Bexarotene, a retinoid X receptor (RXR) agonist, is approved by FDA to treat cutaneous T-cell lymphoma. However, it has also demonstrated promising therapeutic potential for neurological diseases such as stroke, traumatic brain injury, Parkinson’s disease, and particularly Alzheimer's disease(AD). In AD, bexarotene inhibits the production and aggregation of amyloid β (Aβ), activates Liver X Receptor/RXR heterodimers to increase lipidated apolipoprotein E to remove Aβ, mitigates the negative impact of Aβ, regulates neuroinflammation, and ultimately improves cognitive function. For other neurological diseases, its mechanisms of action include inhibiting inflammatory responses, up-regulating microglial phagocytosis, and reducing misfolded protein aggregation, all of which aid in alleviating neurological damage. Here, we briefly discuss the characteristics, applications, and adverse effects of bexarotene, summarize its pharmacological mechanisms and therapeutic results in various neurological diseases, and elaborate on the problems encountered in preclinical research, with the aim of providing help for the further application of bexarotene in central nervous system diseases.

Bexarotene 是一种视黄醇 X 受体 (RXR) 激动剂，经 FDA 批准用于治疗皮肤 T 细胞淋巴瘤。然而，它也显示出对神经系统疾病（如中风、创伤性脑损伤、帕金森病，特别是阿尔茨海默病（AD））的潜在治疗潜力。在AD中，贝沙罗汀抑制β淀粉样蛋白（Aβ）的产生和聚集，激活肝脏X受体/RXR异二聚体以增加脂化载脂蛋白E以去除Aβ，减轻Aβ的负面影响，调节神经炎症，最终改善认知功能。对于其他神经系统疾病，其作用机制包括抑制炎症反应、上调小胶质细胞吞噬作用和减少错误折叠的蛋白质聚集，所有这些都有助于减轻神经损伤。在此，我们简要讨论贝沙罗汀的特点、应用及不良反应，总结其药理机制和对多种神经系统疾病的治疗效果，并详细阐述临床前研究中遇到的问题，旨在为贝沙罗汀的进一步应用提供帮助。在中枢神经系统疾病中。