Selpercatinib: A narrative drug review

Abstract

Rearranged during transfection (RET) alteration promotes oncogenesis in a few cancers. RET mutation positivity is seen in approximately 70% of medullary thyroid cancers, around 30% of differentiated papillary thyroid cancers, and 1-2% of non-small-cell lung cancers (NSCLC). To write this narrative drug review, we searched various websites like the United States Food and Drug Administration, PubMed, Google Scholar, UpToDate, and recently published papers in various international conferences using the search terms “RET,” “RET alteration,” “Retevmo,” “RET inhibitors,” and “selpercatinib.” We shortlisted 31 articles published between January 1980 and January 2024. We discuss the history, mechanism of action, resistance, pharmacodynamics, pharmacokinetics, dosing, toxicity, pivotal trials, and indications of selpercatinib. Selective RET inhibitors like selpercatinib are indicated in the treatment of RET-altered NSCLC and thyroid cancer.