Galimberti Daniela, Scarpini Elio
a Neurology Unit, Department of Pathophysiology and Transplantation , University of Milan, Fondazione Cà Granda, IRCCS Ospedale Maggiore Policlinico , Milan , Italy.
Expert Opin Investig Drugs. 2017 Jan;26(1):97-101. doi: 10.1080/13543784.2017.1265504. Epub 2016 Dec 4.
Alzheimer's disease (AD) is the most common cause of dementia in the elderly. Pharmacological treatment of AD includes Anticholinesterase Inhibitors (AChEIs) for mild-moderate AD, and memantine for severe AD. These drugs provide mainly symptomatic short-term benefits without clearly influencing the progression of the disease. Pioglitazone (AD4833) is an insulin sensitizer of the thiazolidinedione class of nuclear Peroxisome-Proliferator Activated Receptor γ (PPARγ) agonists. It binds to PPARγ, affecting gene transcription and reducing inflammation. Areas covered: This review discusses the history of Pioglitazone, its pharmacokinetics and pharmacodynamics profile, and safety issues, together with an overview of clinical trials carried out so far. A literature search was made in Pubmed for pioglitazone, AD, trial, and on the ClinicalTrials.gov site for clinical trials with Pioglitazone. Expert opinion: A Phase II study in AD, and its previous indication for diabetes, showed that Pioglitazone is safe and well tolerated. So far, two large Phase III trials are ongoing, but there are no preliminary results yet on a possible beneficial effect on cognition in patients with AD.
阿尔茨海默病(AD)是老年人痴呆最常见的病因。AD的药物治疗包括用于轻度至中度AD的抗胆碱酯酶抑制剂(AChEIs)以及用于重度AD的美金刚。这些药物主要提供短期的症状缓解,而未对疾病进展产生明显影响。吡格列酮(AD4833)是噻唑烷二酮类核过氧化物酶体增殖物激活受体γ(PPARγ)激动剂中的胰岛素增敏剂。它与PPARγ结合,影响基因转录并减轻炎症。涵盖领域:本综述讨论了吡格列酮的历史、其药代动力学和药效学特征以及安全性问题,同时概述了迄今为止开展的临床试验。在PubMed上检索了吡格列酮、AD、试验等相关文献,并在ClinicalTrials.gov网站上检索了吡格列酮的临床试验。专家观点:一项针对AD的II期研究及其先前用于糖尿病的适应证表明,吡格列酮安全且耐受性良好。目前,两项大型III期试验正在进行中,但尚未有关于其对AD患者认知可能产生有益影响的初步结果。