Bisantrene (dihydrochloride)

Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1^[1][2][3][4]. IC50 & Target:Topoisomerase^[1] In Vitro: Bisantrene dihydrochloride promots DNase I cleavage at oligopurine-oligopyrimidine tracts and slightly reduces the cleavage activity at alternating purine-pyrimidine sequences^[1].
Bisantrene dihydrochloride is an inhibitor of [³H]uridine incorporation into RNA and [³H]thymidine incorporation into DNA^[2]. In Vivo: Bisantrene dihydrochloride is an antitumor agent active against a number of experimental tumors, including P388 leukemia, L1210 leukemia, Lieberman plasma cell tumor, B16 melanoma, colon tumor 26, and Ridgway osteogenic sarcoma^[3].
Bisantrene dihydrochloride is effective over a dose range of 1.56 to 150 mg/kg depending upon the frequency, route, and schedule of the treatment and the tumor model used^[3].
Bisantrene dihydrochloride (25, 50 and 100 mg/kg; i.p.; once) pretreats with macrophages shows antitumor effect to mice with P815 tumor cells injection^[3].
Bisantrene dihydrochloride (10-150 mg/kg; i.v.; once) dose-dependently induces leukopenia in Neo mice. B cells and macrophages are targets for bisantrene dihydrochloride toxicity^[4].