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Lead optimization and development of novel targeted small molecule therapeutics for Alzheimers disease

Award Number: R44AG043243
ORGANIZATION: NATIONAL INSTITUTE ON AGING
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 08/15/2012
PERIOD OF PERFORMANCE END DATE: 04/30/2024

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Lead optimization and development of novel targeted small molecule therapeutics for Alzheimers disease - Alzheimer's disease (AD) is a devastating disease, with an insidious onset and relentless progress. It produces distressing changes in memory, thought, perception, and often behavior. These changes increasingly impact the patient's daily life, reducing functional independence, until ultimately, the patients are entirely dependent on others. AD is a progressive disease, where the neurons in the brain gradually degenerate. One of the consequences of this degeneration of the brain is an increased level of cellular waste between the neurons, known as plaques and tangles. As AD progresses, the physical volume of the brain decreases as more and more neurons die. AD is the most common cause of dementia, accounting for up to 80% of all cases. Studies show that as many as 5% of all people above the age of 65 will develop AD. The number of Americans living with AD is growing rapidly. An estimated 5.7 million Americans of all ages have Alzheimer's disease in 2018. Therefore, identification of molecular regulators required to improve cognition, promote cell survival and facilitate neuroprotectants as new therapeutics is essential. Endoplasmic reticulum (ER) protein sigma-1 receptor (S1R) represents a unique chaperone activity in the central nervous system, and it exerts a potent influence on a number of neurotransmitter systems. S1R is distinct from GPCRs and ionotropic receptors and is expressed in neurons in multiple brain regions in post-mortem human brains. S1R plays a modulatory role in biological mechanisms associated with neurodegeneration. S1R ligands activation is known to improve cognition, promote cell survival and facilitate release of the neuroprotectant BDNF. In addition, PET Imaging studies with [11C]SA4503, a specific S1R ligand, have demonstrated that the S1R is widely distributed in normal and AD human brains indicating that our target receptor is present in the disease state. More important is that our proposed target receptor is easily detected in AD brain and our preliminary efficacy data of EPGN644 suggesting that the S1R is a suitable target for novel AD therapies. The research plan presented herein realizes this objective and combines the drug discovery and development expertise of Epigen Biosciences towards commercialization with the in vivo pharmacology expertise of Prof. Dave Morgan and Prof. Kevin Nash’s group at Michigan State University and the University of South Florida, respectively.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2024 ( Subtotal = -$43,433 )
2024	2020	EPIGEN BIOSCIENCES INC	6725 MESA RIDGE RD STE 260	SAN DIEGO	CA	92121	SAN DIEGO	USA	Aging Research	000	4	9/9/2024	NON-COMPETING CONTINUATION	-$43,433
														Subtotal = -$43,433

Issue Date FY: 2023 ( Subtotal = $320,495 )
2023	2020	EPIGEN BIOSCIENCES INC	6725 MESA RIDGE RD	SAN DIEGO	CA	92121	SAN DIEGO	USA	Aging Research	001	4	6/2/2023	NON-COMPETING CONTINUATION	$0
2023	2020	EPIGEN BIOSCIENCES INC	6725 MESA RIDGE RD	SAN DIEGO	CA	92121	SAN DIEGO	USA	Aging Research	000	4	4/7/2023	NON-COMPETING CONTINUATION	$320,495
														Subtotal = $320,495

Issue Date FY: 2022 ( Subtotal = $0 )
2022	2020	EPIGEN BIOSCIENCES INC.	10225 BARNES CANYON RD, STE A104	SAN DIEGO	CA	92121	SAN DIEGO	USA	Aging Research	000	4	4/8/2022	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2020 ( Subtotal = $1,002,264 )
2020	2020	EPIGEN BIOSCIENCES INC.	10225 BARNES CANYON RD, STE A104	SAN DIEGO	CA	92121	SAN DIEGO	USA	Aging Research	001	4	3/23/2020	NON-COMPETING CONTINUATION	$1,002,264
2020	2019	EPIGEN BIOSCIENCES INC.	10225 BARNES CANYON RD, STE A104	SAN DIEGO	CA	92121	SAN DIEGO	USA	Aging Research	000	3	11/15/2019	COMPETING CONTINUATION	$0
														Subtotal = $1,002,264

Issue Date FY: 2019 ( Subtotal = $1,169,102 )
2019	2019	EPIGEN BIOSCIENCES INC.	10225 BARNES CANYON RD, STE A104	SAN DIEGO	CA	92121	SAN DIEGO	USA	Aging Research	000	3	8/9/2019	COMPETING CONTINUATION	$1,169,102
														Subtotal = $1,169,102

Grand Total All Awards = $2,448,428

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Lead optimization and development of novel targeted small molecule therapeutics for Alzheimers disease

Award Number: R44AG043243

ORGANIZATION: NATIONAL INSTITUTE ON AGING

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 08/15/2012

PERIOD OF PERFORMANCE END DATE: 04/30/2024

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