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A targeted therapy is one that has been developed to affect a specific target, such as an enzyme or receptor. Targeted therapies can either block or increase the function of their target in order to treat a given disease; in this case, cancer.
Smith et al. report the design of ripretinib, an investigational tyrosine kinase inhibitor that forces the activation loop of KIT and PDGFRα into an inactive conformation and targets a broad spectrum of KIT and PDGFRα mutants in GIST.