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Kozinova MT , Abalakov GA , Sharipova DV , Shimanovsky NL
Molecular-Genetic Basis of Gastrointestinal Stromal Tumor Personalized Therapy by Receptor Tyrosine Kinase Inhibitors (a Review)
Pharmaceutical Chemistry Journal. 2021 Jul;55(4) :315-322
PMID: WOS:000676084300001   
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Abstract
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.
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