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Finerenone: a New Mineralocorticoid Receptor Antagonist Without Hyperkalemia: an Opportunity in Patients with CKD?

机译:Finerenone:无高钾血症的新型盐皮质激素受体拮抗剂:CKD患者的机会吗?

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摘要

Aldosterone binds to the mineralocorticoid receptor and has an important regulatory role in body fluid and electrolyte balance. It also influences a variety of different cell functions such as oxidative stress, inflammation and organ fibrosis. The important role of the tissue-specific mineralocorticoid receptors in cardiovascular and renal injury has been shown in knockout animals and in clinical studies Mineralocorticoid receptor antagonists seem to exert their beneficial effects via anti-oxidative, anti-inflammatory and anti-fibrotic effects. Spironolactone and eplerenone were the first steroidal mineralocorticoid receptor antagonist. The established steroidal mineralocorticoid receptor antagonists show important therapeutic effects but are hampered by a variety of side effects, most importantly clinically significant hyperkaliemia. Selective non-steroidal mineralocorticoid receptor antagonists have been recently developed and demonstrate effectiveness in early clinical trials. Finereroneholds promise for the future application of this new mineralocorticoid receptor antagonist class in patients with chronic kidney disease since it has shown a significant reduction in UACR combined with a safety profile similar to that in the placebo group. However, further long-term studies investigating relevant clinical end points like reduction in cardiovascular or renal event rate are warranted.
机译:醛固酮与盐皮质激素受体结合,在体液和电解质平衡中具有重要的调节作用。它还会影响多种不同的细胞功能,例如氧化应激,炎症和器官纤维化。在敲除动物和临床研究中已显示出组织特异性盐皮质激素受体在心血管和肾脏损伤中的重要作用。盐皮质激素受体拮抗剂似乎通过抗氧化,抗炎和抗纤维化作用发挥其有益作用。螺内酯和依普利酮是第一个甾体盐皮质激素受体拮抗剂。既定的类固醇盐皮质激素受体拮抗剂显示出重要的治疗作用,但受到多种副作用(最重要的是临床上显着的高钾血症)的影响。选择性非甾体盐皮质激素受体拮抗剂最近已经开发出来,并在早期临床试验中证明了其有效性。 Finereroneholds有望在慢性肾病患者中应用这种新型盐皮质激素受体拮抗剂,因为它已显示UACR显着降低,并且安全性与安慰剂组相似。但是,有必要进行进一步的长期研究来研究相关的临床终点,例如降低心血管或肾脏事件的发生率。

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