Phase II clinical and pharmacological study of oral 4-demethoxydaunorubicin in advanced non-pretreated small cell lung cancer.

4-Demethoxydaunorubicin (4-DMDNR) is an oral anthracycline with antitumour activity demonstrated in a number of clinical studies. We have assessed the usefulness of 4-DMDNR in 16 patients with advanced small cell lung cancer, none of whom had received previous chemotherapy. There were no complete or partial responders among the 14 evaluable patients, but 9 patients showed a minor radiographic improvement and 6 reported transient symptomatic improvement. Side effects were mostly minor or moderate, although one patient succumbed to septicaemia during neutropenia following treatment. There was no evidence of cardiotoxicity in any patient. Pharmacological studies were undertaken in 8 patients. A previously undescribed metabolite, identified as the 7-deoxyaglycone of 4-demethoxydaunorubicinol, was detected in 3 patients and these 3 patients all showed some anti-tumor response.