canertinib

Canertinib (CI-1033) is an orally available, potent and irreversible pan-ErbB tyrosine kinase inhibitor developed for the treatment of cancer. It inhibits all four members of the ErbB receptor family (EGFR/ErbB1, HER2/ErbB2, ErbB3-dependent signaling via inhibition of other family members, and HER4/ErbB4), with low nanomolar IC50 values. Canertinib binds covalently to the ATP-binding site in the tyrosine kinase domain of these receptors through its acrylamide group. This results in permanent inactivation and prolonged suppression of downstream signaling pathways such as Ras/MAPK and PI3K/AKT. The drug was investigated primarily for solid tumors including non-small cell lung cancer (NSCLC), breast cancer, and esophageal squamous cell carcinoma but did not demonstrate sufficient efficacy in clinical trials to warrant further development[1][5][6][10]. Development was discontinued by Pfizer.

Other names

canertinibcanertinib dihydrochlorideN-(4-(3-chloro-4-fluorophenylamino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamideC78W1K5ASFC-78W1K5ASFC 78W1K5ASF