BC-02

**BC-02** is a preclinical small-molecule mutual prodrug created by covalently linking the aminopeptidase N inhibitor bestatin, also known as ubenimex, to fluorouracil. It was designed for hepatocellular carcinoma, particularly chemoresistant CD13-positive liver cancer stem-cell populations. BC-02 inhibits aminopeptidase N, also called CD13, increases intracellular reactive oxygen species, and promotes ROS-associated DNA damage, thereby suppressing cancer stem-cell self-renewal and tumor-cell proliferation. Preclinical studies reported activity in fluorouracil-resistant liver cancer models and H22 tumor-bearing mice, although poor plasma stability was subsequently identified as a limitation for further development.