- Gefitinib, a selective and potent tyrosine kinase inhibitor, exhibits high specificity for the epidermal growth factor receptor (EGFR), predominantly targeting the ATP-binding domain of the receptor’s intracellular tyrosine kinase region.
- This small molecule inhibitor demonstrates particular efficacy against specific EGFR mutations, including deletions in exon 19 and the L858R point mutation in exon 21.
- The mechanism of action of Gefitinib involves reversible competitive binding at the ATP-binding site of EGFR. Through this competitive inhibition, Gefitinib prevents ATP from accessing its binding site, thereby inhibiting the subsequent phosphorylation events necessary for receptor activation and signal transduction. This inhibition is particularly effective in tumors harboring activating EGFR mutations.
- Upon EGFR inhibition, Gefitinib effectively disrupts multiple downstream signaling cascades critical for cell survival and proliferation. These include the RAS/RAF/MEK/ERK pathway, PI3K/AKT/mTOR pathway, and JAK/STAT pathway. The disruption of these signaling networks leads to the inhibition of cell proliferation, increased apoptosis, and reduced angiogenic signaling in EGFR-dependent cells.
- The selective inhibitory properties of Gefitinib demonstrate significant clinical efficacy in various malignancies, particularly in non-small cell lung cancer (NSCLC) with activating EGFR mutations. Its therapeutic application has revolutionized the treatment paradigm for EGFR-mutant NSCLC, establishing the role of molecular targeted therapy in clinical oncology.
- Furthermore, the characteristic molecular profile of Gefitinib has made it an invaluable tool for studying EGFR-dependent cellular processes and developing strategies to overcome acquired resistance mechanisms.
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