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

General Information of Drug (ID: DMMP51W)

Drug Name

sparsentan Drug Info

Synonyms

Sparsentan; RE-021; 254740-64-2; UNII-9242RO5URM; PS433540; PS-433540; CHEMBL539423; 9242RO5URM; BMS-346567; retrophin; Sparsentan [USAN]; compound 7 [PMID 15634011]; PS 33540; Sparsentan (RE-021); Sparsentan(PS433540); SCHEMBL535109; GTPL8448; BCP23969; BDBM50175523; SB16876; DB12548; CS-7947; DARA-a (Dual Acting Receptor Antagonist of angiotension and endothelin receptors); HY-17621; L023324; 4'-((2-butyl-4-oxo-1,3-diazaspiro[44]non-1-en-3-yl)methyl)-N-(4,5-dimethylisoxazol-3-yl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide; RE-021

Indication

Disease Entry	ICD 11	Status	REF
Focal segmental glomerulosclerosis	MF8Y	Phase 3	[1]
Hypertension	BA00-BA04	Phase 2	[2]
Myocardial infarction	BA41-BA43	Phase 2	[3]

Cross-matching ID

PubChem CID: 10257882
CAS Number: CAS 254740-64-2
TTD Drug ID: DMMP51W

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin II receptor type-1 (AGTR1)	TT8DBY3	AGTR1_HUMAN	Antagonist	[4]
Endothelin A receptor (EDNRA)	TTKRD0G	EDNRA_HUMAN	Antagonist	[4] , [5]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Endothelin A receptor (EDNRA)	DTT	EDNRA	3.776	4.505	5.121	3.536
Angiotensin II receptor type-1 (AGTR1)	DTT	AGTR1	9.315	6.241	6.761	5.625

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Focal segmental glomerulosclerosis

ICD Disease Classification

MF8Y

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Angiotensin II receptor type-1 (AGTR1)	DTT	AGTR1	8.95E-01	1.34E-02	0.07

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	ClinicalTrials.gov (NCT03493685) Study of Sparsentan in Patients With Primary Focal Segmental Glomerulosclerosis (FSGS) (DUPLEX). U.S. National Institutes of Health.
2	ClinicalTrials.gov (NCT00635232) A Study To Evaluate The Dose-Related Efficacy and Safety of PS433540 in Subjects With Hypertension. U.S. National Institutes of Health.
3	Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. J Med Chem. 2005 Jan 13;48(1):171-9.
4	Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
5	DOI: 10.1038/hr.2009.135