Although we cannot infer any conclusion about the clinical profile of Sdox, taken together, the in silico, in vitro, and in vivo findings demonstrate that it displays a higher efficacy against Pgp-positive cells, different selectivity towards cancer targets, and a more favorable ADME/toxicity profile than Dox, thus representing a significant advancement in the treatment of Dox-resistant/Pgp-overexpressing tumors. Here, PGP is linked to cancer.