glecirasib

Glecirasib is an orally available, small molecule, irreversible allosteric inhibitor of the oncogenic KRAS G12C mutation. Developed by Jacobio Pharmaceuticals, it selectively and covalently binds to the cysteine residue at position 12 of GDP-bound KRAS G12C, locking the protein in its inactive state and thereby blocking downstream oncogenic signaling pathways such as MAPK. This inhibition leads to reduced tumor cell proliferation and increased apoptosis. Glecirasib has demonstrated high selectivity for mutant KRAS G12C over wild-type RAS isoforms and shows potent anti-tumor activity in preclinical models of non-small cell lung cancer (NSCLC), colorectal cancer, pancreatic ductal adenocarcinoma (PDAC), and other solid tumors harboring this mutation. The drug is being evaluated both as monotherapy and in combination with agents like SHP2 inhibitors or cetuximab. It has received orphan drug designation for pancreatic cancer from both the FDA (US) and EMA (Europe), as well as breakthrough therapy designation from Chinese regulatory authorities[1][2][3][4][5].

Brand names

glecirasib

Other names

glecirasib