The antileukemic activity of the Imatinib loaded PEGylated Polypropyleneimine (PPI) dendrimer of Tyrosin kinase inhibitor antitumor bioactive was studied. The ascetic form of myelogenous leukemia AML-193 (transplantation dose 1x105 tumor cells/mouse, i. p.), in hybrid mice BDF1, was used as tumor model. An antileukemic activity of the studied Imatinib loaded PEGylated Polypropyleneimine (PPI) dendrimer was found. The criterion “increase of life span” (ILS %) reached maximally 278.7 % for the drug loaded dendrimer. The studied dendrimer with Imatinib showed lower toxicity with improved antileukemic activity in comparison with free Imatinib. The further experiments in this field are in progress, aiming to design better dendritic formulations, with potential clinical use.