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tirabrutinib hydrochloride 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| agammaglobulinaemia tyrosine kinase (Bruton tyrosine kinase) inhibitors | 5423 | 1351636-18-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tirabrutinib is a potent and selective Bruton’s tyrosine kinase (BTK) inhibitor that irreversibly and covalently binds to BTK Cys-481 in B cells and inhibits aberrant B cell receptor signalling in B cell-related cancers and autoimmune diseases.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ABL1,ABL2,ACVR2B,AURKA,AURKB,BLK,BMX,BRAF,BTK,CAMK2D,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT3,FYN,GAK,ITK,JAK3,KDR,KIT,LCK,LYN,MAP3K21,MAP4K1,MAP4K2,MAP4K3,MAPK10,MARK4,MET,NTRK1,PDGFRB,PDK1,PDK2,PDK4,PTK6,RET,RIPK3,SIK2,SRC,STK33,SYK,TTK,YES1 | 50 | |||
| kinase-selectivity-class | ACVR2B,AURKA,BLK,BMX,BTK,CSF1R,CSK,EGFR,ERBB2,ERBB4,FYN,JAK3,KDR,LCK,LYN,MAP2K1,MAP3K21,PIK3CD,RIPK3,SRC,YES1 | 21 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 8.204 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| rat-kpuu-brain | Rat brain Kpuu | 0.034 | % | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 25, 2020 | PMDA | Ono Pharmaceutical |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Enterocolitis infectious | 27.31 | 21.51 | 3 | 4 | 2044 | 90626396 |
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 |
|---|---|---|
| ATC | L01EL06 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Bruton's tyrosine kinase (BTK) inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L01EL Bruton's tyrosine kinase (BTK) inhibitors 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Malignant lymphoma | indication | 118600007 | DOID:0060058 |
| Waldenström macroglobulinemia | indication | 190818004 | DOID:0050747 |
| Primary central nervous system lymphoma | indication | 307649006 | DOID:3234 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase BTK | Kinase | INHIBITOR | IC50 | 8.17 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Receptor tyrosine-protein kinase erbB-2 | Kinase | Kd | 6.21 | CHEMBL | |||||
| Platelet glycoprotein VI | Membrane receptor | IC50 | 5.92 | CHEMBL | |||||
| Receptor tyrosine-protein kinase erbB-4 | Kinase | INHIBITOR | IC50 | 7.11 | SCIENTIFIC LITERATURE | ||||
| Tyrosine-protein kinase Lck | Kinase | IC50 | 6.43 | CHEMBL | |||||
| Tyrosine-protein kinase Tec | Kinase | INHIBITOR | IC50 | 7.32 | SCIENTIFIC LITERATURE | ||||
| Tyrosine-protein kinase TXK | Kinase | INHIBITOR | IC50 | 7.04 | SCIENTIFIC LITERATURE | ||||
| Tyrosine-protein kinase Blk | Kinase | INHIBITOR | IC50 | 6.52 | SCIENTIFIC LITERATURE | ||||
| Cytoplasmic tyrosine-protein kinase BMX | Kinase | INHIBITOR | IC50 | 8.22 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| D11070 | KEGG_DRUG |
| U374135N48 | UNII |
| C4683808 | UMLSCUI |
| CHEBI:759297 | CHEBI |
| CHEMBL5314600 | ChEMBL_ID |
| 71571562 | PUBCHEM_CID |
| CHEMBL4071161 | ChEMBL_ID |
| C000608238 | MESH_SUPPLEMENTAL_RECORD_UI |
| DB15227 | DRUGBANK_ID |
| A1EK0 | PDB_CHEM_ID |
| 10320 | INN_ID |
| 9265 | IUPHAR_LIGAND_ID |
| 1439901-97-9 | SECONDARY_CAS_RN |
| U374135N48 | INXIGHT DRUGS |
Pharmaceutical products:
None