OncoMatch/Clinical Trials/Selpercatinib

Selpercatinib (Retevmo) Clinical Trials

Selpercatinib (Retevmo, LOXO-292) is a highly selective, ATP-competitive RET kinase inhibitor with CNS penetration and activity against a broad spectrum of oncogenic RET alterations. It received FDA approval in 2020 for RET fusion-positive NSCLC, RET-mutant medullary thyroid cancer, and RET fusion-positive thyroid cancer — the first RET-specific inhibitor approved across these indications. The Phase 3 LIBRETTO-431 trial compared selpercatinib to pembrolizumab plus platinum-based chemotherapy (carboplatin and pemetrexed) as first-line therapy in RET fusion-positive NSCLC and demonstrated superior progression-free survival, supporting conversion from accelerated to full FDA approval in that setting. Active trials investigate selpercatinib in combination with checkpoint inhibitors and in RET-altered tumors beyond lung and thyroid. Eligibility requires confirmed RET fusion (NSCLC) or RET activating mutation (medullary thyroid cancer) by an approved assay.