MA13.05 TA0953/HM06, a Novel RET-specific Inhibitor Effective in Extracranial and CNS Disease Models of NSCLC with RETfusions

RET kinase fusions act as oncogenic drivers in approximately 2% of NSCLC patients. Two RET-selective inhibitors, selpercatinib and pralsetinib, have proven effective at reducing tumor burden, are FDA-approved. However, the emergence resistance to these drugs, brain metastasis, remain serious clinical challenges. TAS0953/HM06 is a new pharmacologically advanced RET-specific inhibitor that structurally different from other has superior penetration kinetics compared retains activity setting G810 (solvent front) mutations.