ImClone Systems Corporation, 33 ImClone Drive, Branchburg, NJ 08876, USA.
Cancer. 2010 Feb 15;116(4 Suppl):1013-7. doi: 10.1002/cncr.24787.
FMS-related tyrosine kinase receptor 3 (FLT3) is a class III receptor tyrosine kinase that holds considerable promise as a therapeutic target in hematologic malignancies. Current efforts directed toward the development of small-molecule tyrosine kinase inhibitors of FLT3 may be limited by off-target toxicities and the development of drug resistance. Target-specific antibodies could overcome these hurdles and provide additional mechanisms to enhance the antitumor efficacy of FLT3 inhibitors. IMC-EB10 is a novel antibody directed against FLT3. The binding of IMC-EB10 to FLT3 results in antiproliferative effects in vitro and in mouse models engrafted with human leukemia cells that harbor wild-type or constitutively activated FLT3. Future clinical trials will test these notions formally and will identify the most appropriate opportunities for this member of a new generation of antileukemic therapies.
成纤维细胞生长因子受体相关酪氨酸激酶 3（FLT3）是一种 III 类受体酪氨酸激酶，作为血液系统恶性肿瘤的治疗靶点具有很大的潜力。目前针对 FLT3 的小分子酪氨酸激酶抑制剂的开发可能受到脱靶毒性和耐药性的限制。针对特定靶点的抗体可以克服这些障碍，并提供额外的机制来增强 FLT3 抑制剂的抗肿瘤疗效。IMC-EB10 是一种针对 FLT3 的新型抗体。IMC-EB10 与 FLT3 的结合导致体外增殖效应，并在携带野生型或组成性激活 FLT3 的人白血病细胞移植的小鼠模型中发挥作用。未来的临床试验将正式检验这些观点，并确定这一新代抗白血病治疗药物的最佳应用机会。
