culmerciclib

Culmerciclib (TQB3616) is an orally bioavailable small-molecule inhibitor targeting cyclin-dependent kinases 2, 4, and 6 (CDK2/4/6). Developed by Chia Tai Tianqing Pharmaceutical Group, it is primarily being investigated for the treatment of advanced solid tumors, including hormone receptor-positive (HR+) breast cancer and liposarcoma. By inhibiting CDK4/6, culmerciclib prevents the phosphorylation of the retinoblastoma (Rb) protein, leading to G1 cell cycle arrest and the inhibition of cancer cell proliferation. The additional inhibition of CDK2 is intended to delay or overcome resistance mechanisms that frequently develop against selective CDK4/6 inhibitors, such as the bypass of CDK4/6 via CDK2 activation. Culmerciclib is currently undergoing Phase II clinical evaluation both as a monotherapy and in combination with other agents.

Brand names

Saitanxin

Other names

culmerciclib