Sparsentan

Angiotensin 2 Receptor Blocker — CARDIOVASCULAR SYSTEM

Key facts

Sparsentan is an onp drug in the Angiotensin 2 Receptor Blocker class catalogued in DrugCentral. It was first approved by the FDA in 2023. Its mechanism of action is classified as Angiotensin 2 Type 1 Receptor Antagonists, Breast Cancer Resistance Protein Inhibitors and Cytochrome P450 2B6 Inducers. DrugCentral lists 2 molecular targets, including AGTR1 and EDNRA. Recorded indications include Primary immunoglobulin A nephropathy.

• Approval status: onp (first approved 2023 by the FDA).
• Drug class: Angiotensin 2 Receptor Blocker; Endothelin Receptor Antagonist.
• Mechanism of action: Angiotensin 2 Type 1 Receptor Antagonists; Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2B6 Inducers.
• Molecular targets: AGTR1 and EDNRA (2 listed in DrugCentral).
• Indications: Primary immunoglobulin A nephropathy.
• ATC code: C09XX01 (Other agents acting on the renin-angiotensin system).
• Molecular formula: C32H40N4O5S; molecular weight 592.76 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Primary immunoglobulin A nephropathy

Contraindications (1)

• Pregnancy, function

Mechanism & targets

• Mechanism of action (MoA): Angiotensin 2 Type 1 Receptor Antagonists; Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2B6 Inducers; Cytochrome P450 2C19 Inducers; Cytochrome P450 2C9 Inducers; Endothelin Receptor Antagonists; P-Glycoprotein Inhibitors
• Established pharmacologic class: Angiotensin 2 Receptor Blocker; Endothelin Receptor Antagonist

Molecular targets (2)

Target	Gene	Action	Activity
Type-1 angiotensin II receptor	AGTR1	antagonist	Ki 9.44
Endothelin-1 receptor	EDNRA	antagonist	Ki 7.89

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2023-02-17	FDA	—	TRAVERE	Yes

ATC classification

ATC code	Therapeutic hierarchy
C09XX01	CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › Other agents acting on the renin-angiotensin system

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Hypotension	172.9
Urine protein/creatinine ratio increased	170.6
Glomerular filtration rate decreased	143.9
Glucose urine present	116.5
Blood creatinine increased	112.0
Urine albumin/creatinine ratio increased	108.8
Proteinuria	104.9
Dizziness	80.8
Blood urea increased	72.5
Product use in unapproved indication	64.1
Blood glucose increased	63.6
Blood chloride increased	60.1

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Sparsentan is on its molecule page.

• Molecular formula: C₃₂H₄₀N₄O₅S
• Molecular weight: 592.76 g/mol
• CAS number: 254740-64-2
• InChIKey: WRFHGDPIDHPWIQ-UHFFFAOYSA-N
• PubChem CID: 10257882

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

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Sparsentan used for?

DrugCentral lists the following indications for Sparsentan: Primary immunoglobulin A nephropathy.

How does Sparsentan work?

Sparsentan is classified as Angiotensin 2 Type 1 Receptor Antagonists, Breast Cancer Resistance Protein Inhibitors and Cytochrome P450 2B6 Inducers; its molecular targets in DrugCentral include AGTR1 (antagonist) and EDNRA (antagonist).

When was Sparsentan first approved?

Sparsentan was first approved by the FDA in 2023.

What drug class does Sparsentan belong to?

Sparsentan is in the Angiotensin 2 Receptor Blocker class.

What is the chemical formula of Sparsentan?

Sparsentan has the molecular formula C32H40N4O5S and a molecular weight of 592.76 g/mol.

Sources

• DrugCentral drug card 5711 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL539423 — compound record and bioactivity
• PubChem CID 10257882 — chemical identifiers
• DrugBank DB12548 — drug record
• FDA UNII 9242RO5URM — substance identity
• DailyMed: FDA labels for Sparsentan — current prescribing information (label search)
• UniProt P30556 (AGTR1) — target protein
• UniProt P25101 (EDNRA) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.