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BAY 1217389
- Development stage
- Phase 1
- Lead developer
- Bayer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
BAY 1217389 is an orally bioavailable, potent, and highly selective small molecule inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1), also known as TTK. Mps1 is a core component of the spindle assembly checkpoint (SAC), which ensures proper chromosome alignment during mitosis. Inhibition of Mps1 by BAY 1217389 abrogates this checkpoint, driving tumor cells into mitotic catastrophe and cell death due to chromosomal missegregation and aneuploidy. This mechanism offers a novel approach for cancer therapy by targeting proliferating tumor cells with high mitotic activity. Developed by Bayer, BAY 1217389 has been evaluated in phase I clinical trials primarily for advanced solid tumors in combination with paclitaxel[1][5][6][8].
- Other names
- BAY-1217389BAY1217389BAY 1217389CAS 1554458-53-5CAS1554458-53-5CAS-1554458-53-5PD057592PD-057592PD 057592
02
Targets
TTK (TTK protein kinase)
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