Huperzine A is a sesquiterpene alkaloid found in the chemical composition of the medical plant Huperzia serrata. Huperzine A has attracted the attention of neuroscientists after the discovery of its strong and selective inhibitory activity on the acetylcholinesterase enzyme. Preclinical pharmacological studies have indicated that this alkaloid has strong neuroprotective effects against various agents such as ß-amyloid protein, hydrogen peroxide, staurosporine and glutamate, or toxicity induced by ischemia. According to the obtained findings, Huperzine A has multiple action mechanisms due to its acetylcholinesterase inhibitory, neuroprotective and neurogenesis-supporting activities. In vivo studies have suggested that, Huperzine A has significant nootropic activity against cognitive impairments induced by various experimental models. Data from clinical trials have also pointed out that Huperzin A may be an effective agent for the treatment of cognitive disorders caused by senile senescence, Alzheimer’s Disease (AD), cerebrovascular events or psychotic disorders. Apart from the mentioned nootropic efficacy, it has been suggested that Huperzine A has an important potential for the treatments of myasthenia gravis and neonatal hypoxic-ischemic encephalopathy and also for the prophylaxis of organophosphate poisonings. Despite its potent and multidirectional activity potential and safe side-effect profile, Huperzine A is licensed for symptomatic treatment of AD only in the People’s Republic of China. Well-designed clinical trials are needed to confirm the efficacy and the safety of long-term treatment of this agent in order to consider Huperzine A as a potent, safe and low-cost new alternative among the limited number of drugs already used in the treatment of AD