%0 Journal Article
%T An updated patent review of rearranged during transfection (RET) kinase inhibitors (2016-present).
%A Acharya B
%A Frett B
%J Expert Opin Ther Pat
%V 0
%N 0
%D Oct 2022 5
%M 36198171
%F 6.714
%R 10.1080/13543776.2022.2132851
%X <B>UNASSIGNED: </B>Rearranged during transfection (RET) is a transmembrane receptor tyrosine kinase. Aberrations in RET signaling due to mutations, gene fusions, or overexpression can lead to carcinomas. Six inhibitors have been approved for the treatment of RET-driven cancers: vandetanib, cabozantinib, lenvatinib, sorafenib, selpercatinib, and pralsetinib. Only selpercatinib and pralsetinib have been developed specifically for RET while the remaining are multikinase inhibitors. Several other RET targeted candidates are under clinical development.<BR><B>UNASSIGNED: </B>This review covers recent patent literature describing small molecules that are active against RET from 2016-present.<BR><B>UNASSIGNED: </B>RET represents a major therapeutic target as its alterations occur in nearly 2% of all cancers. Recent approvals for RET targeted therapy have been developed specifically to target the RET oncogene. These approvals represent a paradigm shift from the last decade to now focus on development of selective RET inhibitors rather than multikinase inhibitors. These newly approved RET inhibitors still have clinical issues with drug resistance. It is imperative that the next iteration of RET inhibitors are developed to block common treatment resistant mutations. To accomplish this, RET inhibitors should be developed in concert with genomic profiling to ensure the most relevant clinical mutations are targeted.