Two novel targeted protein degraders (TPD) developed by TargetRx - TGRX-3544, an orally active and highly mutation-selective KIT degrader, and TGRX-3911, a potent BTK degrader - have been selected for poster presentation at the 2025 American Association for Cancer Research (AACR) Annual Meeting based on their preclinical research data.

About TGRX-3544

TGRX-3544 is a highly mutant- selective, event-driven, scaffold-eliminating KIT degrader with superior cellular potency and in vivo oral activity. It potently and selectively induces degradation of KIT E11, E17 and E11/E17 mutants, and moderately the E9 mutant. The preclinical profile supports its further clinical investigation in KIT-driven malignancies such as GIST and SM.

About TGRX-3911

TGRX-3911 is a potent BTK degrader that induces degradation of wildtype (WT), kinase-proficient, kinase-impaired and even compound mutant BTK, prevents activation of the BCR signaling pathway and inhibits proliferation of lymphoma cells. TGRX-3911 has the potential to address clinical resistance to currently available BTK inhibitors.