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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5209 610798-31-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • icotinib
  • icotinib hydrochloride
Icotinib is a new epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that developed and used in China for the treatment of patients with non-small cell lung cancer (NSCLC).
  • Molecular weight: 391.43
  • Formula: C22H21N3O4
  • CLOGP: 4.16
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 74.73
  • ALOGS: -4.49
  • ROTB: 2

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None China Food and Drug Administration (CFDA) Zhejiang Beta Pharma Inc.

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:

SourceCodeDescription
ATC L01EB08 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

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

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.01 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
Epidermal growth factor receptor Kinase INHIBITOR IC50 8.70 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Cyclin-G-associated kinase Kinase Kd 6.14 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 5.58 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 5.98 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 6.64 CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma Kinase Kd 5.33 CHEMBL
Mitotic checkpoint serine/threonine-protein kinase BUB1 Kinase Kd 5.54 CHEMBL
Cysteine--tRNA ligase, cytoplasmic Enzyme Kd 6.19 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.38 CHEMBL

External reference:

IDSource
9G6U5L461Q UNII
1204313-51-8 SECONDARY_CAS_RN
C2604307 UMLSCUI
CHEMBL2087361 ChEMBL_ID
22024915 PUBCHEM_CID
DB11737 DRUGBANK_ID
CHEMBL4297665 ChEMBL_ID
7641 IUPHAR_LIGAND_ID
C531470 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None