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PMID
Authors Peggy A Thompson, Nathan P Young, Craig R Stumpf, Boreth Eam, Vikas K Goel, Joan Chen, Sarah Fish, Gregory S Parker, Adina Gerson-Gurwitz, Maria Barrera, Eric Sung, Jocelyn Staunton, Gary G Chiang, Christopher J Wegerski, Samuel Sperry, Kevin R Webster and Siegfried H Reich
Title eFT226, a first in class inhibitor of eIF4A1, targets FGFR1/2 and HER2 driven cancers
Journal
Vol
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Date
URL https://mct.aacrjournals.org/content/18/12_Supplement/B133
Abstract Text Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133

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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
Drug Name Trade Name Synonyms Drug Classes Drug Description
eFT226 Zotatifin|eFT-226|eFT 226 Zotatifin (eFT226) is an eukaryotic initiation factor 4A1 (eIF4A1) inhibitor that promotes binding of eIF4A1 to the 5'-UTR in a sequence selective manner, which leads to repression of mRNA translation, including translation of the receptor tyrosine kinases FGFR1/2 and ERBB2 (HER2), and potentially results in induction of apoptosis and inhibition of tumor growth (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133, PMID: 32470302).
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 lung non-small cell carcinoma sensitive eFT226 Preclinical - Cell line xenograft Actionable In a preclinical study, eFT226 inhibited tumor growth in a cell line xenograft model of FGFR1-amplified non-small cell lung cancer (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133). detail...
FGFR2 amp colorectal cancer sensitive eFT226 Preclinical - Cell line xenograft Actionable In a preclinical study, eFT226 inhibited cell growth, and induced apoptosis in a FGFR2-amplified colorectal cancer cell line in culture, and inhibited tumor growth, and induced regression in a cell line xenograft model (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133). detail...
ERBB2 amp breast cancer sensitive eFT226 Preclinical - Cell line xenograft Actionable In a preclinical study, eFT226 inhibited cell growth and induced apoptosis in a ERBB2 (HER2)-amplified breast cancer cell line in culture, and induced tumor regression in a cell line xenograft model (Mol Cancer Ther 2019;18(12 Suppl):Abstract nr B133). detail...