Findings from a phase I study indicate that the investigational RET inhibitor BLU-667 is safe and well tolerated, inducing good responses in patients with RET-altered medullary thyroid cancer or non-small cell lung cancer.
In first-in-human testing, BLU-667 significantly inhibited RET signaling and induced durable clinical responses in patients with <i>RET</i>-altered NSCLC and MTC without notable off-target toxicity, providing clinical validation for selective RET targeting.<b>Significance:</b> Patients with <i>RET</i>-driven cancers derive limited benefit from available MKIs.
Four genes showed loss-of-expression or reduced mRNA levels in non-small cell lung cancer (CACNA2D2/alpha2delta-2, SEMA3B [formerly SEMA(V), BLU, and HYAL1] or small cell lung cancer (SEMA3B, BLU, and HYAL1) cell lines.