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Synthesis and Antitumor Efficacy of a β-Glucuronidase-Responsive Albumin-Binding Prodrug of Doxorubicin

2012; American Chemical Society; Volume: 55; Issue: 9 Linguagem: Inglês

10.1021/jm300348r

1520-4804

Thibaut Legigan, Jonathan Clarhaut, Brigitte Renoux, Isabelle Tranoy‐Opalinski, Arnaud Monvoisin, Jean‐Marc Berjeaud, François Guilhot, Sébastien Papot,

Monoclonal and Polyclonal Antibodies Research

In this paper we describe the synthesis and biological evaluation of the first β-glucuronidase-responsive albumin-binding prodrug designed for the selective delivery of doxorubicin at the tumor site. This prodrug leads to superior antitumor efficacy in mice compared to HMR 1826, a well-known glucuronide prodrug of doxorubicin that cannot bind covalently to circulating albumin. Furthermore, this compound inhibits tumor growth in a manner similar to that of doxorubicin while avoiding side effects induced by the free drug.