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CTS-21166 is a small-molecule, orally bioavailable beta-secretase (BACE1) inhibitor developed as a potential disease-modifying treatment for Alzheimer's disease. It acts by selectively inhibiting beta-secretase, an enzyme critical in the production of amyloid-beta peptides implicated in the pathogenesis of Alzheimer's disease. Preclinical and clinical studies have shown that CTS-21166 can cross the blood-brain barrier, has high selectivity and metabolic stability, and demonstrates excellent pharmacokinetic properties. In Phase I clinical trials, it produced rapid and significant reductions in plasma amyloid-beta levels with good safety and tolerability profiles. The drug was originally discovered by Dr. Jordan Tang at Oklahoma Medical Research Foundation and further developed by CoMentis[1][3][6][8].
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