Small molecule inhibitor of cognitive impairment associated with neurodegenerative disease

This technology is an analog of the retired clinical psychotropic drug minaprine for the treatment of cognitive or behavioral disorders associated with neurodegenerative disorders.

Unmet Need: Treatment for cognitive impairment caused by neurodegenerative diseases

Neurodegenerative diseases are associated with progressive deterioration of brain regions that are essential for cognitive and behavioral functioning. Currently, neurodegenerative diseases lack treatments for neuropsychiatric symptoms, particularly for diseases such as Alzheimer’s disease. Furthermore, current treatments primarily involve the use of atypical antipsychotics and antidepressants, which are associated with side effects that have limited their use. Identifying and developing small molecule inhibitors can assist in treating neurodegenerative diseases specifically by reducing behavioral and cognitive dysfunction and associated neuropsychiatric symptoms such as anxiety and/or depression.

The Technology: Small molecule inhibitor for reduction of neurodegeneration-associated cognitive dysfunction

This technology identifies an analog of the retired clinical psychotropic drug minaprine—without its pharmacogenetic liability—for the treatment of cognitive or behavioral issues stemming from neurodegenerative disorders. The technology enhances serotonin receptor 2B antagonism activity and was shown to reduce behavioral dysfunction and synaptic dysfunction in animal models of Alzheimer’s disease. The technology can address amyloid-beta and tau-induced defects and holds potential in treating neurodegenerative disorders such as Alzheimer’s disease and Parkinson’s disease.

This technology has been validated in mouse models of Alzheimer’s disease.

Applications:

• Treatment for neurodegenerative disorders
• Research platform for analysis of neurodegeneration pathophysiology
• Research tool for the study of serotonin receptor 2B antagonism activity
• Treatment to slow the progression of neurodegeneration and cognitive dysfunction
• Treatment for neuropsychiatric symptoms associated with neurodegenerative disorders
• Research tool for studying synaptic dysfunction in human disease

Advantages:

• Does not have the pharmacogenetic liability of minaprine
• Suppresses long-term potentiation defects
• Suppresses defects in associative and spatial memory, as shown in models of amyloid-beta and tau elevation
• Can be used in combination with other treatments

Lead Inventor:

Ottavio Arancio, M.D., Ph.D.

Patent Information:

Patent Pending (WO/2024/148148)

Related Publications:

• Acquarone E, Argyrousi EK, Arancio O, Watterson DM, Roy SM. “The 5HT2b receptor in Alzheimer’s disease: increased levels in patient brains and antagonist attenuation of amyloid and tau induced dysfunction.” J Alzheimer’s Dis. 2024 Apr 16; 98(4):1349-1360.

Tech Ventures Reference:

• IR CU23096

• Licensing Contact: Jerry Kokoshka