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Ref Type
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 Issue Date Pages Journal Short Title
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
Zotatifin Zotatifin 2 1
Drug Name Trade Name Synonyms Drug Classes Drug Description
Zotatifin eFT226|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
FGFR2 amp colorectal cancer sensitive Zotatifin Preclinical - Cell line xenograft Actionable In a preclinical study, Zotatifin (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...
FGFR1 amp lung non-small cell carcinoma sensitive Zotatifin Preclinical - Cell line xenograft Actionable In a preclinical study, Zotatifin (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...