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Authors | V.T. Phan, E. Verner, M. Gerritsen, J.M. Bradshaw, D.M. Goldstein, R.J. Hill, D. Karr, J. LaStant, P. Nunn, D. Tam, J. Shu, J.O. Funk, K. Brameld | ||||||||||||
Title | Irreversible Covalent Pan-FGFR Inhibitors are Highly Efficacious Against FGFR-dependent Cancers | ||||||||||||
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URL | http://www.ejcancer.com/article/S0959-8049%2814%2970609-4/pdf | ||||||||||||
Abstract Text | Eu J Cancer Nov 2014 Volume 50, Supplement 6, Page 157 |
Molecular Profile | Treatment Approach |
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Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
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PRN1109 | PRN 1109|PRN-1109 | FGFR Inhibitor (Pan) 26 | PRN1109 is a pan-FGFR inhibitor that blocks FGF/FGFR signaling, leading to anti-tumor activities (Eu J Cancer 2014 Vol 50, Suppl 6:157). | |
PRN1371 | FGFR Inhibitor (Pan) 26 | PRN1371 is an irreversible inhibitor of FGFR1-4 that blocks FGFR signaling, leading to apoptosis and tumor regression in animal models (Eu J Cancer 2014 Vol 50, Suppl 6:157, PMID: 31167419). |
Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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FGFR2 amp | stomach cancer | predicted - sensitive | PRN1109 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, PRN1109 treatment resulted in tumor regression in gastric cancer cell line xenograft models harboring FGFR2 amplification (Eu J Cancer 2014 Vol 50, Suppl 6:157). | detail... |