Bisantrene was classed as an anthracycline chemotherapeutic agent. It inhibits replication, kills tumor cells in clonogenic assays, and intercalates with DNA, where it inhibits both DNA and RNA synthesis. Bisantrene preferentially binds to A-T rich regions of DNA, where it effects changes to supercoiling and initiates strand breaks in association with DNA-associated proteins. This results from the inhibition of the enzyme topoisomerase II, which relaxes DNA coiling during replication and transcription. Toxicity studies in dogs and monkeys revealed that leukopenia, anorexia, diarrhea injection site necrosis, enterocolitis, muscle degeneration, and pulmonary edema were observed with high doses. Bisantrene was found to have less associated cardiotoxicity than other anthracenes. The existing data for bisantrene clearly demonstrated activity in acute myeloid leukemia, and in other indications including lymphoma, refractory breast cancer, and ovarian cancer.