Objective: To review the pharmacology, pharmacokinetics, clinical efficacy, and toxicity of gefitinib in non-small-cell lung cancer (NSCLC).
Data sources: Primary literature search through MEDLINE and CANCERLIT, and abstract presentations (1966-May 2003).
Study selection and data extraction: All published trials and abstracts citing gefitinib were evaluated, and all information deemed relevant was included in this article.
Data synthesis: NSCLC is known to overexpress epidermal growth factor receptor (EGFR). Gefitinib is a selective EGFR tyrosine kinase inhibitor. Based on the Phase I/II trial results, the optimal dose is 250 mg/d orally. It is well tolerated, with minimal and reversible toxicity. Skin rash and diarrhea are the most common adverse effects. Recent trials have shown that gefitinib provided a 10% tumor response rate and improved disease-related symptoms in patients with refractory, advanced NSCLC.
Conclusions: Gefitinib, with a unique mechanism of action and favorable toxicity profile, has demonstrated clinical activity in NSCLC patients with chemotherapy-refractory disease. It provides a valuable addition to the treatment options as monotherapy in patients with advanced NSCLC after failure of both platinum-based and docetaxel chemotherapies. Further research is required to evaluate the use of gefitinib in different clinical settings.