TGRX-3544 / Shenzhen TargetRx - LARVOL DELTA

TGRX-3544 is a highly potent and mutant-selective degrader of oncogenic KIT with oral activity (AACR 2025) - "The cellular activity of TGRX-3544 against the E11, E17 and E11/E17 mutants was superior to that of all the currently approved KIT inhibitors imatinib, sunitinib, regorafenib, avapritinib and ripretinib. In summary, we have developed a highly mutant-selective, event-driven, scaffold-eliminating KIT degrader with superior cellular potency and in vivo oral activity. The balanced preclinical profile of TGRX-3544 supports its further clinical investigation in KIT-driven malignancies such as GIST and SM."

Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Oncology • ABL1 • BCR • EGFR • FLT3 • PDGFRA • STAT5