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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5211 811803-05-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rivoceranib
  • apatinib
  • apatinib mesylate
  • apatinib mesilate
  • YN968D1
Apatinib is an oral tyrosine kinase inhibitor approved in China for the treatment of patients with advanced metastatic gastric cancer.
  • Molecular weight: 397.48
  • Formula: C24H23N5O
  • CLOGP: 3.72
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 90.70
  • ALOGS: -4.52
  • ROTB: 6

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None China Food and Drug Administration (CFDA)

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bone marrow failure 70.94 53.13 17 96 27432 29546982

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Palmar-plantar erythrodysaesthesia syndrome 85.10 63.80 20 225 28799 64469688
Bone marrow failure 65.53 63.80 18 227 47934 64450553

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Secondary malignant neoplasm of stomach indication 94606003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.66 acidic
pKa2 6.69 Basic
pKa3 4.82 Basic

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
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 9 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 5.32 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase Kd 5.62 CHEMBL
Tyrosine-protein kinase CSK Kinase INHIBITOR IC50 6.28 IUPHAR
Proto-oncogene tyrosine-protein kinase Src Kinase INHIBITOR IC50 6.28 SCIENTIFIC LITERATURE
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase INHIBITOR IC50 7.89 SCIENTIFIC LITERATURE
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 6.37 SCIENTIFIC LITERATURE

External reference:

IDSource
C2346836 UMLSCUI
CHEMBL3186534 ChEMBL_ID
11315474 PUBCHEM_CID
DB14765 DRUGBANK_ID
CHEMBL3545414 ChEMBL_ID
7648 IUPHAR_LIGAND_ID
5S371K6132 UNII
10596 INN_ID
018934 NDDF
C553458 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None