Clinical translation of folate receptor-targeted therapeutics

Abstract

Each of the two strategies has advantages and disadvantages. Identification of the best target patient population is likely critical to the ultimate success of FR-targeted agents in the clinic. A successful clinical strategy may require the integration between FR expression analysis and an optimal combination of FR-targeted therapy and standard chemotherapy. Advancement into Phase III trials and the ongoing clinical development of several additional folate conjugates are likely to usher in a new era of clinical translation and validation of FR-targeted imaging and therapeutic agents.

177Lu-Dendrimer Conjugated to Folate and Bombesin with Gold Nanoparticles in the Dendritic Cavity: A Potential Theranostic Radiopharmaceutical

“…Folate is a basic component of cell metabolism and DNA synthesis and repair. Cancer cells, which rapidly divide, have an increased requirement for folate to maintain DNA synthesis, an observation supported by the widespread use of antifolates in cancer chemotherapy [14,15].…”

Vintafolide: a novel targeted therapy for the treatment of folate receptor expressing tumors

“…Farletuzumab is a fully humanized antibody derived from the murine antibody LK26, which binds FRα to promote cell lysis by both complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity [Farrell et al 2012;Jelovac and Armstrong, 2012;Teng et al 2012]. In addition, the binding of farletuzumab to FRα also suppresses the proliferation and growth of FRα-expressing cells and tumors by preventing the phosphorylation of substrates specific for Lyn kinase [Jelovac and Armstrong, 2012].…”

Imaging the Folate Receptor on Cancer Cells with 99mTc-Etarfolatide: Properties, Clinical Use, and Future Potential of Folate Receptor Imaging

“…99m Tc-etarfolatide takes advantage of the more optimal SPECT imaging characteristics of technetium (half-life of 6 h and 140-keV photon) and has been evaluated in several clinical trials (1,3,11,13,16).…”

“…Folate is a water-soluble B vitamin that is essential for cellular processes such as nucleotide biosynthesis (1). Cellular folate transport can be mediated by folate receptors (FRs), of which the a and b subtypes are the most studied (2).…”