新型中枢肾素-血管紧张素-醛固酮系统抑制剂:Firibastat

Nidhi Maheshwari, Vandana Tayal
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引用次数: 0

摘要

摘要高血压是缺血性心脏病、中风、残疾、血管性痴呆、心力衰竭、肾功能障碍、视网膜病变和过早死亡的最重要危险因素之一。尽管使用了两种或两种以上的降压药物,但相当一部分患者表现出控制不佳。目前的抗高血压药物在肥胖人群、某些种族(如黑人)以及肾损伤患者中的使用和效果有限。因此,迫切需要开发新型抗高血压药物,这些药物作用于具有多种作用机制的新靶点,以更有效地控制血压升高。随着心血管疾病中过度活跃的脑肾素-血管紧张素系统的最新概念的引入,已经尝试鉴定具有抑制参与血管紧张素III形成的氨基肽酶的潜力的分子,还有一种前药Firibastat目前正在进行高血压和慢性心力衰竭的III期临床试验。在此,我们提供了迄今为止使用Firibastat产生的证据的最新摘要,并对这种新的候选药物的治疗潜力进行了初步了解,该候选药物扩展到了原发性高血压的范围之外
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Novel Class of Central Renin Angiotensin Aldosterone System Inhibitor: Firibastat
Abstract Hypertension is one of the most important risk factors for the development of ischemic heart diseases, stroke, disability, vascular dementia, heart failure, renal dysfunction, retinopathy, and premature death. Despite the use of two or more blood pressure lowering medications, a considerable proportion of patients show poor control. Current antihypertensive medications show the limitation of use and effect in obese population, certain races like black population and also in renal impairment. Thus, there is an impending need to develop novel classes of antihypertensive agents acting on new targets with diversified mechanisms of action to more effectively manage raised blood pressure. With the introduction of the recent concept of overactive brain renin angiotensin system in cardiovascular disorders, attempts have been made to identify a molecule with the potential of inhibiting aminopeptidases involved in the formation of Angiotensin III. A novel aminopeptidase A inhibitor, also a prodrug Firibastat is currently undergoing development in Phase III clinical trials for hypertension as well as chronic heart failure. We hereby, provide an updated summary of evidence generated so far with Firibastat and also a glimpse into the therapeutic potential of this novel candidate extending beyond the spectrum of essential hypertension
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