The Novartis RET inhibitor, compound 1, demonstrated robust oral in vivo efficacy in RET-driven tumor xenografts at low doses (10 mpk QD). RET inhibitors (selpercatinib and pralsetinib) have recently been approved in RET+ cancers based on significant efficacy in selected patients. Compound 1 was advanced through preclinical studies [...]
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Dec. 20, 2021
Compound 1: a RET inhibitor
compound 1
oral RET kinase inhibitor effective in tumor xenograft model from scaffold hopping & optimization ACS Medicinal Chemistry Letters Novartis Genomics Institute