Selpercatinib for RET Fusion–Positive Non–Small-Cell Lung Cancer

RET fusions are identified in 1% to 2% of non–small-cell lung cancer (NSCLC) patients. Selpercatinib — an oral, ATP-competitive, small-molecule inhibitor of RET kinase — has central nervous system (CNS) penetrance capability and is able to target RET-activating fusions, point mutations, and certain acquired resistance mutations.

Now, investigators have conducted an industry-funded, international, phase I/II trial (LIBRETTO-001) to test the efficacy and safety of selpercatinib (160 mg twice daily) in 144 patients with RET fusion–positive NSCLC. Of these patients,105 were pretreated with a median 3 lines of systemic therapy (including ≥1 line of platinum-based chemotherapy), and 39 were previously untreated.

Results at a median follow-up of 12.…