FLT3 Inhibition in Acute Myeloid Leukaemia – Current Knowledge and Future Prospects

doi:10.2174/1570163817666200518075820
摘要

30%的急性髓系白血病(AML)患者在诊断时出现FMS样酪氨酸激酶3 (FLT3)的激活突变，并带来不良的临床预后。突变的FLT3已经成为一个可行的治疗靶点，在过去的10~15年里，许多FLT3导向的酪氨酸激酶抑制剂已经通过临床开发取得进展。过去两年里，美国食品和药物管理局(FDA)批准的多激酶抑制剂米哚妥林用于最近确诊的FLT3突变患者，与强化化疗联合使用，以及与FLT3选择性更强的gilteritinib药物单药治疗复发或难治性FLT3突变AML患者。“第二代”药物奎扎替尼和crenolanib也处于临床开发的晚期。在协商各种潜在的获得性耐药机制和优化现有及新治疗方法在不同临床环境下的FLT3抑制药物的测序，包括一线治疗、复发/难治性疾病和维持治疗，仍面临重大挑战。本文综述了FLT3的生物学、FLT3突变的AML带来的临床挑战、关键FLT3抑制化合物的发展历史、抗病机制，以及这类药物的未来展望，包括目前和计划中的临床试验。C
关键词: 急性髓系白血病(AML)， FLT3抑制剂，米哚妥林
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图形摘要

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DOI https://dx.doi.org/10.2174/1570163817666200518075820	Print ISSN 1568-0096
Publisher Name Bentham Science Publisher	Online ISSN 1873-5576
当代肿瘤药物靶点

FLT3抑制急性髓系白血病的研究现状和未来展望

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当代肿瘤药物靶点

FLT3抑制急性髓系白血病的研究现状和未来展望

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