Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 5306 | 1254053-43-4 |
None
None
Date | Agency | Company | Orphan |
---|---|---|---|
Sept. 21, 2018 | PMDA | Astellas Pharma Inc | |
Nov. 28, 2018 | FDA | ASTELLAS | |
Oct. 24, 2019 | EMA | ASTELLAS PHARMA EUROPE BV |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Febrile neutropenia | 243.27 | 43.85 | 97 | 1429 | 94530 | 46590006 |
Acute myeloid leukaemia | 189.29 | 43.85 | 52 | 1474 | 15726 | 46668810 |
Hepatic function abnormal | 141.62 | 43.85 | 50 | 1476 | 34371 | 46650165 |
Myelosuppression | 109.17 | 43.85 | 29 | 1497 | 7674 | 46676862 |
Platelet count decreased | 104.41 | 43.85 | 55 | 1471 | 99969 | 46584567 |
Cytopenia | 94.82 | 43.85 | 26 | 1500 | 7742 | 46676794 |
Neutrophil count decreased | 85.48 | 43.85 | 37 | 1489 | 43389 | 46641147 |
Differentiation syndrome | 84.70 | 43.85 | 16 | 1510 | 895 | 46683641 |
Acute myeloid leukaemia recurrent | 54.96 | 43.85 | 12 | 1514 | 1384 | 46683152 |
Acute febrile neutrophilic dermatosis | 52.12 | 43.85 | 13 | 1513 | 2672 | 46681864 |
Blast cell count increased | 44.19 | 43.85 | 8 | 1518 | 353 | 46684183 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Acute myeloid leukaemia | 208.36 | 41.88 | 62 | 1303 | 17944 | 29933169 |
Febrile neutropenia | 180.23 | 41.88 | 90 | 1275 | 106603 | 29844510 |
Myelosuppression | 176.76 | 41.88 | 45 | 1320 | 7277 | 29943836 |
Hepatic function abnormal | 115.98 | 41.88 | 50 | 1315 | 41895 | 29909218 |
Platelet count decreased | 91.98 | 41.88 | 58 | 1307 | 106071 | 29845042 |
Differentiation syndrome | 58.68 | 41.88 | 13 | 1352 | 1147 | 29949966 |
Source | Code | Description |
---|---|---|
ATC | L01EX13 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors |
CHEBI has role | CHEBI:35610 | cytostatic |
CHEBI has role | CHEBI:62434 | alk inhibitor |
CHEBI has role | CHEBI:68495 | type i programmed cell-death inducer |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Acute myeloid leukemia, disease | indication | 91861009 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.78 | acidic |
pKa2 | 8.76 | Basic |
pKa3 | 5.0 | Basic |
pKa4 | 4.38 | Basic |
pKa5 | 3.81 | Basic |
pKa6 | 0.35 | Basic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 40MG BASE | XOSPATA | ASTELLAS | N211349 | Nov. 28, 2018 | RX | TABLET | ORAL | Nov. 28, 2023 | NEW CHEMICAL ENTITY |
EQ 40MG BASE | XOSPATA | ASTELLAS | N211349 | Nov. 28, 2018 | RX | TABLET | ORAL | Nov. 28, 2025 | INDICATED FOR THE TREATMENT OF ADULT PATIENTS WHO HAVE RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH A FMS-LIKE TYROSINE KINULLSE 3 (FLT3) MUTATION AS DETECTED BY AN FDA-APPROVED TEST |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Receptor-type tyrosine-protein kinase FLT3 | Kinase | INHIBITOR | IC50 | 8.30 | SCIENTIFIC LITERATURE | DRUG LABEL |
ID | Source |
---|---|
1254053-84-3 | SECONDARY_CAS_RN |
4038030 | VANDF |
C3896738 | UMLSCUI |
CHEBI:145372 | CHEBI |
C6F | PDB_CHEM_ID |
CHEMBL3301622 | ChEMBL_ID |
CHEMBL3301603 | ChEMBL_ID |
DB12141 | DRUGBANK_ID |
D10709 | KEGG_DRUG |
49803313 | PUBCHEM_CID |
C000609080 | MESH_SUPPLEMENTAL_RECORD_UI |
8708 | IUPHAR_LIGAND_ID |
10048 | INN_ID |
66D92MGC8M | UNII |
2105806 | RXNORM |
299484 | MMSL |
35657 | MMSL |
35755 | MMSL |
d09076 | MMSL |
017854 | NDDF |
017855 | NDDF |
782974005 | SNOMEDCT_US |
782987004 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Xospata | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-1425 | TABLET | 40 mg | ORAL | NDA | 29 sections |