zeteletinib

Zeteletinib (BOS172738) is a highly potent and selective small molecule inhibitor of the RET (rearranged during transfection) kinase. It was designed to target RET gene alterations—specifically fusions and activating mutations—that drive oncogenesis in several tumor types, including non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), and other solid tumors. Zeteletinib demonstrates nanomolar potency against RET with over 300-fold selectivity versus vascular endothelial growth factor receptor 2 (VEGFR2), aiming to maximize efficacy while minimizing off-target toxicities commonly seen with less selective multi-kinase inhibitors. Clinical studies have shown promising anti-tumor activity in patients with RET-altered cancers, including those with brain metastases. The drug has been generally well tolerated in clinical trials, with most adverse events being mild or moderate and unrelated to the drug[1][4][6][7][8].

Brand names

zeteletinib

Other names

zeteletinib