Gefitinib CAS 184475-35-2 Purity >99.5% (HPLC)

Gefitinib (CAS: 184475-35-2) is a highly specific anti-tumor targeted therapeutic drug developed by AstraZeneca, UK. It is the first molecular targeted drug for the treatment of non-small cell lung cancer. It works by selectively inhibiting the signal transduction pathway of epidermal growth factor receptor tyrosine kinase (EGFR-TK). Epidermal growth factor (EGF) is a polypeptide with a relative molecular mass of 6.45 × 103, which can combine with epidermal growth factor receptor (EGFR) on the target cell membrane to produce biological effects. EGFR is a tyrosine kinase (TK) type receptor. When it binds to EGF, it can promote TK activation in the recipient body, resulting in autophosphorylation of receptor tyrosine residues, providing continuous division signals to cells, causing cell proliferation and differentiation. EGFR is abundant in human tissues and is highly expressed in malignant tumors. By blocking the EGFR signaling pathway on the cell surface, gefitinib hinders tumor growth, metastasis and angiogenesis, and can induce apoptosis of tumor cells. In August 2002, gefitinib was first marketed in Japan as a first-line treatment for non-small cell lung cancer under the trade name Iressa. In May 2003, the U.S. Food and Drug Administration approved gefitinib as the third-line monotherapy for patients with advanced non-small cell lung cancer who were ineffective with platinum-based anticancer drugs and docetaxel chemotherapy. At present, it has been approved by Australia, Japan, Argentina, Singapore and South Korea for the treatment of advanced non-small cell lung cancer. On February 28, 2005, the China Food and Drug Administration approved gefitinib for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that had previously received chemotherapy. It is not currently approved for use as first-line therapy for advanced NSCLC. On July 1, 2009, the European Medicines Agency officially approved gefitinib for the first-line, second-line and third-line treatment of locally advanced or metastatic non-small cell lung cancer with EGFR gene mutations in adults.