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Alofanib is a first-in-class, small-molecule, allosteric inhibitor of fibroblast growth factor receptor type 2 (FGFR2). It binds to the extracellular domain of FGFR2 and inhibits its activity, thereby blocking basic FGF/FGFR2-related signal transduction pathways. This results in inhibition of FGF-induced endothelial cell proliferation and migration as well as suppression of tumor cell proliferation in FGFR2-overexpressing cancers. Unlike other FGFR inhibitors that act intracellularly, alofanib targets the extracellular region, potentially overcoming resistance due to isoform variation or mutations. Alofanib is being developed primarily for antineoplastic and antiangiogenic indications, with clinical trials focused on metastatic gastric cancer[1][2][3][4][5][6][7][8].
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