sparsentan   Click here for help

GtoPdb Ligand ID: 8448

Synonyms: DARA-a (Dual Acting Receptor Antagonist of angiotension and endothelin receptors) | BMS-346567 | compound 7 [PMID 15634011] | Filspari® | RE-021 | retrophin
Approved drug Immunopharmacology Ligand
sparsentan is an approved drug (FDA (2023))
Compound class: Synthetic organic
Comment: Sparsentan (RE-021) is a selective dual-acting receptor antagonist with affinity for endothelin (A type) and angiotensin II receptors (Type 1) [5-6]. Sparsentan combines the active moieties of the selective AT1 receptor antagonist irbesartan and a selective ETA receptor antagonist (see ligand 91 in [5]).
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 1
Rotatable bonds 12
Topological polar surface area 122.48
Molecular weight 592.27
XLogP 5.9
No. Lipinski's rules broken 2
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Canonical SMILES CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2
Isomeric SMILES CCCCC1=NC2(C(=O)N1Cc1ccc(c(c1)COCC)c1ccccc1S(=O)(=O)Nc1noc(c1C)C)CCCC2
InChI 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)
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Summary of Clinical Use Click here for help
Sparsentan progressed to phase 3 clinical trial for evaluation as a potential treatment for focal segmental glomerulosclerosis (FSGS) [3]. FSGS is a rare glomerular disorder which results in proteinuria and progression to end-stage kidney disease (ESKD) over 5-10 years. The EMA issued orphan designation for the treatment of primary IgA nephropathy (IgAN) in January 2022 [2]. FDA approval for this indication was granted in February 2023 (under their accelerated approval program) [7]. The FDA's approval indicates sparsentan's use for patients with primary IgAN who are at high risk of rapid disease progression. Sparsentan is administered to reduce proteinuria in these patients.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Reduction of proteinuria in FSGS is regarded as being beneficial by slowing disease progression [1].
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03493685 Study of Sparsentan in Patients With Primary Focal Segmental Glomerulosclerosis (FSGS) Phase 3 Interventional Travere Therapeutics, Inc. 4
NCT01613118 Randomized, Double-Blind, Safety and Efficacy Study of RE-021 (Sparsentan) in Focal Segmental Glomerulosclerosis Phase 2 Interventional Travere Therapeutics, Inc. 8