Mimopezil, A Huperzine A Derivative Undergoing Clinical Development For The Treatment Of Alzheimer's Disease

Mimopezil is a novel cholinesterase inhibitor, non-enzymatically transformed after administration into the active compound Huperzine A. Huperzine A is a quinolizidine alkaloid with potent and selective acetylcholinesterase inhibition properties, originally isolated from a Chinese club moss (Huperzia serrata or Lycopodium serrata). The plant has been used for centuries in China to treat disorders such as memory loss, schizophrenia and hypertension. Huperzine A's pharmacokinetic profile implies a two to four times a day dosing schedule. In the search for huperzine A derivatives adapted to clinical use, mimopezil was selected among over 100 other compounds for its optimal profile in potency, selectivity, and progressive biotransformation into huperzine A. These characteristics allowed to target a once daily oral dosing schedule and to develop an injectable, monthly sustained-release formulation.