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Details

Stereochemistry ACHIRAL
Molecular Formula C32H40N4O5S
Molecular Weight 592.749
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SPARSENTAN

SMILES

CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC(COCC)=C(C=C3)C4=CC=CC=C4S(=O)(=O)NC5=NOC(C)=C5C

InChI

InChIKey=WRFHGDPIDHPWIQ-UHFFFAOYSA-N
InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35)

HIDE SMILES / InChI

Molecular Formula C32H40N4O5S
Molecular Weight 592.749
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Sparsentan (RE-021; BMS-346567; PS433540; DARA-a) is a novel candidate in development by Retrophin for the treatment of focal segmental glomerulosclerosis (FSGS), a serious kidney disorder that often leads to end-stage renal disease (ESRD). Sparsentan is a first-in-class, orally active, dual-acting angiotensin receptor blocker (ARB) and highly selective endothelin Type A receptor antagonist. Sparsentan has been used in trials studying the treatment of focal segmental glomerulosclerosis. The FDA and European Commission have granted sparsentan orphan drug designation for FSGS. Retrophin also is advancing sparsentan for the treatment of immunoglobulin A nephropathy (IgAN) , or Berger’s disease, which also can lead to ESRD. Retrophin is examining the ability of sparsentan to slow the decline of kidney function in patients with FSGS and IgAN.

Approval Year

PubMed

PubMed

TitleDatePubMed

Sample Use Guides

Primary focal segmental glomerulosclerosis (FSGS): oral sparsentan 200 mg, 400 mg, or 800 mg once daily
Route of Administration: Oral
Sparsentan is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively.
Substance Class Chemical
Created
by admin
on Sat Dec 16 05:42:25 GMT 2023
Edited
by admin
on Sat Dec 16 05:42:25 GMT 2023
Record UNII
9242RO5URM
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SPARSENTAN
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
DARA
Common Name English
RE-021
Code English
FILSPARI
Brand Name English
Sparsentan [WHO-DD]
Common Name English
sparsentan [INN]
Common Name English
(1,1'-BIPHENYL)-2-SULFONAMIDE, 4'-((2-BUTYL-4-OXO-1,3-DIAZASPIRO(4.4)NON-1-EN-3-YL)METHYL)-N-(4,5-DIMETHYL-3-ISOXAZOLYL)-2'-(ETHOXYMETHYL)-
Systematic Name English
PS-433540
Code English
SPARSENTAN [USAN]
Common Name English
4'-((2-BUTYL-4-OXO-1,3-DIAZASPIRO(4.4)NON-1-EN-3-YL)METHYI)-N-(4,5- DIMETHYLISOXAZOL-3-YL)-2'-(ETHOXYMETHYL)BIPHENYL-2-SULFONAMIDE
Systematic Name English
PS433540
Code English
Classification Tree Code System Code
NCI_THESAURUS C66930
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
FDA ORPHAN DRUG 614417
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
FDA ORPHAN DRUG 410113
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
EU-Orphan Drug EU/3/15/1574
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
Code System Code Type Description
ChEMBL
CHEMBL539423
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
SMS_ID
100000163983
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
USAN
AB-139
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
EVMPD
SUB178314
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
CAS
1304732-86-2
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
NO STRUCTURE GIVEN
DAILYMED
9242RO5URM
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
CAS
254740-64-2
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
DRUG BANK
DB12548
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
NCI_THESAURUS
C152412
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
INN
10092
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
FDA UNII
9242RO5URM
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
PUBCHEM
10257882
Created by admin on Sat Dec 16 05:42:25 GMT 2023 , Edited by admin on Sat Dec 16 05:42:25 GMT 2023
PRIMARY
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