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Ref Type Journal Article
PMID (27535969)
Authors Watanabe Miyano S, Yamamoto Y, Kodama K, Miyajima Y, Mikamoto M, Nakagawa T, Kuramochi H, Funasaka S, Nagao S, Sugi NH, Okamoto K, Minoshima Y, Nakatani Y, Karoji Y, Ohashi I, Yamane Y, Okada T, Matsushima T, Matsui J, Iwata M, Uenaka T, Tsuruoka A
Title E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical Models.
Journal Molecular cancer therapeutics
Vol 15
Issue 11
Date 2016 Nov
URL
Abstract Text The FGFR signaling pathway has a crucial role in proliferation, survival, and migration of cancer cells, tumor angiogenesis, and drug resistance. FGFR genetic abnormalities, such as gene fusion, mutation, and amplification, have been implicated in several types of cancer. Therefore, FGFRs are considered potential targets for cancer therapy. E7090 is an orally available and selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses of the interaction between E7090 and FGFR1 tyrosine kinase, E7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. E7090 showed selective antiproliferative activity against cancer cell lines harboring FGFR genetic abnormalities and decreased tumor size in a mouse xenograft model using cell lines with dysregulated FGFR Furthermore, E7090 administration significantly prolonged the survival of mice with metastasized tumors in the lung. Our results suggest that E7090 is a promising candidate as a therapeutic agent for the treatment of tumors harboring FGFR genetic abnormalities. It is currently being investigated in a phase I clinical trial. Mol Cancer Ther; 15(11); 2630-9. ©2016 AACR.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
E7090 E7090 11 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
E7090 E-7090 FGFR1 Inhibitor 23 FGFR2 Inhibitor 16 FGFR3 Inhibitor 13 E7090 is a selective inhibitor of FGFR1, FGFR2, and FGFR3, which may result in inhibition of cell proliferation and antitumor activity (PMID: 27535969).
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
FGFR1 amp FGFR2 amp breast cancer sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line, harboring FGFR1 amplification and FGFR2 amplification, treated with E7090 demonstrated decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR1 amp lung small cell carcinoma sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, a small cell lung cancer cell line harboring FGFR1 amplification demonstrated sensitivity to E7090, resulting in decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR2 amp stomach cancer sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a gastric cancer cell line harboring FGFR2 amplification demonstrated decreased cell viability in culture and antitumor activity in xenograft models when treated with E7090 (PMID: 27535969). 27535969
FGFR2 S252W endometrial cancer sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, an endometrial cancer cell line harboring FGFR2 S252W (PMID: 18552176) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 18552176 27535969
FGFR1 amp lung non-small cell carcinoma sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, a non-small cell lung cancer cell line, harboring FGFR1 amplification, treated with E7090 demonstrated decreased cell viability in culture and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR1 amp estrogen-receptor positive breast cancer sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line harboring FGFR1 amplification (PMID: 7506125) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 7506125 27535969
FGFR3 - TACC3 urinary bladder cancer sensitive E7090 Preclinical - Cell line xenograft Actionable In a preclinical study, urinary bladder cancer cells harboring FGFR3-TACC3 demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability, and antitumor activity in xenograft models (PMID: 27535969). 27535969
FGFR3 Y373C multiple myeloma sensitive E7090 Preclinical - Cell culture Actionable In a preclinical study, a multiple myeloma cell line harboring FGFR3 Y373C (PMID: 19901323) demonstrated sensitivity to E7090 in culture, resulting in decreased cell viability (PMID: 27535969). 19901323 27535969
FGFR2 pos FGFR3 pos breast carcinoma sensitive E7090 Preclinical Actionable In a preclinical study, a mouse breast carcinoma cell line xenograft model demonstrated inhibition of tumor growth when treated with E7090, a result of decreased FGFR2 and FGFR3 activity (PMID: 27535969). 27535969