Hydroxytacrine maleate

Hydroxytacrine maleate is a cholinesterase inhibitor and a potential Alzheimer's therapeutic of low toxicity. Exhibits biochemical and pharmacological profile similar to tacrine (THA) except that it is far less toxic and without measurable liver toxicity in humans. Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex. Major form of metabolism is in the liver via hydroxylation of benzylic carbon by CYP450. This forms the major metabolite 1-hydroxy-tacrine (velnacrine) which is still active. Hydroxytacrine maleate is an inhibitor of AChE.