过氧化物酶体增殖因子激活受体调节对非酒精性脂肪肝和非酒精性脂性肝炎的治疗潜力

L. Gellrich, D. Merk
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引用次数: 9

摘要

代谢综合征是一种长期被忽视的肝脏表现,非酒精性脂肪性肝病(NAFLD)和非酒精性脂性肝炎(NASH)是一种严重的健康负担,其全球发病率令人担忧。该疾病复合体目前吸引了人们对药物发现的极大兴趣,在临床开发的各个阶段都研究了许多实验方法。过氧化物酶体增殖物激活受体(PPARs)作为药物靶点在治疗代谢综合征的几个方面有着成功的历史,因此,PPARs调节剂在NAFLD/NASH中的治疗价值是显而易见的。然而,到目前为止,只有PPARα/δ激动剂依非布拉诺显示出明确的疗效并达到了晚期发展阶段,而更成熟的PPAR亚型PPARα和PPARγ则令人失望。尽管如此,临床试验设计和人群可能掩盖了有益的活性,此外,协同多靶点方法和选择性PPAR调节剂可以产生更安全、更高疗效的方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Therapeutic Potential of Peroxisome Proliferator-Activated Receptor Modulation in Non-Alcoholic Fatty Liver Disease and Non-Alcoholic Steatohepatitis
A long neglected hepatic manifestation of the metabolic syndrome, non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) arise as serious health burden with alarming global prevalence. The disease complex is currently attracting considerable interest of drug discovery and many experimental approaches are studied in all stages of clinical development. Peroxisome proliferator-activated receptors (PPARs) have a successful history as pharmaceutical targets in the treatment of several aspects of the metabolic syndrome and, therefore, a putative therapeutic value of PPAR modulators in NAFLD/NASH is obvious. However, so far only the PPARα/δ agonist elafibranor has revealed clear efficacy and reached an advanced stage of development while the far more established PPAR subtypes PPARα and PPARγ have disappointed. Still, clinical trial design and population might have obscured beneficial activities and, in addition, synergistic multi-target approaches as well as selective PPAR modulators could generate safer approaches with higher therapeutic efficacy.
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