Hydroxytacrine is a bioactive monohydroxylated metabolite of the cholinesterase inhibitor, tacrine , produced by cytochrome P450 1A-catalyzed hydroxylation. While tacrine has been used clinically in the treatment of Alzheimer’s disease, its prolonged use is associated with liver toxicity. Hydroxytacrine demonstrates similar anticholinesterase activity to tacrine, yet has less acute toxicity in both animal and clinical studies of Alzheimer’s disease.
