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Alzheimer’s Disease

The Need

Alzheimer’s disease (AD) is a debilitating neurodegenerative disease with significant opportunity for superior therapies. There are currently 5.3 million people in the United States and more than half a million in Canada living with AD. In Canada, 1 in 11 adults over the age of 65 are inflicted with AD. As AD is primarily found in this segment of the population, the incidence rate for AD is expected to increase rapidly in the coming years as the “baby boomers” begin to turn 65 in 2011.

There are currently only two classes of drugs approved by the FDA for AD and both are symptomatic therapies: Acetylcholinesterase Inhibitors and N-Methyl-D-Aspartate Receptor Antagonists. The approved treatments for AD that currently dominate the market have not produced results that consistently meet the requirements of healthcare professionals and patients. According to Decision Resources, going forward several new therapies will enter the AD market, including those with the potential for disease modification, which may be used in combination with current therapies which will nearly triple the AD market despite the genericization of currently available agents.

Our Solution

In July 2009 COTI completed the discovery, optimization, and final selection of its library of novel, lead compounds for the oral treatment of Alzheimer’s Disease.

The COTI scientific team has focused their research efforts on the area of secretases, a class of enzymes that cut the amyloid precursor protein into three fragments. Sequential cutting by beta secretase and gamma secretase produces the beta amyloid peptide fragments that accumulate into the "plaques" or scars found in the brains of people with AD. These inhibitors target both beta and gamma secreatases.

COTI’s novel, optimized lead compounds targeted against AD have already undergone extensive computational and human medicinal chemistry optimization, a chemical synthetic feasibility review and an intellectual property assessment. The first six dual secretase inhibitors on three different scaffolds are now ready for synthesis and preclinical evaluation. COTI is actively seeking partners to co-develop this exciting new program.



Development Status



  Select a therapeutic target


  Identify novel validated cellular target(s)


  Design a candidate molecule library


  Profile/Optimize the candidates using in silico + traditional medicinal chemistry methods


  Conduct a patent search on most promising candidates


Synthesize the most
promising candidates
a. The Alzheimer's Disease library of lead compounds is ready to be synthesized.


  Test and develop in vitro / in vivo to confirm the computational predictions


  Patent the most promising candidates


  License successful candidates
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