Afatinib CAS 439081-18-2 Purity >99.5% (HPLC) Factory

Afatinib, also known as BIW-2992, (CAS: 439081-18-2) 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. On July 12, 2013, it became a new drug for anti-small cell lung cancer approved by the US FDA under the trade name of Gilotrif. This drug is a tablet. It is used for the treatment of the patients diagnosed with metastatic non-small cell lung cancer (NSCLC) with the loss of the 19th exon or L858R mutation in the 21th exon of the tumor epidermal growth factor receptor (EGFR) confirmed using the kit approved by FDA. The drug is also effective in the treatment of HER2-positive patients with advanced breast cancer. Afatinib belongs to a class of drugs known as tyrosine kinase inhibitors. Tyrosine kinase inhibitors are designed to block the action of a specific enzyme called tyrosine kinase. This enzyme plays a big role in the function of cells, and is active in promoting tumor growth and progression. Afatinib works to inhibit the function of two types of tyrosine kinases: epidermal growth factor receptor (EGFR) and Her2, which are "over-expressed" by several types of cancer. By blocking the function of these tyrosine kinases, Afatinib may prevent cancer cells from dividing and growing.