velzatinib

Velzatinib (formerly IDRX-42 or GSK6042981) is an orally bioavailable, potent, and highly selective small molecule inhibitor of the KIT receptor tyrosine kinase. Developed through a collaboration between IDRx and GSK, it is specifically designed to address the limitations of current gastrointestinal stromal tumor (GIST) therapies by targeting both primary KIT mutations (typically in exons 9 and 11) and a broad spectrum of secondary resistance mutations (exons 13, 14, 17, and 18). By inhibiting these diverse KIT variants while sparing closely related kinases like VEGFR2, velzatinib aims to provide deeper and more durable responses in patients with GIST. It is currently being evaluated in Phase 3 clinical trials (StrateGIST-3) as a first-line treatment compared to the standard-of-care imatinib for patients with unresectable or metastatic disease.