pralsetinib

Pralsetinib is an orally administered, selective small molecule inhibitor of the rearranged during transfection (RET) receptor tyrosine kinase. It is used primarily to treat metastatic non-small cell lung cancer (NSCLC) and certain types of thyroid cancer, including medullary thyroid cancer and RET fusion-positive thyroid cancers in adults and children 12 years or older. Pralsetinib works by specifically inhibiting RET kinase activity—including wild-type RET, oncogenic RET fusions, and various activating mutations—thereby blocking downstream signaling pathways that drive tumor cell proliferation. The drug demonstrates high selectivity for RET over other kinases but can also inhibit DDR1, TRKC, FLT3, JAK1/2, TRKA, VEGFR2, PDGFRb, and FGFR1/2 at clinically relevant concentrations. Developed as a targeted therapy with improved safety compared to earlier multi-kinase inhibitors due to its selectivity for RET.

Brand names

Gavreto

Other names

pralsetinib