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胃肠道间质瘤(gastrointestinal stromal tumors,GISTs)是消化道常见的间叶肿瘤,不同于消化道真正的平滑肌瘤、神经源性肿瘤,其发生主要与Kit基因和血小板衍生生长因子受体α(platelet-derived growth factor receptor alpha,PDGFRα)基因突变有关。KIT靶点的发现使得胃肠道间质瘤治疗进入新治疗模式。伊马替尼与舒尼替尼,均为酪氨酸激酶抑制剂,分别被批准为进展期GISTs治疗的第一线及第二线靶向治疗药物。本文就GISTs的分子生物学分型以及分子靶向药物治疗进展作一概述。
Gastrointestinal stromal tumors (GISTs) are common mesenchymal tumors in the digestive tract, which are different from the true leiomyomas and neurogenic tumors in the digestive tract. The occurrence of gastrointestinal stromal tumors is mainly associated with the Kit gene and platelet-derived growth factor receptor α (platelet-derived growth factor receptor alpha, PDGFRα) gene mutation. The discovery of KIT targets has led to a new therapeutic paradigm for gastrointestinal stromal tumors. Imatinib and Sunitinib, both tyrosine kinase inhibitors, were approved as first-line and second-line targeted therapies for the treatment of advanced GISTs. This article summarizes the molecular biology of GISTs and the progress of molecularly targeted drug therapies.