Development of S-PCT3010 to treat cognitive impairment in Alzheimers Disease

NIH RePORTER · NIH · R44 · $456,633 · view on reporter.nih.gov ↗

Abstract

PolyCore Therapeutics LLC is developing S-PCT3010 as a therapeutic for improved cognitive function in patients suffering from Parkinson’s Disease and is proposing to evaluate S-PCT3010 as a therapeutic for improved cognitive function in Alzheimer’s patients. S-PCT3010 is a selective D3R agonist with biased signaling through the G-protein pathway which does not recruit -arrestin. The drug does not induce tolerance in vitro or in vivo in rats. Further, S- PCT3010 is a selective inhibitor of norepinephrine transporter and promotes improvement in sustaining attention and cognitive flexibility in rodent models of Parkinson’s Disease without producing compulsive or impulsive behaviors. S-PCT3010 is highly pharmaceutically tractable with excellent oral bioavailability and blood brain barrier penetration. In this proposal, PolyCore Therapeutics LLC is proposing to complete pilot studies in a in vivo transgenic mouse model of Alzheimer’s Disease evaluating both behavioral and pathological changes following S-PCT3010 administration. Per the Alzheimer’s Association, an estimated 5.8 million Americans age 65 and older are living with Alzheimer's dementia in 2020 with eighty percent over 75 years old. These numbers represent one in ten people over the age of 65 living with various cognitive impairments. Alzheimer's Disease also represents a significant risk of death and is the sixth- leading cause of death in the United States. The financial burden of Alzheimer's Disease is projected to cost more than $1.1 trillion dollars in 2020, and a significant portion of this cost relates to patient management around cognitive disorders and dementia. In this application, PolyCore Therapeutics LLC teams with leading Parkinson’s and Alzheimer’s researchers at Drexel University to evaluate the changes in cognitive function resulting from Alzheimer’s Disease. The team plans to evaluate S-PCT3010 for use in mitigation of cognitive disorders and memory loss using a transgenic mouse model of Alzheimer’s disease. PolyCore Therapeutics LLC is actively developing S-PCT3010 for Parkinson Disease under an ongoing Phase II SBIR (1R44NS117201-01).

Key facts

NIH application ID
10287800
Project number
3R44NS117201-01S1
Recipient
POLYCORE THERAPEUTICS, LLC
Principal Investigator
Thais Sielecki
Activity code
R44
Funding institute
NIH
Fiscal year
2021
Award amount
$456,633
Award type
3
Project period
2021-03-01 → 2022-02-28