bezuclastinib

Bezuclastinib is an orally bioavailable, highly selective small molecule inhibitor of mutated forms of the receptor tyrosine kinase KIT, particularly targeting exon 17 mutations such as KIT D816V. These mutations are implicated in diseases like systemic mastocytosis and advanced gastrointestinal stromal tumors (GIST), where aberrant KIT signaling drives disease pathology. By inhibiting mutant KIT activity, bezuclastinib reduces abnormal mast cell proliferation and tumor growth. The drug demonstrates minimal off-target activity against related kinases (such as PDGFRα/β and CSF1R), which may reduce the risk of certain side effects seen with less selective inhibitors. Bezuclastinib is being developed by Cogent Biosciences for indications including advanced systemic mastocytosis and GIST[1][2][3][7].

Other names

1616385-51-3