bezuclastinib + sunitinib

Bezuclastinib + sunitinib is a combination of two small-molecule tyrosine kinase inhibitors under investigation for the treatment of gastrointestinal stromal tumors (GIST), particularly in patients who have progressed on or are intolerant to imatinib. Bezuclastinib is a selective type I TKI that targets KIT mutations, especially those in exons 17 and 18 associated with resistance to other therapies. Sunitinib is an approved multi-targeted TKI that inhibits several receptor tyrosine kinases including KIT (exons 9, 11, 13, and 14), PDGF receptors (PDGFRα/β), VEGF receptors (VEGFR1-3), FLT3, CSF-1R, and RET. The combination aims to provide broader inhibition across primary and secondary KIT mutations responsible for GIST progression after first-line therapy. Clinical studies have shown improved efficacy and tolerability compared to sunitinib alone[1][2][5][7].

Brand names

Sutent

Other names

CGT9486 plus sunitinibCGT-9486 plus sunitinibCGT 9486 plus sunitinibbezuclastinib plus sunitinib