All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

sparsentan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
endothelin receptor antagonists	5711	254740-64-2

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: sparsentan filspari PS433540 RE-021

Sparsentan is a single molecule with antagonism of the endothelin type A receptor (ETAR) and the angiotensin II type 1 receptor (AT1R). Sparsentan has high affinity for both the ETAR (Ki= 12.8 nM) and the AT1R (Ki=0.36 nM), and greater than 500-fold selectivity for these receptors over the endothelin type B and angiotensin II subtype 2 receptors. Endothelin-1 and angiotensin II are thought to contribute to the pathogenesis of IgAN via the ETAR and AT1R, respectively Molecular weight: 592.76 Formula: C32H40N4O5S CLOGP: LIPINSKI: 2 HAC: 9 HDO: 1 TPSA: 114.10 ALOGS: ROTB: 11 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Feb. 17, 2023	FDA	TRAVERE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
FDA MoA	N0000175364	Endothelin Receptor Antagonists
FDA EPC	N0000175561	Angiotensin 2 Receptor Blocker
FDA EPC	N0000175581	Endothelin Receptor Antagonist
FDA MoA	N0000180999	Angiotensin 2 Type 1 Receptor Antagonists
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000185507	Cytochrome P450 2C9 Inducers
FDA MoA	N0000185607	Cytochrome P450 2C19 Inducers
FDA MoA	N0000187064	Cytochrome P450 2B6 Inducers
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Primary immunoglobulin A nephropathy	indication	68779003
Pregnancy, function	contraindication	289908002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
200MG	FILSPARI	TRAVERE	N216403	Feb. 17, 2023	RX	TABLET	ORAL	9993461	March 29, 2030	TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) IN ADULTS AT RISK OF RAPID DISEASE PROGRESSION
400MG	FILSPARI	TRAVERE	N216403	Feb. 17, 2023	RX	TABLET	ORAL	9993461	March 29, 2030	TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) IN ADULTS AT RISK OF RAPID DISEASE PROGRESSION

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
200MG	FILSPARI	TRAVERE	N216403	Feb. 17, 2023	RX	TABLET	ORAL	Feb. 17, 2028	NEW CHEMICAL ENTITY
400MG	FILSPARI	TRAVERE	N216403	Feb. 17, 2023	RX	TABLET	ORAL	Feb. 17, 2028	NEW CHEMICAL ENTITY
200MG	FILSPARI	TRAVERE	N216403	Feb. 17, 2023	RX	TABLET	ORAL	Feb. 17, 2030	TO REDUCE PROTEINURIA IN ADULTS WITH PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) AT RISK OF RAPID DISEASE PROGRESSION, GENERALLY A URINE PROTEIN-TO-CREATININE RATIO (UPCR) > OR = 1.5 G/G
400MG	FILSPARI	TRAVERE	N216403	Feb. 17, 2023	RX	TABLET	ORAL	Feb. 17, 2030	TO REDUCE PROTEINURIA IN ADULTS WITH PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) AT RISK OF RAPID DISEASE PROGRESSION, GENERALLY A URINE PROTEIN-TO-CREATININE RATIO (UPCR) > OR = 1.5 G/G

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Type-1 angiotensin II receptor	GPCR	P30556	AGTR1_HUMAN	ANTAGONIST	Ki	9.44		DRUG LABEL	DRUG LABEL
Endothelin-1 receptor	GPCR	P25101	EDNRA_HUMAN	ANTAGONIST	Ki	7.89		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
CHEMBL539423	ChEMBL_ID
C000634424	MESH_SUPPLEMENTAL_RECORD_UI
8448	IUPHAR_LIGAND_ID
DB12548	DRUGBANK_ID
019314	NDDF
4042062	VANDF
C4489760	UMLSCUI
10092	INN_ID
10257882	PUBCHEM_CID
2630535	RXNORM
D11776	KEGG_DRUG
9242RO5URM	UNII
365302	MMSL
41258	MMSL
d10011	MMSL

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
FILSPARI	HUMAN PRESCRIPTION DRUG LABEL	1	68974-200	TABLET, FILM COATED	200 mg	ORAL	NDA	26 sections
FILSPARI	HUMAN PRESCRIPTION DRUG LABEL	1	68974-400	TABLET, FILM COATED	400 mg	ORAL	NDA	26 sections