pro-FTY720

pro-FTY720 (also known as pro-FTY) is an experimental, preclinical small molecule prodrug of fingolimod (FTY720) being developed for the treatment of breast cancer, including multidrug-resistant forms. It utilizes an acrolein-responsive drug delivery system where the prodrug selectively reacts with acrolein—which is highly and specifically expressed in cancer cells—to release active FTY720 locally within the tumor microenvironment. Once released, FTY720 is phosphorylated to FTY720-P, which acts as a functional antagonist of sphingosine-1-phosphate receptor 1 (S1PR1), thereby blocking sphingosine-1-phosphate (S1P) signaling. This tumor-specific activation mechanism is designed to inhibit S1P-mediated cancer cell survival and metastasis while avoiding systemic lymphocytopenia, a major dose-limiting immunosuppressive side effect associated with systemic FTY720 administration. pro-FTY720 has been co-developed by a collaborative research group including Hyogo Medical University, the Institute of Science Tokyo, RIKEN, and Osaka International University.

Other names

pro-FTYprodrug-FTY720prodrug-FTY-720prodrug-FTY 720