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Afatinib


Mechanism of action:

Afatinib is an irreversible tyrosine kinase inhibitor (TKI) that mainly targets members of the epidermal growth factor receptor (EGFR) family, including EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4). Its mechanism involves covalent binding to the ATP-binding site of these receptors, thereby inhibiting their tyrosine kinase activity and blocking downstream signaling pathways such as the RAS-RAF-MEK-ERK and PI3K-AKT pathways. This ultimately suppresses tumor cell growth, proliferation, and survival.

Reference(s):

Modjtahedi et al. (2014). A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer. Naunyn Schmiedebergs Arch Pharmacol.

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