SY-5007 is a novel, ATP-competitive small molecule inhibitor that selectively targets RET.25 In vitro kinase assays demonstrated that SY-5007 exhibits sub-nanomolar inhibitory activity against RET kinases, including both wild-type RET and prevalent mutations associated with resistance to MKIs,26 such as RETM918T (commonly observed in thyroid cancer), RETV804M (a gatekeeper mutation), and RETG810S (a solvent front mutation). The gene discussed is RET; the disease is thyroid cancer.