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Targeted drug delivery via folate receptors in recurrent ovarian cancer: a review

Authors Marchetti C, Palaia I, Giorgini M, De Medici C, Iadarola R, Vertechy L, Domenici L, Di Donato V, Tomao F, Muzii L, Benedetti Panici P

Received 8 January 2014

Accepted for publication 8 April 2014

Published 10 July 2014 Volume 2014:7 Pages 1223—1236

DOI https://doi.org/10.2147/OTT.S40947

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4


Claudia Marchetti, Innocenza Palaia, Margherita Giorgini, Caterina De Medici, Roberta Iadarola, Laura Vertechy, Lavinia Domenici, Violante Di Donato, Federica Tomao, Ludovico Muzii, Pierluigi Benedetti Panici

Department of Gynecology, Obstetrics and Urological Sciences, Sapienza University of Rome, Rome, Italy

Abstract: Ovarian cancer is the most common cause of gynecological cancer-related mortality, with the majority of women presenting with advanced disease; although chemotherapeutic advances have improved progression-free survival, conventional treatments offer limited results in terms of long-term responses and survival. Research has recently focused on targeted therapies, which represent a new, promising therapeutic approach, aimed to maximize tumor kill and minimize toxicity. Besides antiangiogenetic agents and poly (ADP-ribose) polymerase inhibitors, the folate, with its membrane-bound receptor, is currently one of the most investigated alternatives. In particular, folate receptor (FR) has been shown to be frequently overexpressed on the surface of almost all epithelial ovarian cancers, making this receptor an excellent tumor-associated antigen. There are two basic strategies to targeting FRs with therapeutic intent: the first is based on anti-FR antibody (ie, farletuzumab) and the second is based on folate–chemotherapy conjugates (ie, vintafolide/etarfolatide). Both strategies have been investigated in Phase III clinical trials. The aim of this review is to analyze the research regarding the activity of these promising anti-FR agents in patients affected by ovarian cancer, including anti-FR antibodies and folate–chemotherapy conjugates.

Keywords: ovarian cancer, targeted therapies, folate receptor, antifolate, farletuzumab, vintafolide

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