菲尼酮治疗慢性肾病的新药发现。

Akshita Rana, Jagdish K Sahu
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引用次数: 0

摘要

背景:慢性肾病(CKD)最常见的病因是糖尿病肾病(DN)。治疗 CKD 的药物主要有矿质皮质激素受体拮抗剂(MRAs)(螺内酯和依普利酮)、血管紧张素转换酶抑制剂或血管紧张素受体阻滞剂,但由于高钾血症的风险较高,这些药物很少联合使用。目前,非格列酮于 2021 年获得美国食品和药物管理局批准后,在治疗慢性肾脏病方面取得了良好疗效。非格列酮能延缓糖尿病肾病的进展,降低 DN 患者的心血管发病率:这篇综述文章的主要目的是全面深入地概述非格列酮的作用,主要侧重于其药理特性、毒性、用途、用于测定的生物分析技术以及治疗方案:非格列酮通过抑制矿物皮质激素受体的作用而发挥作用。非格列酮经口服后可迅速从消化道吸收,并在 1-2 小时内达到血浆浓度峰值:非格列酮会通过氧化、环氧化取代和直接羟化作用被积极代谢。非奈酮通过尿液和粪便排出体外。非奈酮可通过 HPLC-MS 和 LSC 进行检测:本综述全面介绍了非奈瑞酮的 ADME 特性、生物分析技术、临床试验、毒性以及该领域可能的发展方向。与其他矿质皮质激素受体类药物螺内酯和依普利酮相比,非格列酮能有效治疗慢性肾病。
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Finerenone: A Novel Drug Discovery for the Treatment of Chronic Kidney Disease.

Background: The most common cause of chronic kidney disease (CKD) is diabetic nephropathy (DN). Primarilymineralocorticoid receptor antagonists (MRAs) (spironolactone and eplerenone), angiotensin-converting enzyme inhibitors or angiotensin receptor blockers were used for the treatment of CKD, but due to the high risk of hyperkalaemia, the combination was infrequently used. Currently after approval by FDA in 2021, finerenone was found to be effective in the treatment of CKD. Finerenone slowdowns the progression of diabetic nephropathy and lessens the cardiovascular morbidity in DN patients.

Objective: The main objective of this review article is to provide a comprehensive and insightful overview of the role of finerenone by mainly focusing on its pharmacological properties, toxicity, uses, bioanalytical technique used for determination, and treatment options.

Materials and method: Finerenone works by inhibiting the action of the mineralocorticoid receptor. Finerenone is quickly absorbed from the digestive tract after oral treatment and achieves peak plasma concentrations in 1-2 hours.

Result: Finerenone is actively metabolized through oxidation, epoxidation substitution, and direct hydroxylation. Elimination of finerenone is done through urine and feces. Determination of finerenone can be done through HPLC-MS and LSC.

Conclusion: The present review covers the complete picture of ADME properties, bioanalytical techniques, clinical trials, toxicity, and possible avenues in this arena. Finerenone is effective compared to other mineralocorticoid receptor-like spironolactone and eplerenone, for the treatment of chronic kidney disease.

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