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TC-1 is a novel tertiary carbinamine, potent beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1) inhibitor. It has demonstrated the ability to significantly lower cerebrospinal fluid (CSF) and plasma A beta levels in nonhuman primates. The drug exhibits excellent passive membrane permeability and low susceptibility to P-glycoprotein transport, although it undergoes CYP3A4-mediated metabolism. Co-administration with ritonavir, a CYP3A4 inhibitor, was shown to sustain TC-1 exposure and its A beta-lowering effects. Its primary indication is for Alzheimer's disease, targeting the reduction of neurotoxic A beta 42 peptides.
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