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Afatinib is an oral small molecule tyrosine kinase inhibitor used primarily for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with specific non-resistant epidermal growth factor receptor (EGFR) mutations. It is also indicated for metastatic squamous NSCLC in patients who have progressed after platinum-based chemotherapy. Afatinib acts as a potent and selective irreversible blocker of the ErbB family of receptors by covalently binding to and inhibiting EGFR (ErbB1), HER2 (ErbB2), ErbB3, and HER4 (ErbB4) signaling pathways. This mechanism disrupts tumor cell proliferation driven by these receptors. Developed by Boehringer Ingelheim, afatinib was first approved in 2013 under the brand name Gilotrif.
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