Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.

Aldoxorubicin hydrochloride (0.27 to 2.16 μM) inhibits formation of blood vessel and reduces growth of multiple myeloma cell in a pH-dependent fashion[1].

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