Erlotinib

EGFR Inhibitor
DB00530
Approved Indication

For the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Also for use, in combination with gemcitabine, as the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic c

2 Targets
4 Resistance Mutations
17 References
1M17 Structure Loaded
3D Structure PDB: 1M17
Switch structure: RCSB ↗
Mechanism of Action

The mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the cell surface of normal cells and cancer cells.

Resistance Mutations — 122 resistance samples observed in COSMIC
Click a chip to highlight in viewer
EGFR
p.T745M 2 p.T790M 5
MET
p.L982_D1028del
PIK3CB
p.D1067V 5

Resistance mutations sourced from COSMIC Drug Resistance database. Cyan = on-target · Amber = off-target · numbered badge = PubMed references for that mutation

Details
DrugBank ID DB00530 ↗
Approval Date 2005-04-30
Molecular Weight 393.4357 g/mol
Drug Class EGFR Inhibitor
ATC Codes L01XE03
Synonyms Erlotinib, OSI-774
SMILES
COCCOC1=C(OCCOC)C=C2C(NC3=CC=CC(=C3)C#C)=NC=NC2=C1
ADMET Profile
Computing properties…