Pharmacokinetics of 4-demethoxydaunorubicin in cancer patients

Summary The clinical pharmacokinetics of 4-demethoxydaunorubicin was investigated in 28 cancer patients who received the drug orally. The majority of the patients were elderly (median age, 72 years). Nine of them also received an i. v. dose, and the bioavailability of the oral dose ranged between 9% and 39%. 4-Demethoxydaunorubicin peak levels were achieved 2–4 h after the oral dose in most patients. The drug was rapidly and extensively metabolized to 4-demethoxy-13-hydroxydaunorubicin, which is probably as active as the parent drug. The metabolite levels were much higher and longer lasting than the parent drug, suggesting that it may play an important role in the drug's pharmacological effects.