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

Stem definitionDrug idCAS RN
agammaglobulinaemia tyrosine kinase (Bruton tyrosine kinase) inhibitors 5423 1351636-18-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tirabrutinib
  • tirabrutinib hydrochloride
  • velexbru
  • GS-4059
  • ONO-4059
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.
  • Molecular weight: 454.49
  • Formula: C25H22N6O3
  • CLOGP: 3.05
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 1
  • TPSA: 104.89
  • ALOGS: -4.23
  • ROTB: 5

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 25, 2020 PMDA Ono Pharmaceutical

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:

None

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

DiseaseRelationSNOMED_IDDOID
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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 Unclassified 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:

IDSource
D11070 KEGG_DRUG
U374135N48 UNII
C4683808 UMLSCUI
71571562 PUBCHEM_CID
CHEMBL4071161 ChEMBL_ID
C000608238 MESH_SUPPLEMENTAL_RECORD_UI
9265 IUPHAR_LIGAND_ID
DB15227 DRUGBANK_ID
10320 INN_ID
1439901-97-9 SECONDARY_CAS_RN

Pharmaceutical products:

None