RT Journal Article SR Electronic T1 Fibroblast Growth Factor Receptor Inhibitors as a Cancer Treatment: From a Biologic Rationale to Medical Perspectives JF Cancer Discovery JO CANCER DISCOVERY FD American Association for Cancer Research SP 264 OP 279 DO 10.1158/2159-8290.CD-12-0362 VO 3 IS 3 A1 Dieci, Maria Vittoria A1 Arnedos, Monica A1 Andre, Fabrice A1 Soria, Jean Charles YR 2013 UL http://cancerdiscovery.aacrjournals.org/content/3/3/264.abstract AB The fibroblast growth factor/fibroblast growth factor receptor (FGF/FGFR) signaling pathway plays a fundamental role in many physiologic processes, including embryogenesis, adult tissue homeostasis, and wound healing, by orchestrating angiogenesis. Ligand-independent and ligand-dependent activation have been implicated in a broad range of human malignancies and promote cancer progression in tumors driven by FGF/FGFR oncogenic mutations or amplifications, tumor neoangiogenesis, and targeted treatment resistance, thereby supporting a strong rationale for anti-FGF/FGFR agent development. Efforts are being pursued to develop selective approaches for use against this pathway by optimizing the management of emerging, class-specific toxicity profiles and correctly designing clinical trials to address these different issues. Significance: FGF/FGFR pathway deregulations are increasingly recognized across different human cancers. Understanding the mechanisms at the basis of these alterations and their multiple roles in cancer promotion and drug resistance is a fundamental step for further implementation of targeted therapies and research strategies. Cancer Discov; 3(3); 264–79. ©2012 AACR.