EVT-301

EVT-301 is a small molecule, reversible inhibitor of monoamine oxidase type B (MAO-B) that was developed by Evotec for the treatment of Alzheimer's disease. The therapeutic rationale for using MAO-B inhibitors in Alzheimer's involves the reduction of oxidative stress and the modulation of neurotransmitter levels, particularly dopamine, which may be depleted or dysregulated in the disease. Clinical studies, including PET imaging, demonstrated that EVT-301 achieves high, dose-dependent occupancy of the MAO-B enzyme in the human brain, with occupancy levels reaching up to 90% at a 150 mg dose. Although Phase 1 data suggested the compound was well-tolerated and achieved target engagement suitable for further clinical development, the program was ultimately discontinued.