Twelve patients affected by different types of acute
leukemia received
idarubicin (4-demethoxy-daunorubicin) by oral route at the total dosage of 45, 60 or 90 mg/m2 distributed over three consecutive days.
Drug response was assessed by the decrease in blast cells in peripheral blood and showed some variations between the different types of
leukemia.
Acute myelogenous leukemia patients and those with blastic crisis of
chronic myeloid leukemia appeared to be the more responsive groups; however, the lower dose schedule could explain the less satisfactory results obtained in lymphatic
leukemia patients. Data suggest that
idarubicin is absorbed rapidly after oral ingestion, in spite of
nausea and
vomiting, which appeared 3-4 h later and were easily controlled by
antiemetic therapy. The purpose of fractionating the
drug dosage over three consecutive days is to prolong in the blood an elevated concentration of the main
idarubicin metabolite (13-dihydro-derivative), which presents in experimental models an antileukemic potency similar to the parent compound. This study confirms that
idarubicin is effective in acute
leukemia also by oral route. This formulation could offer some advantages for subjects who cannot tolerate parenteral
chemotherapy and it could be proposed in maintenance
leukemia protocols.