Afatinib dimaleate

Afatinib is an irreversible dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinase. It shows IC₅₀ values of 0.5 nM and 14 nM for EGFR kinase and HER2 kinase respectively. It inhibits EGF-induced EGFR phosphorylation and cellular proliferation in cell lines such as EGFR-overexpressing and HER2-expressing cell lines A431, NIH-3T3-HER2, NCI-N87 and BT-474. It causes tumour regression in mice carrying EGFR-overexpressing and HER2-expressing A431 xenografts, EGFR-overexpressing and HER2-expressing MDA-MB-453 xenografts and NCI-N87 gastric and SKOV-3 ovarian models.