Aclarubicin is one of the derivatives of anthracycline drugs exhibiting less side effects in comparison with the commonly used anthracyclines Generation - doxorubicin and daunorubicin. This article presents the current knowledge of the molecular mechanisms of the cytotoxic effect of the ACL, such as the effect on the activity of topoisomerase I and II, the processes of replication and transcription. Also discussed was the impact of the ACL with the cell membrane, drug transport through the membrane and the plasma membrane involved in the acquisition of multidrug resistance. Also shows the role of reactive oxygen species in the induction of antitumor activity of the drug and shown to aclarubicin directs the cancer cells undergoing apoptosis and is involved in the processes of differentiation and metastasis of tumors.