GH2616

GH2616 is a highly potent and selective small molecule inhibitor of KIF18A, a kinesin motor protein involved in chromosome positioning and spindle length regulation during metaphase. It demonstrates robust antitumor activity as monotherapy in several preclinical tumor models, particularly those with TP53 mutations and whole genome doubling (WGD+) or chromosomal instability (CIN). The drug exhibits favorable pharmacokinetic properties, including high oral bioavailability, long half-life for sustained target inhibition, and brain penetration—making it promising for treating brain tumors and metastases. Mechanistically, inhibition of KIF18A disrupts mitotic spindle assembly in WGD+ cancer cells, prolonging mitosis or activating the spindle checkpoint to block cell division at G2/M phase and induce tumor cell death. GH2616 is being developed by Genhouse Bio (Suzhou Genhouse Bio Co., Ltd.)/Qinhao Pharmaceutical (Suzhou) Co., Ltd., with clinical trials ongoing for advanced solid tumors[1][2][3][4][5].