阿伐替尼:一种有前景的胃肠道间质瘤新治疗选择的临床前研究

M. Urbini
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摘要

胃肠道间质瘤(gist)是最常见的胃肠道间质肿瘤(80%),年发病率为每百万人10-15例(1)。由于其分子分类能够预测治疗反应,gist已成为使用分子诊断和靶向治疗的典范。大多数gist是由KIT(70-80%的病例)或PDGFRA(10%)受体酪氨酸激酶激活突变驱动的。这一发现代表了使用小分子酪氨酸激酶抑制剂(TKIs)治疗这种恶性肿瘤的靶向治疗效果的基本原理(1,2)。
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Avapritinib: preclinical studies of a promising novel therapeutic option for gastrointestinal stromal tumors
Gastrointestinal stromal tumors (GISTs) represent the most common mesenchymal tumor of the gastrointestinal tract (80%), with an annual incidence of 10–15 cases per million people (1). GISTs have become a paradigm for the use of molecular diagnostics and targeted therapy, since its molecular classification is able to predict treatment response. Most GISTs are driven by activating mutations in KIT (70–80% of cases) or PDGFRA (10%) receptor tyrosine kinases. This discovery represents the rationale of the efficacy of target therapies efficacy using small molecule tyrosine kinase inhibitors (TKIs) for this malignancy (1,2).
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