论法内甾体X受体激动剂的药理学:给我一个“A”,就像“酸”一样

E. Hambruch, O. Kinzel, C. Kremoser
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引用次数: 6

摘要

Farnesoid X受体(FXR)最近因使用FXR激动剂obticholic Acid的临床数据而受到关注,该数据证明了这种胆汁酸样药物对原发性胆汁性肝硬化和非酒精性脂肪性肝炎(NASH)患者的有效性。FXR有望成为各种疾病的有吸引力的药物靶点,从非酒精性脂肪性肝病(NAFLD)、NASH、肝硬化、门脉高压和各种胆汁淤积性疾病到肠道疾病,包括炎症性肠病和胆汁酸腹泻。尽管具有广泛的治疗潜力,但令人惊讶的是,针对FXR的药物的药理学,药代动力学和组织分布特性知之甚少。组织特异性FXR激动剂是否适用于不同适应症,或者一种配体是否适合所有用途?本综述旨在总结这一临床和药理学相关主题的稀疏数据,并为理解体内组织特异性作用提供一个机制模型。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
On the Pharmacology of Farnesoid X Receptor Agonists: Give me an "A", Like in "Acid"
The Farnesoid X Receptor (FXR) has recently moved into the spotlight through the release of clinical data using Obeticholic Acid, an FXR agonist, that demonstrated effectiveness of this bile acid-like drug in patients with Primary Biliary Cirrhosis and Non-alcoholic Steatohepatitis (NASH). FXR holds the promise to become an attractive drug target for various conditions, from Non-alcoholic Fatty Liver Disease (NAFLD), NASH, liver cirrhosis, portal hypertension and a variety of cholestatic disorders to intestinal diseases including inflammatory bowel disease and bile acid diarrhea. Despite the wide therapeutic potential, surprisingly little is known about the pharmacology, pharmacokinetics and tissue distribution properties of drugs targeting FXR. Are tissue specific FXR agonists preferable for different indications, or might one type of ligand fit all purposes? This review aims to summarize the sparse data which are available on this clinically and pharmacologically relevant topic and provides a mechanistic model for understanding tissue-specific effects in vivo.
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