RET Inhibitor for NSCLC Granted Breakthrough Therapy Designation by FDA
Posted: Monday, September 10, 2018
The U.S. Food and Drug Administration (FDA) recently granted Breakthrough Therapy designation to LOXO-292, a selective RET inhibitor, for the treatment of patients with metastatic RET fusion–positive non–small cell lung cancer (NSCLC) who require systemic therapy and have experienced disease progression after platinum-based chemotherapy and an anti–PD-1 or anti–PD-L1 therapy. This Breakthrough Therapy designation was based on data from the ongoing global phase I/II LIBRETTO-001 clinical trial (ClinicalTrials.gov identifier NCT03157128).
LOXO-292 is an oral and selective investigational new drug in clinical development for the treatment of patients with cancers that harbor abnormalities in the rearranged during transfection (RET) kinase. LOXO-292 was designed to inhibit native RET signaling as well as anticipated acquired resistance mechanisms that could otherwise limit the activity of this therapeutic approach.
Genomic alterations in the RET kinase, which include fusions and activating point mutations, lead to overactive RET signaling and uncontrolled cell growth. RET fusions have been identified in approximately 2% of NSCLCs.
