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atrasentan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| endothelin receptor antagonists | 5767 | 195733-43-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Atrasentan is an ETA receptor antagonist (Ki = 0.034 nM) with >1800-fold selectivity for the ETA receptor compared to the endothelin type B receptor (Ki = 63.3 nM). Endothelin (ET)-1 is thought to contribute to the pathogenesis of immunoglobulin A nephropathy (IgAN) via the ETAR. It is indicated to reduce proteinuria in adults with primary IgAN at risk of rapid disease progression.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 2, 2025 | FDA | Novartis |
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 | N0000175581 | Endothelin Receptor Antagonist |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D065128 | Endothelin Receptor Antagonists |
| MeSH PA | D065130 | Endothelin A Receptor Antagonists |
| CHEBI has role | CHEBI:51452 | endothelin A receptor antagonist |
| CHEBI has role | CHEBI:76595 | nephroprotective agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Primary immunoglobulin A nephropathy | indication | 68779003 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 8623819 | Aug. 22, 2028 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 11874283 | Feb. 18, 2032 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 9364458 | July 7, 2034 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 11491137 | Dec. 16, 2040 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 11998526 | Dec. 16, 2040 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 12121509 | Dec. 16, 2040 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 12370174 | Dec. 16, 2040 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 12521369 | March 2, 2041 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | 12582631 | March 25, 2043 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 0.75MG BASE | VANRAFIA | NOVARTIS | N219208 | April 2, 2025 | RX | TABLET | ORAL | April 2, 2030 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Endothelin-1 receptor | GPCR | ANTAGONIST | Ki | 10.47 | DRUG LABEL | DRUG LABEL | |||
| Endothelin B receptor | GPCR | ANTAGONIST | Ki | 10.47 | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 173937-91-2 | SECONDARY_CAS_RN |
| CHEMBL9194 | ChEMBL_ID |
| 3487 | IUPHAR_LIGAND_ID |
| DB06199 | DRUGBANK_ID |
| 4025236 | VANDF |
| C0935914 | UMLSCUI |
| D000077868 | MESH_DESCRIPTOR_UI |
| CHEBI:135810 | CHEBI |
| CHEMBL2106068 | ChEMBL_ID |
| 7970 | INN_ID |
| D03009 | KEGG_DRUG |
| 159594 | PUBCHEM_CID |
| 393838 | MMSL |
| 43959 | MMSL |
| d10269 | MMSL |
| 020045 | NDDF |
| 020046 | NDDF |
| V6D7VK2215 | UNII |
| 2710448 | RXNORM |
| C000731977 | MESH_SUPPLEMENTAL_RECORD_UI |
| V6D7VK2215 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| VANRAFIA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-1420 | TABLET, FILM COATED | 0.75 mg | ORAL | NDA | 30 sections |