SAFETY AND ANTITUMOR ACTIVITY OF GEFITINIB: AN OVERVIEW

Gefitinib is an epidermal growth factor receptor tyrosine kinase inhibitor, a promising anticancer agent for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC), especially in EGFR mutated patients. It acts by interfering with the proliferation and survival of cancer cells and other host-dependent process promoting cancer cell growth by blocking signal transduction pathways. The major advantage of Gefitinib over standard chemotherapy is that it selectively inhibits cellular pathways involved in tumor survival with minimal effect on normal cells. Gefitinib was the first agent to be tested in clinical trials among tyrosine kinase inhibitors class of anticancer drugs. Gefitinib is a very slightly soluble novel anticancer drug whose solubility and dissolution can be improved by its complexation with cyclodextrins. Gefitinib is a generally well-tolerated treatment, with skin rash and diarrhea being the most common treatment adverse effects. Gefitinib has the potential of stimulating cell immunity against malignant cells. Binding of Gefitinib to human plasma protein is extensive. This article reviews the safety and efficacy of Gefitinib along with chemistry, mechanism, pharmacokinetics, drug interactions and special precautions to be taken in special cases like Geriatrics, Paediatrics, Pregnant women and nursing women during treatment with Gefitinib.