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7171672 
Journal Article 
Orlistat as a FASN inhibitor and multitargeted agent for cancer therapy 
Schcolnik-Cabrera, A; Chavez-Blanco, A; Dominguez-Gomez, G; Taja-Chayeb, L; Morales-Barcenas, R; Trejo-Becerril, C; Perez-Cardenas, E; Gonzalez-Fierro, A; Duenas-Gonzalez, A; , 
2018 
Yes 
Expert Opinion on Investigational Drugs
ISSN: 1354-3784 
TAYLOR & FRANCIS LTD 
ABINGDON 
475-489 
29723075 
WOS:000432689500005 
Introduction: Cancer cells have increased glycolysis and glutaminolysis. Their third feature is increased de novo lipogenesis. As such, fatty acid (FA) synthesis enzymes are over-expressed in cancer and their depletion causes antitumor effects. As fatty acid synthase (FASN) plays a pivotal role in this process, it is an attractive target for cancer therapy.Areas covered: This is a review of the lipogenic phenotype of cancer and how this phenomenon can be exploited for cancer therapy using inhibitors of FASN, with particular emphasis on orlistat as a repurposing drug.Expert opinion: Disease stabilization only has been observed with a highly selective FASN inhibitor used as a single agent in clinical trials. It is too early to say whether the absence of tumor responses other than stabilization results because even full inhibition of FASN is not enough to elicit antitumor responses. The FASN inhibitor orlistat is a dirty' drug with target-off actions upon at least seven targets with a proven role in tumor biology. The development of orlistat formulations suited for its intravenous administration is a step ahead to shed light on the concept that drug promiscuity can or not be a virtue.