The emerging role of FTY720 (Fingolimod) in cancer treatment
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Christopher White1,*, Heba Alshaker2,3,*, Colin Cooper3, Matthias Winkler4 and Dmitri Pchejetski3
1 School of Medicine, Imperial College London, London, UK
2 Department of Pharmacology and Biomedical Sciences, Faculty of Pharmacy and Medical Sciences, University of Petra, Amman, Jordan
3 School of Medicine, University of East Anglia, Norwich, UK
4 Department of Surgery and Cancer, Imperial College London, London, UK
* These authors have contributed equally to this work
Christopher White, email:
Heba Alshaker, email:
Keywords: sphingolipid, sphingosine kinase, fingolimod, FTY720, cancer
Received: August 29, 2015 Accepted: January 19, 2016 Published: February 02, 2016
FTY720 (Fingolimod) is a clinically approved immunomodulating therapy for multiple sclerosis that sequesters T-cells to lymph nodes through functional antagonism of sphingosine-1-phosphate 1 receptor. FTY720 also demonstrates a proven efficacy in multiple in vitro and in vivo cancer models, suggesting a potential therapeutic role in cancer patients. A potential anticancer mechanism of FTY720 is through the inhibition of sphingosine kinase 1, a proto-oncogene with in vitro and clinical cancer association. In addition, FTY720’s anticancer properties may be attributable to actions on several other molecular targets. This study focuses on reviewing the emerging evidence regarding the anticancer properties and molecular targets of FTY720. While the clinical transition of FTY720 is currently limited by its immune suppression effects, studies aiming at FTY720 delivery and release together with identifying its key synergetic combinations and relevant patient subsets may lead to its rapid introduction into the clinic.
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