Clinical trials with 1,3-bis(2-chloroethyl)-1-nitrosourea, NSC-409962.

Abstract

Summary The compound 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) has unusual physical and chemical properties and is a highly effective anti-cancer agent in animals. Preliminary trials were conducted in 144 patients with various maligmant diseases at several dose levels and schedules. These trials indicated that the following i.v. dose schedules were tolerable and comparable in toxicity: 250 mg/sq m in a single dose, 125 mg/sq m for 3 successive days, and 90 mg/sq m/week for 6 weeks. Hematopoietic toxicity was dose limiting and was delayed and prolonged after drug administration. Reversible minor hepatic and renal toxicity was seen in 26% and 10% of the patients, respectively. Anti-tumor activity was noted in a variety of tumors in man.