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To test the hypothesis that a TAT would be more potent and effective at controlling tumor growth than a beta- emitter, Fusion conducted dose/response studies of intravenously administered [ 225 Ac]-FPI-2059 and [ 177 Lu]- FPI-2057 (previously [ 177 Lu]-IPN01087) in HT29 colorectal cancer xenograft tumor models.[177 LU] -FPI-2057在8325 MBQ/kg的单剂量中有效控制肿瘤生长，但在3885 MBQ/kg时无效。相反，在同一小鼠模型[225 AC] -FPI-2059中显示出≥1.85MBQ/kg的单剂量功效，这表明放射性药物的TAT形式比β-发射器高约1500倍。两种化合物在所有剂量水平上均得到很好的耐受性。
FPI-2059
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