nkt3447

NKT3447 is an orally bioavailable, highly selective small molecule inhibitor of cyclin-dependent kinase 2 (CDK2), developed by NiKang Therapeutics for the treatment of advanced or metastatic solid tumors characterized by cyclin E amplification or overexpression. The drug binds to inactive monomeric CDK2, disrupting the CDK2/cyclin E complex without affecting CDK1, and suppresses activating phosphorylation of CDK2 on Thr160. This results in substantial downregulation of cyclin E and sustained pharmacodynamic effects, potentially preventing resistance mechanisms seen with other cell cycle inhibitors. Preclinical studies have shown that NKT3447 selectively inhibits proliferation in cancer cells dependent on CDK2 while sparing normal cells. It is currently being evaluated as a single agent in Phase 1 clinical trials for various cancers including ovarian, endometrial, gastric cancers, and other advanced/metastatic solid tumors[2][4][5][6][7].

Other names

NKT-3447NKT3447NKT 3447