMUNTE3	Breast cancer	2C60-2C65	Approved	[7]
Acetaminophen	DMUIE76	Pain	MG30-MG3Z	Approved	[8]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[9]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[8]
Verapamil	DMA7PEW	Hypertension	BA00-BA04	Approved	[10]
Diclofenac	DMPIHLS	Osteoarthritis	FA00-FA05	Approved	[11]
Estrone	DM5T6US	Menopausal and postmenopausal disorder	GA30	Approved	[12]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[13]
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Drug(s) Targeting Urate anion exchanger 1 (URAT1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
URC102	DMY89BN	Gout	FA25	Phase 2	[14]
RDEA-684	DMNWYHD	Gout	FA25	Phase 2	[3]
RDEA3170	DM1TKG4	Hyperuricaemia	5C55.Y	Phase 2	[15]
Sulfonamide derivative 11	DMJBR86	N. A.	N. A.	Patented	[16]
Cycloalkyl acid derivative 1	DMXMGSP	N. A.	N. A.	Patented	[16]
2-ethyl-3-(4-hydroxy) benzoyl benzofuran derivative 1	DMHYIAV	N. A.	N. A.	Patented	[16]
Tihoacetate derivative 1	DM6QHO0	N. A.	N. A.	Patented	[16]
Cycloalkyl acid derivative 2	DM09LY3	N. A.	N. A.	Patented	[16]
Succinamide derivative 1	DMTXDSG	N. A.	N. A.	Patented	[16]
Benzene sulfonamide derivative 16	DMATBZW	N. A.	N. A.	Patented	[16]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Urate anion exchanger 1 (URAT1)	TTA592U	S22AC_HUMAN	Modulator	[3]

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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	[4]

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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	ClinicalTrials.gov (NCT01493531) Combining Lesinurad With Allopurinol in Inadequate Responders. U.S. National Institutes of Health.
3	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).
4	FDA Label of Lesinurad. The 2020 official website of the U.S. Food and Drug Administration.
5	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.
6	Tamoxifen inhibits cytochrome P450 2C9 activity in breast cancer patients. J Chemother. 2006 Aug;18(4):421-4.
7	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.
8	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
9	Drug-drug interactions with imatinib: an observational study. Medicine (Baltimore). 2016 Oct;95(40):e5076.
10	Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos. 2000 Feb;28(2):125-30.
11	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.
12	A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7.
13	A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63.
14	Clinical pipeline report, company report or official report of Chugai Pharmaceutical (2013).
15	The pathophysiology of hyperuricaemia and its possible relationship to cardiovascular disease, morbidity and mortality. BMC Nephrol. 2013; 14: 164.
16	Urate transporter URAT1 inhibitors: a patent review (2012 - 2015).Expert Opin Ther Pat. 2016 Jul 30:1-10.