Phase I experience with emetine hydrochloride (NSC 33669) as an antitumor agent

This report details a Phase I dose‐ranging experiment of the use of emetine in patients with a variety of malignant diseases. The data show that emetine can be given intravenously at 4‐day intervals with minimal toxicity. Severe muscle weakness, the most important dose‐limiting toxic effect, began at approximately a 15 mg/kg cumulative dose level and resulted in discontinuance of therapy in two patients. Of 5 patients who received greater than 10.4 mg/kg, 2 stabilized previously rapidly progressive disease, one had marked reduction in a purulent bloody vaginal discharge, and 2 who had received the highest total dose had 50% or greater reduction in lung tumor size. The present data suggest a reasonable regimen to be 1.5 mg/kg IV weekly for a minimum total dose of 15 mg/kg. Emetine is not myelosuppressive and therefore may be useful in the patient with poor marrow reserve. Alternatively, it can be used in combination with agents of different toxicities in hope of showing additive effects without additive toxicity.