The Rediscovery of Bisantrene: A Review of the Literature

Abstract

Bisantrene is an anthracene with anthracycline-like antitumor activity that has been the subject of over 60 clinical trials but which was lost for over 30 years due to various merger and acquisition transactions. In over 2000 patients, bisantrene has been well tolerated and shown to lack the cardiac dose-limiting toxicity of the anthracycline class and perhaps to lack a propensity to induce multi-drug resistance. Aside from inhibition of topoisomerase II, macrophage-activating activity and telomerase inhibiting activity have been reported for this agent. Within an extensive body of publications comprising over 40 clinical trials, clinical activity has been documented in a number of indications, including lymphoma, refractory breast cancer, and ovarian cancer. In 7 phase 2 trials, therapeutic utility was seen in acute myeloid leukemia (AML) comparable or superior to drugs currently in development. Although never marketed, bisantrene was approved for the treatment of AML in France in 1991 under the name Zantrene. Originally developed in the 1970s and 1980s, bisantrene is a well-tolerated and useful drug that has resumed clinical development.