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.) significantly reduces tumor volumes and IgG levels by day 28, showing high tolerability with a 90% survival rate in mice with LAGκ-1A tumors [1]. It demonstrates a favorable safety profile at doses up to 260 mg/mL doxorubicin equivalents, effectively inducing tumor regression in breast cancer, small cell lung cancer, and sarcoma during a phase I study [2]. Additionally, it outperforms doxorubicin in murine renal cell carcinoma and breast carcinoma xenograft models [3].