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Ref Type Journal Article
PMID (27136102)
Authors Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Khochenkov D, Joose JB, Solomko E, Van Akene K, Peretolchina N, Yin W, Ryabaya O, Byakhov M, Tjulandin S
Title Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models.
Abstract Text Alofanib (RPT835) is a novel selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). We showed previously that alofanib could bind to the extracellular domain of FGFR2 and has an inhibitory effect on FGF2-induced phoshphorylation of FRS2α. In the present study, we further showed that alofanib inhibited phosphorylation of FRS2α with the half maximal inhibitory concentration (IC50) values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer), alofanib inhibited FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose dependently inhibited the proliferation and migration of human and mouse endothelial cells (GI50 11-58 nmol/l) compared with brivanib and bevacizumab. Treatment with alofanib ablated experimental FGF-induced angiogenesis in vivo. In a FGFR-driven human tumour xenograft model, oral administration of alofanib was well tolerated and resulted in potent antitumour activity. Importantly, alofanib was effective in FGFR2-expressing models. These results show that alofanib is a potent FGFR2 inhibitor and provide strong rationale for its evaluation in patients with FGFR2-driven cancers.


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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
Alofanib Alofanib 2 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
Alofanib RPT 835|RPT-835|RPT 835|ES000835 FGFR2 Inhibitor 23 Alofanib (RPT835) is a small molecule that binds to the extracellular domain of Fgfr2 and inhibits downstream signaling, potentially resulting in decreased tumor cell proliferation (PMID: 27136102).
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 positive triple-receptor negative breast cancer sensitive Alofanib Preclinical - Cell culture Actionable In a preclinical study, Alofanib (RPT835) treatment led to inhibition of cell proliferation in triple-receptor negative breast cancer cell lines expressing FGFR2 in culture, and inhibited tumor growth in cell line xenograft models (PMID: 27136102). 27136102
FGFR2 positive ovarian cancer predicted - sensitive Alofanib Preclinical - Cell culture Actionable In a preclinical study, Alofanib (RPT835) inhibited growth in an ovarian cancer cell line expressing FGFR2 in culture (PMID: 27136102). 27136102