Parkinson's disease (PD) is a prevalent neurodegenerative disorder, which cannot be completely cured by current medications. Abnormal metabolism of dopamine mediates mitochondrial and lysosomal dysfunction, which is one of the important factors in the pathogenesis of PD. Monoamine oxidase B (MAO-B) is a key molecule regulating the dopamine metabolic process and is also an important drug target for the clinical treatment of PD. However, the first/second generation irreversible inhibitors selegiline and rasagiline exhibit poor selectivity and significant side effects, and the third-generation reversible inhibitor safinamide is of poor efficacy with single-agent therapy. Therefore, there is an urgent need to develop highly effective and low-toxic new-generation MAO-B inhibitors for alleviating PD symptoms at all stages of the disease, promoting neuroprotection, and delaying disease progression.

BLT001 is a potent, reversible, highly selective fourth-generation MAO-B inhibitor (ZL202110549040.1; ZL202310991613.5; PCT/CN2023/133138). It has excellent drug metabolism properties and blood-brain barrier permeability, and does not affect the neural functions in the brain. BLT001 has multiple characteristics and multimodal pharmacological mechanisms. It can effectively enhance the motor ability of zebrafish and mouse PD models, alleviate dopaminergic neuron damage, and significantly improve depressive-like, anxiety-like and pain symptoms.

   
Figure. BLT001 is a potent, reversible, and highly selective fourth-generation MAO-B inhibitor, which significantly improve motor disorders, exert neuroprotective effects and alleviate non-motor symptoms.