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b-Galactosidase-responsive prodrugs of chemotherapeutics targeted to cancer surface receptors

In vitro and mouse studies suggest tumor-penetrating, b-galactosidase-responsive prodrugs could help treat cancers. A monomethyl auristatin E (MMAE) prodrug that is activated by the b-galactosidase found inside cells was designed to include a ligand targeting the cancer-specific folate receptor. Cancer cells expressing the folate receptor took up the prodrug and showed cytotoxicity, whereas cells lacking the receptor did not. In mice with folate receptor-expressing tumor xenografts, the MMAE prodrug caused near-complete tumor elimination without weight loss. Next steps include additional preclinical studies of the prodrugs.

SciBX 5(40); doi:10.1038/scibx.2012.1064
Published online Oct. 11, 2012

Patent application filed; available for licensing

Legigan, T. et al. Angew. Chem. Int. Ed.; published online Sept. 20, 2012;
Contact: Sébastien Papot,
University of Poitiers, Poitiers, France