Description
Canertinib is an irreversible inhibitor of EGFR (HER2/ErbB). This compound is currently in clinical trials as an anticancer chemotherapeutic, displaying activity against a variety of cancers. In a cellular model of melanoma, canertinib exhibits cytostatic activity, stopping cell growth in the G1 phase, but not inducing apoptosis except at very high concentrations. In a related animal model, canertinib inhibits tumor growth. Separately, canertinib inhibits Akt and ERK1/2 in cells lacking ErbB receptors and induces caspase-mediated apoptosis.
References
Djerf Severinsson EA, Trinks C, Gréen H, et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8. PMID: 21982771.
Trinks C, Severinsson EA, Holmlund B, et al. The pan-ErbB tyrosine kinase inhibitor canertinib induces caspase-mediated cell death in human T-cell leukemia (Jurkat) cells. Biochem Biophys Res Commun. 2011 Jul 8;410(3):422-7. PMID: 21669187.
Zinner RG, Nemunaitis J, Eiseman I, et al. Phase I clinical and pharmacodynamic evaluation of oral CI-1033 in patients with refractory cancer. Clin Cancer Res. 2007 May 15;13(10):3006-14. PMID: 17505003.
