| 曹雅婷,毕世杰,朱昊滨,等.FLT3抑制剂耐药机制及新型FLT3抑制剂开发策略研究进展[J].中国海洋药物,2025,44(5):77-86. |
| FLT3抑制剂耐药机制及新型FLT3抑制剂开发策略研究进展 |
| Research progress on resistance mechanism and coping strategies of FLT3 inhibitors |
| 投稿时间：2025-05-26 修订日期：2025-09-01 |
| DOI：10.13400/j.cnki.cjmd.2025.05.001 |
| 中文关键词: 急性髓性白血病、FLT3-ITD突变、FLT3抑制剂、耐药机制 |
| English Keywords:Acute myeloid leukemia, FLT3-ITD mutation, FLT3 inhibitor, Resistance mechanism |
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| 中文摘要: |
| FLT3-ITD突变是急性急性髓系白血病(AML)发展的关键驱动性突变,与不良与后年有关。FLT3抑制剂可显著抑制FLT3-ITD突变AML细胞增殖,但易产生二次耐药(FLT3-ITD-TKD)突变,导致FLT3抑制剂临床失效,为AML的治疗带来极大的挑战。本文综述了FLT3抑制剂的研究进展、耐药机制及应对策略、克服FLT3-ITD 二次耐药新型抑制剂的开发策略。 |
| English Summary: |
| The FLT3-ITD mutation is a critical driver mutation in the pathogenesis of acute myeloid leukemia (AML) and is associated with a poor prognosis. FLT3 inhibitors have demonstrated significant efficacy in inhibiting the proliferation of AML cells harboring the FLT3-ITD mutation; however, these therapies are often compromised by the emergence of secondary resistance mutations, specifically FLT3-ITD-TKD mutations. This phenomenon leads to clinical failure of FLT3 inhibitors and presents substantial challenges in the management of AML. This article reviews recent advancements in research on FLT3 inhibitors, elucidates their mechanisms of resistance and potential coping strategies, as well as explores developmental approaches for novel inhibitors aimed at overcoming secondary resistance to FLT3-ITD. |
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