Gefitinib, commercially known by brand names such as Gefttinat Table, is a first-generation EGFR tyrosine kinase inhibitor (EGFR-TKI). It is primarily used to treat non-small cell lung cancer (NSCLC) that has tested positive for EGFR mutations. First approved in Japan and later globally, Gefitinib represents a significant leap in cancer therapeutics due to its targeted action and minimal systemic toxicity.
Unlike older, non-specific chemotherapies that destroy all rapidly dividing cells, Gefitinib's mechanism of action allows it to selectively target and inhibit EGFR-mutant cancer cells, thereby enhancing efficacy while reducing unnecessary side effects.
How Gefitinib Works: The Science Behind the Therapy
Gefitinib belongs to the class of protein kinase inhibitors. Specifically, it blocks the ATP-binding site of the epidermal growth factor receptor (EGFR) tyrosine kinase domain. This inhibition prevents the phosphorylation and activation of EGFR, a receptor that drives the uncontrolled proliferation of cancer cells in many NSCLC patients.