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Ref Type Journal Article
PMID (26078430)
Authors Touat M, Ileana E, Postel-Vinay S, André F, Soria JC
Title Targeting FGFR Signaling in Cancer.
URL
Abstract Text The fibroblast growth factor signaling pathway (FGFR signaling) is an evolutionary conserved signaling cascade that regulates several basic biologic processes, including tissue development, angiogenesis, and tissue regeneration. Substantial evidence indicates that aberrant FGFR signaling is involved in the pathogenesis of cancer. Recent developments of deep sequencing technologies have allowed the discovery of frequent molecular alterations in components of FGFR signaling among several solid tumor types. Moreover, compelling preclinical models have demonstrated the oncogenic potential of these aberrations in driving tumor growth, promoting angiogenesis, and conferring resistance mechanisms to anticancer therapies. Recently, the field of FGFR targeting has exponentially progressed thanks to the development of novel agents inhibiting FGFs or FGFRs, which had manageable safety profiles in early-phase trials. Promising treatment efficacy has been observed in different types of malignancies, particularly in tumors harboring aberrant FGFR signaling, thus offering novel therapeutic opportunities in the era of precision medicine. The most exciting challenges now focus on selecting patients who are most likely to benefit from these agents, increasing the efficacy of therapies with the development of novel potent compounds and combination strategies, and overcoming toxicities associated with FGFR inhibitors. After examination of the basic and translational research studies that validated the oncogenic potential of aberrant FGFR signaling, this review focuses on recent data from clinical trials evaluating FGFR targeting therapies and discusses the challenges and perspectives for the development of these agents.

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Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
GSK3052230 GSK3052230 4 1
MGFR1877S MGFR1877S 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
GSK3052230 FP-1039|HGS1036|GSK-3052230|GSK 3052230 GSK3052230 (FP-1039) is an FGF ligand trap which prevents FGF1, FGF2, and FGF4 from binding corresponding receptors thereby preventing downstream signaling and activation (PMID: 26078430, PMID: 31065954, PMID: 31446228).
MGFR1877S RG744 FGFR3 Antibody 4 MGFR1877S is a monoclonal antibody selective for Fgfr3, which induces antitumor activity (PMID: 26078430).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References