olmutinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5210 1353550-13-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • olmutinib
  • olita
  • BI 1482694
  • HM 61713
  • olmutinib hydrochloride
  • olmutinib HCl
Olmutinib is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) for the treatment of non-small cell lung cancer (NSCLC). Third-generation EGFR TKIs with covalent binding to the receptors demonstrate irreversible enzymatic inhibition of activating EGFR mutations and T790M mutation (a common reason for acquired EGFR TKI resistance), while sparing wild-type EGFR.
  • Molecular weight: 486.59
  • Formula: C26H26N6O2S
  • CLOGP: 5.14
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 2
  • TPSA: 82.62
  • ALOGS: -4.79
  • ROTB: 7

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None Korean Food and Drug Administration (KFDA)

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XE40 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors

Drug Use (View source of the data)

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

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.82 acidic
pKa2 8.43 Basic
pKa3 5.75 Basic
pKa4 1.26 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 8.04 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
CHL9B67L95 UNII
10093 INN_ID
54758501 PUBCHEM_CID
D10859 KEGG_DRUG
1842366-97-5 SECONDARY_CAS_RN
DB13164 DRUGBANK_ID
CHEMBL3786343 ChEMBL_ID
CHEMBL3989930 ChEMBL_ID
9196 IUPHAR_LIGAND_ID
C000617753 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None