The US Food and Drug Administration (FDA) recently granted a breakthrough therapy designation to LOXO-292 for the treatment of certain RET-altered cancers. LOXO-292 is indicated for the treatment of patients with RET-mutant medullary thyroid cancer (MTC) who require systemic therapy and progressed after previous treatment, and for refractory patients with metastatic RET–fusion-positive non–small-cell lung cancer (NSCLC) who require systemic therapy and progressed following anti–programmed death ligand 1 (PD-L1) therapy or platinum-based chemotherapy plus anti-PD-1 therapy.
“Multikinase inhibitors have limited activity in RET–fusion-positive and RET-mutant cancers, questioning the therapeutic potential of these targets,” wrote Alexander Drilon, MD, and colleagues in an abstract presented at the American Society of Clinical Oncology 2018 annual meeting. “LOXO-292 selectively targets RET and has preclinical activity against activating RET fusions/mutations, potential resistance mutations, and brain metastases.”
LOXO-292 is a small, highly selective RET inhibitor that has potent action against an ambit of RETalterations. Furthermore, the drug is well tolerated and highly bioavailable, with the ability to cross the blood-brain barrier.
Source: Cancer Network