gigaxitinib

Gigaxitinib hydrochloride (ZG19018) is an orally bioavailable, potent, and selective small molecule inhibitor of the KRAS G12C mutation, developed by Suzhou Zelgen Biopharmaceuticals. It functions by irreversibly binding to the cysteine residue at position 12 of the KRAS protein when it is in its inactive, GDP-bound conformation. This covalent modification prevents the exchange of GDP for GTP, effectively trapping KRAS G12C in an inactive state and inhibiting the activation of downstream signaling pathways, such as the RAF-MEK-ERK (MAPK) pathway, which are critical for the growth and survival of KRAS G12C-mutant tumor cells. Gigaxitinib is primarily being investigated for the treatment of advanced solid tumors, including non-small cell lung cancer (NSCLC) and colorectal cancer. In clinical trials, it is being evaluated as a monotherapy and in combination with other therapeutic agents, such as the PD-1/TIGIT bispecific antibody ZG005, to enhance efficacy and address potential resistance mechanisms in patients who have failed prior therapies.

Other names

gigaxitinib hydrochlorideZG19018 hydrochlorideZG-19018 hydrochlorideZG 19018 hydrochloride