Abstract
Excitotoxicity contributes to neuronal cell death due to overstimulation of N-methyl-D-aspartate (NMDA) receptors by glutamate, which plays a significant role in the development and progression of Alzheimer’s disease (AD) and other neurodegenerative disorders. Studies have been conducted to identify a well-tolerated and selective NMDA receptor blocker in an effort to alleviate neurodegeneration. Memantine has been found to induce a distinct low-affinity NMDA receptor blockade in both preclinical and clinical studies Therefore, FDA approved this drug as a well-tolerated noncompetitive NMDA receptor blocker for treating moderate to severe cases of AD. Further, memantine showed neuroprotective effects in preclinical studies by selectively blocking excessive NMDA receptor activation. Altogether, this novel drug is well-tolerated and effective for treating moderate to severe AD in various clinical studies. This paper is a review of preclinical and clinical studies on the drug development process of memantine.
 Keywords: Memantine, Excitotoxicity, N-methyl-D-aspartate, Glutamate, Alzheimer’s disease, neurodegeneration
Highlights
The number of patients with Alzheimer’s disease (AD) has been estimated to reach more than 13.5 millions by 2050 in the United States [1]
The exact molecular mechanisms underlying the interaction of memantine with NMDA receptors still need to be studied more to improve the efficacy and outcomes of this treatment strategy in the management of AD
Clinical studies have demonstrated that memantine is effective for treating AD, it is not a cure
Summary
The number of patients with Alzheimer’s disease (AD) has been estimated to reach more than 13.5 millions by 2050 in the United States [1]. Excitotoxicity contributes to neuronal cell death, which plays a significant role in the development and progression of AD and other neurodegenerative disorders. Excitotoxic neuronal cell death and injury occur primarily due to the overstimulation of N-methyl-D-aspartate (NMDA) receptors by glutamate, which is the primary excitatory amino acid transmitter in the mammalian brain [3]. Studies have been conducted to identify selective NMDA receptor blockers as neuroprotective agents to treat neurodegenerative disorders. Memantine induced a distinct lowaffinity NMDA receptor blockade in both preclinical and clinical studies. Althobaiti memantine was approved by FDA as a welltolerated noncompetitive NMDA receptor blocker for treating moderate to severe AD [5]. The aim of this report was to review memantine drug development in preclinical and clinical studies
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