tegtociclib

PF-07104091 (tegtociclib) is an orally bioavailable, first-in-class, selective small molecule inhibitor of cyclin-dependent kinase 2 (CDK2), developed by Pfizer. It is designed to target the cell cycle machinery in cancers where CDK2 activity drives proliferation or resistance to existing therapies. Specifically, CDK2 inhibition is intended to overcome resistance to CDK4/6 inhibitors in hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer and to provide a therapeutic option for CCNE1-amplified tumors, such as certain ovarian and lung cancers. By selectively binding to CDK2, PF-07104091 prevents the phosphorylation of the retinoblastoma protein (RB1), thereby inducing G1 phase cell cycle arrest and inhibiting tumor growth. It is currently being investigated in Phase 1/2 clinical trials both as a monotherapy and in combination with other agents, including the CDK4-selective inhibitor atirmociclib (PF-07220060) and endocrine therapies.

Other names

tegtociclibTagtociclib