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Such an approach as molecular repurposing allows \u201cgiving a second life\u201d to available drugs by targeting them to new biotargets and testing them in various combinations. When developing new therapeutic strategies, it is important to consider the unique characteristics of different cancer tissues. Tumors of different organs may have different molecular profiles, and effective treatment should be directed exactly at targets specific to these tissues. This literature review is devoted to analyzing the current state of the pharmacological niche of protein kinase inhibitors, synthesis methods and the mechanism of action of existing approved drugs\u2014inhibitors of major protein kinases. In addition, in this review we highlight modern approaches to modeling 3D tissue\u2010specific organoids (tumoroids) used for testing anticancer agents, which are currently considered a promising platform for screening protein kinase inhibitors. 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