Sabbagh Marwan N, Shill Holly A
Banner Sun Health Research Institute, The Cleo Roberts Center for Clinical Research, 10515 West Santa Fe Drive, Sun City, AZ 85351, USA.
Curr Opin Investig Drugs. 2010 Jan;11(1):80-91.
Latrepirdine (Dimebon) is a small-molecule compound under development by Medivation Inc and Pfizer Inc for the treatment of Alzheimer's disease and Huntington's chorea. Originally developed and marketed as an antihistamine in Russia, latrepirdine has since demonstrated potential for the treatment of neurodegenerative diseases. Early research suggested that the mechanism of action was centered on AChE inhibition and NMDA antagonism. More recent research questions these early findings, and other mechanisms of action have been proposed and investigated. In phase II clinical trials, latrepirdine demonstrated clinically relevant improvements in patients with Alzheimer's disease and Huntington's chorea. At the time of publication, phase III clinical trials had been initiated. Given the robustness of the phase II clinical data, latrepirdine has a high likelihood of success in phase III trials and in subsequently being granted regulatory approval.
拉曲匹定(二甲金刚胺)是Medivation公司和辉瑞公司正在研发用于治疗阿尔茨海默病和亨廷顿舞蹈症的一种小分子化合物。拉曲匹定最初在俄罗斯研发并作为抗组胺药上市,后来已显示出治疗神经退行性疾病的潜力。早期研究表明其作用机制集中在抑制乙酰胆碱酯酶和拮抗N-甲基-D-天冬氨酸。最近的研究对这些早期发现提出质疑,并提出和研究了其他作用机制。在II期临床试验中,拉曲匹定在阿尔茨海默病和亨廷顿舞蹈症患者中显示出具有临床意义的改善。在发表本文时,III期临床试验已经启动。鉴于II期临床数据的稳健性,拉曲匹定在III期试验中取得成功并随后获得监管批准的可能性很大。