sembragiline

Sembragiline is a potent, selective, and reversible small molecule inhibitor of monoamine oxidase type B (MAO-B). Developed by Roche in collaboration with Evotec, it was primarily investigated for the treatment of Alzheimer's disease and smoking cessation. The therapeutic rationale for Alzheimer's disease involves the inhibition of MAO-B to reduce the formation of toxic reactive oxygen species and neuroinflammation, which are associated with the upregulation of MAO-B in reactive astrocytes. While PET imaging confirmed that sembragiline effectively crosses the blood-brain barrier and achieves near-maximal enzyme inhibition at low doses, it failed to meet the primary cognitive endpoints in the Phase II MAyflOwer RoAD study. Consequently, Roche discontinued the development of sembragiline for Alzheimer's disease in 2015.

Other names

sembragilineEVT 302EVT302EVT-302RG1577RG-1577RG 1577RO4602522RO-4602522RO 4602522