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Introduction:
Afatinib (BIBW 2992) is the second-generation potent and irreversible dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinase, developed by Boehringer Ingelheim, Germany. It is capable of irreversibly inhibiting the activity of the tyrosine kinase by undergoing the Michael reaction with the thiol group of cysteine at position 797 of the EGFR.
Function:
1. Like lapatinib and neratinib, afatinib is a protein kinase inhibitor that also irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases.
2. Afatinib is not only active against EGFR mutations targeted by first generation TKIs like erlotinib or gefitinib, but also against mutations such as T790M which are not sensitive to these standard therapies.Because of its additional activity against Her2, it is being investigated for breast cancer as well as other EGFR and Her2 driven cancers.
3. Afatinib is a drug for the first-line treatment of patients with distinct types of metastatic (EGFR mutation positive) non-small cell lung carcinoma (NSCLC).It acts as an irreversible covalent inhibitor of the receptor tyrosine kinases epidermal growth factor receptor (EGFR) and erbB-2 (HER2).