Research Status, Synthesis and Clinical Application of Recently
Marketed and Clinical BCR-ABL Inhibitors

doi:10.2174/0929867328666211012093423
摘要

BCR-ABL融合基因表达的酪氨酸激酶可引起细胞增殖、粘附和存活特性的变化，这是慢性粒细胞白血病（CML）的主要原因。抑制BCR-ABL酪氨酸激酶的活性已成为治疗慢性骨髓性白血病的有效方法之一。最初，伊马替尼是BCR-ABL酪氨酸激酶抑制剂（TKI）的第一个小分子，用于有效治疗慢性骨髓性白血病。后来，由于各种BCR-ABL突变的出现，特别是T315I突变，伊马替尼产生了强烈的抗药性。第二代激酶抑制剂达沙替尼和尼洛替尼能够克服大部分突变耐药性，但不能克服T315I突变。因此，为了进一步克服耐药性问题，开发了新型KTI，如氟马蒂尼和拉替尼，为临床治疗提供了更多的选择。一些新药已进入临床试验。近年来，临床市场引进了2种新的BCRABL抑制剂（氟马替尼和拉替尼）和5种新的BCR-ABL抑制剂。我们回顾了他们的研究现状，合成方法和临床应用。
关键词: 慢性骨髓性白血病（CML），BCR-ABL，酪氨酸激酶抑制剂（TKI），研究现状，合成，临床应用。
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当代药物化学

近期上市和临床BCR-ABL抑制剂的研究现状、合成及临床应用

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当代药物化学

近期上市和临床BCR-ABL抑制剂的研究现状、合成及临床应用

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