BAY1161909 + paclitaxel

**BAY1161909 + paclitaxel** is an investigational **combination therapy** designed for the treatment of advanced malignancies. BAY1161909 (empesertib) is an orally bioavailable, highly selective inhibitor of monopolar spindle 1 (Mps1, also known as TTK) kinase—a serine/threonine kinase critical for the spindle assembly checkpoint (SAC). Mps1 helps ensure proper chromosome segregation during cell division. In cancers, particularly those with overexpressed Mps1 (such as certain lung and breast cancers), inhibiting Mps1 impairs the SAC, leading to chromosomal instability, failed mitotic arrest, and cell death[1][2][3][4][5]. Paclitaxel, a well-established chemotherapy agent, stabilizes microtubules and induces mitotic arrest. The rationale for the combination is that Mps1 inhibition (by BAY1161909) disables the mitotic checkpoint, rendering tumor cells more susceptible to paclitaxel-induced cytotoxicity. This synergistic effect is particularly promising for tumors resistant to paclitaxel alone[5]. The combination was evaluated in a Phase 1 clinical trial for safety, tolerability, pharmacokinetics, and determining recommended dosing[1][3][4][5].

Other names

empesertib + paclitaxel