EPITRACKER NEURODEGENERATIVE DISEASE & THERAPEUTICS PROGRAM
Alzheimer’s disease, the most common form of dementia, involves neuronal degeneration with progressive loss of cognitive function. An estimated 5.4 million people in the U.S. alone have Alzheimer's disease, and this number is expected to increase to 13.8 million by 2050. Currently, there is no cure for Alzheimer's disease or other forms of dementia. Lack of relevant, long-lived animal patient populations with Alzheimer's disease has hindered the discovery of effective treatments.
Epitracker's neurodegenerative therapeutics program has discovered approximately 60 promising molecules, including ETI-059 and ETI-1004, that aim to target neuroinflammation, the heart of neurodegenerative diseases. We will be advancing these and other neuroprotective assets through Amynta Health, Inc., an Epitracker subsidiary.
Epitracker's neurodegenerative therapeutics program has discovered approximately 60 promising molecules, including ETI-059 and ETI-1004, that aim to target neuroinflammation, the heart of neurodegenerative diseases. We will be advancing these and other neuroprotective assets through Amynta Health, Inc., an Epitracker subsidiary.
A New Hope
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A recent publication from researchers at the University of Oxford concluded that dolphins are one of the very few natural animal species to develop a full suite of brain changes consistent with Alzheimer's disease.
By studying aging-associated neurodegenerative changes in archived dolphin brains and pairing those changes with metabolomic, complex lipid, and genomic profiles, Epitracker is discovering molecules that may aid in early, blood-based detection and treatment of Alzheimer's disease and other forms of dementia. Our neurodegenerative therapeutic compound library includes small molecules that may decrease the following components of Alzheimer's disease and other forms of dementia:
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ETI-059 for Dementias and Multiple Sclerosis
ETI-059 is an optimized small molecule that is demonstrating promise as a novel therapeutic for neurodegenerative diseases. ETI-059 is a partial cannabinoid receptor 1 (CNR1) agonist and potent peroxisome proliferator-activated receptor (PPAR)-alpha agonist.
Aging brains have decreased CNR1 receptor activity, which may result in aging-associated neurodegenerative conditions. Compounds with paired CNR1 and PPAR-alpha agonist mechanisms have the potential to lower neuroinflammation and improve cognitive function, providing an a new and exciting approach to treating Alzheimer's disease and multiple sclerosis.
ETI-059 has demonstrated anti-inflammatory and/or antiproliferative activity across numerous human cell systems mimicking T cell-driven inflammation. ETI-059 significantly reduced proinflammatory chemokines, including interferon-inducible T Cell Alpha Chemoattractant (I-TAC/CXCL11), vascular cell adhesion molecule 1 (VCAM-1/CD106), and monocyte chemoattractant protein (MCP)-1. ETI-059 demonstrated no off-target effects across 78 functional assays at 10 concentrations.
Aging brains have decreased CNR1 receptor activity, which may result in aging-associated neurodegenerative conditions. Compounds with paired CNR1 and PPAR-alpha agonist mechanisms have the potential to lower neuroinflammation and improve cognitive function, providing an a new and exciting approach to treating Alzheimer's disease and multiple sclerosis.
ETI-059 has demonstrated anti-inflammatory and/or antiproliferative activity across numerous human cell systems mimicking T cell-driven inflammation. ETI-059 significantly reduced proinflammatory chemokines, including interferon-inducible T Cell Alpha Chemoattractant (I-TAC/CXCL11), vascular cell adhesion molecule 1 (VCAM-1/CD106), and monocyte chemoattractant protein (MCP)-1. ETI-059 demonstrated no off-target effects across 78 functional assays at 10 concentrations.
ETI-1004 for Alzheimer's Disease
ETI-1004's anti-inflammatory activity involves interruption of the inflammatory cyclooxygenase-prostaglandin E2 (PGE2) pathway. This pathway has been implicated in the preclinical development of Alzheimer's disease.
ETI-1004 has demonstrated anti-inflammatory activity in a human cell system mimicking Th1 type chronic inflammation. ETI-1004 significantly reduced secreted prostaglandin E (PGE)-2 and secreted tumor necrosis factor (TNF)-alpha . ETI-1004 demonstrated no cytotoxicity (using 12 human cell systems at four concentrations).
Interestingly, higher serum levels of ETI-1004 independently predicted lower amyloid-beta plaques and neuroinflammation in our collaborative study using retrospective histological and clinical data from archived dolphin brains and paired lifetime blood samples. Thus, ETI-1004 may be both an early blood-based diagnostic and therapeutic for Alzheimer's disease.
ETI-1004 has demonstrated anti-inflammatory activity in a human cell system mimicking Th1 type chronic inflammation. ETI-1004 significantly reduced secreted prostaglandin E (PGE)-2 and secreted tumor necrosis factor (TNF)-alpha . ETI-1004 demonstrated no cytotoxicity (using 12 human cell systems at four concentrations).
Interestingly, higher serum levels of ETI-1004 independently predicted lower amyloid-beta plaques and neuroinflammation in our collaborative study using retrospective histological and clinical data from archived dolphin brains and paired lifetime blood samples. Thus, ETI-1004 may be both an early blood-based diagnostic and therapeutic for Alzheimer's disease.