In two open, randomized, crossover trials in healthy male volunteers, the mean AUC concentration and Cmaxwere decreased by 83% and 65%, respectively, when patients (n = 18) were given 500 mg of gefitinib alone on day 10 of a 16-day dosing regimen of 600 mg/day of rifam-picin (e.g., Rimactone®, Geneva), a potent CYP-3A4 inducer. In [...]

Ranson et al. conducted a phase I, escalating, multiple-dose trial to investigate the tolerability, pharmacokinetics, and antitumor activity of gefitinib in patients with solid malignant tumors. The study was designed to evaluate dose levels of 50, 100, 150, 225, 300, 400, 525, 700, and 925 mg/day. Additional patients could be recruited for the study if [...]

The FDA approved gefitinib based on results from the Iressa Dose Evaluation in Advanced Lung Cancer (IDEAL-2), a phase II trial that included 216 patients, of whom 142 had not responded to both platinum-based and docetaxel chemotherapies. Approximately 10% of patients in this trial achieved a response rate defined as a decrease in tumor size [...]

INTRODUCTION Gefitinib (ZD1839, Iressa™, Astra-Zeneca) is an anilinoquinazoline that has been approved by the U.S. Food and Drug Administration (FDA) as a single-agent therapy for the treatment of patients with locally advanced or meta-static non-small cell lung cancer (NSCLC) who have not responded successfully to chemotherapies with platinum (carboplatin, cisplatin) and doce-taxel (Taxotere®, Aventis), two [...]