Targeting RET Alterations With Selective Inhibitor BLU-667

Vivek Subbiah, MD, associate medical director, Clinical Center for Targeted Therapy, assistant professor, Department of Investigational Cancer Therapeutics, Division of Cancer Medicine, The University of Texas MD Anderson Cancer Center, discusses targetingRETalterations in solid tumors during the 2018 AACR Annual Meeting.

The next-generation tyrosine kinase inhibitor BLU-667 is a highly potent and selective oral inhibitor that targets oncogenicRETfusions, point mutations, and resistance mutations.RETis a rare driver of multiple, diverse tumor types including more than 60% of medullary thyroid cancers (MTC), about 10% of papillary thyroid tumors, and approximately 1% to 2% of non—small cell lung cancer (NSCLC). There are currently no approved potent therapies to targetRET.

In findings from the open-label, first-in-human, phase I ARROW trial, BLU-667 appeared to be well tolerated and showed clinical benefit in patients with advanced,RET-altered solid tumors who had progressed on prior therapies. Fifty-one patients with unresectable, advanced solid tumors were enrolled on the trial, which included 29 withRET-mutant MTC, 19 with NSCLC withRET