empesertib

Empesertib (BAY1161909) is an orally bioavailable, selective small molecule inhibitor of the serine/threonine monopolar spindle 1 (Mps1/TTK) kinase. It was developed for its potential antineoplastic activity in cancer therapy. By binding to and inhibiting Mps1 kinase—a key regulator of the spindle assembly checkpoint (SAC)—empesertib disrupts proper chromosome alignment and segregation during mitosis. This leads to SAC inactivation, accelerated mitosis, chromosomal misalignment and missegregation, increased aneuploidy, and ultimately cell death in cancer cells that overexpress Mps1. Empesertib showed efficacy as a monotherapy in preclinical models but demonstrated enhanced effects when combined with paclitaxel. The drug reached phase I/II clinical trials for advanced malignancies but development was terminated due to the emergence of more promising candidates[2][3][5][6][7].

Other names

empesertib