Aldoxorubicin has effective antitumor activities in various cancer cell lines and in murine tumor models. Aldoxorubicin is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitors).

Aldoxorubicin (0.27 to 2.16 μM) suppresses blood vessel formation. Aldoxorubicin (0.27 to 2.16 μM) also reduces multiple myeloma cell growth in a pH-dependent fashion.

Aldoxorubicin displays a good safety profile at doses up to 260 mg/mL doxorubicin equivalents and is able to cause tumor regressions in breast cancer, small cell lung cancer, and sarcoma in phase I study[2]. In a murine renal cell carcinoma model and in breast carcinoma xenograft models, Aldoxorubicin also shows superior activity over doxorubicin [3]. On days 28, Aldoxorubicin (10.8 mg/kg, i.v.) displays obviously smaller tumor volumes and IgG levels, and is well tolerated with 90% of mice surviving until the termination of the study in the mice bearing the LAGκ-1A tumor[1].