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Molecular-Genetic Basis of Gastrointestinal Stromal Tumor Personalized Therapy by Receptor Tyrosine Kinase Inhibitors (A Review)
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2021-07-23 , DOI: 10.1007/s11094-021-02419-8
M. T. Kozinova 1, 2 , N. L. Shimanovsky 1 , G. A. Abalakov 2 , D. V. Sharipova 2
Affiliation  

Studies of the pharmacotherapy of gastro-intestinal stromal tumor as examples of personalized medicine are reviewed. Peculiarities of the use of imatinib, sunitinib, and regorafenib, which inhibit the ATP-biding domain of tyrosine kinase KIT receptor, which largely determines the development of resistance to all three drugs, are considered. Characteristics of the recently approved drugs ripretinib (inhibiting the KIT receptor activation loop, which increases the sensitivity spectrum among various mutations) and avapritinib (inhibitor for PDGFRa mutant tumors) are also discussed. The new drugs together with the well-known three make it possible to offer patients an individual treatment scenario depending on the particular mutation.



中文翻译:

受体酪氨酸激酶抑制剂胃肠道间质瘤个性化治疗的分子遗传学基础(综述)

综述了作为个性化医疗实例的胃肠道间质瘤的药物治疗研究。考虑了伊马替尼、舒尼替尼和瑞戈非尼使用的特殊性,它们抑制酪氨酸激酶 KIT 受体的 ATP 结合域,这在很大程度上决定了对所有三种药物的耐药性的发展。还讨论了最近批准的药物 ripretinib(抑制 KIT 受体激活环,增加了各种突变之间的敏感性谱)和 avapritinib(PDGFRa 突变肿瘤的抑制剂)的特性。新药与众所周知的三种药物一起,可以根据特定的突变为患者提供个性化的治疗方案。

更新日期:2021-07-23
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