Selpercatinib for adult patients with locally advanced or metastatic RET-altered solid tumors.

[INTRODUCTION] The rearranged during transfection (RET) mutation is an oncogene driver for the development of cancer. Selpercatinib is a highly selective RET inhibitor that has demonstrated anti-tumor activity in RET-mutated cancers. Selpercatinib is approved for use in RET fusion-positive non-small-cell lung cancer (NSCLC), RET-mutated medullary thyroid cancer, RET fusion-positive thyroid cancer, and RET fusion-positive solid tumors.

[AREAS COVERED] This review summarizes the pharmacology, efficacy, safety, and resistance mechanism of selpercatinib.

[EXPERT OPINION] Selpercatinib has demonstrated durable responses with a favorable safety profile making it an excellent treatment option for RET-mutated cancers. Clinical trials are currently underway to determine the optimal sequencing of selpercatinib in RET fusion-positive lung and RET-mutated medullary thyroid cancer in the first-line setting compared to the current standard of care. Selpercatinib has shown promising anti-tumor activity in various RET-altered solid tumors opening a new treatment option for these patients.