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tasurgratinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5835 | 1622204-21-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tasurgratinib succinate is an orally active, small molecule inhibitor of fibroblast growth factor receptors (FGFRs) 1, 2, and 3 being developed for the treatment of solid tumors, including cholangiocarcinoma (i.e., bile duct cancer) and breast cancer.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 24, 2024 | PMDA | Eisai Co., Ltd. |
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 |
|---|---|---|
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Unresectable FGFR2 fusion gene-positive biliary tract cance | indication | 363415003 | DOID:4607 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Fibroblast growth factor receptor 3 | Kinase | INHIBITOR | IC50 | 8.30 | IUPHAR | IUPHAR | |||
| Fibroblast growth factor receptor 1 | Kinase | INHIBITOR | IC50 | 8.20 | IUPHAR | IUPHAR | |||
| Fibroblast growth factor receptor 2 | Kinase | INHIBITOR | IC50 | 8.40 | IUPHAR | IUPHAR | |||
| Fibroblast growth factor receptor 4 | Kinase | INHIBITOR | IC50 | 6.19 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| A1LY1 | PDB_CHEM_ID |
| CHEMBL3686884 | ChEMBL_ID |
| C5667147 | UMLSCUI |
| CHEBI:755704 | CHEBI |
| 11580 | INN_ID |
| 1879965-80-6 | SECONDARY_CAS_RN |
| 78323434 | PUBCHEM_CID |
| 11414 | IUPHAR_LIGAND_ID |
| TN7CUD1NGA | UNII |
| D12404 | KEGG_DRUG |
| TN7CUD1NGA | INXIGHT DRUGS |
Pharmaceutical products:
None