Abstract Thirteen patients were treated with both the oral and intravenous preparations of 4-demethoxydaunorubicin (DMDR). The drug was well tolerated in both forms. Neutropenia was the dose-limiting side-effect. Approximately 30% of the compound was absorbed when given orally. The maximum tolerated dose was 12.5 mg/m 2 intravenously or 50 mg/m 2 (10 mg/m 2 q d × 5) orally, given every 21–28 days.