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缺氧诱导因子脯氨酰羟化酶抑制剂的生物分析、分析、化学及药理学方面

Bioanalysis, Analysis, Chemistry, and Pharmacological Aspects of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors.

作者信息

Jain Sunidhi, Patil Roshani, Sharma Sanjay

机构信息

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS Deemed to be University, Vile Parle West, Mumbai, Maharashtra, India-400056.

出版信息

Curr Top Med Chem. 2025;25(12):1451-1466. doi: 10.2174/0115680266324419241227102847.

DOI:10.2174/0115680266324419241227102847
PMID:39791153
Abstract

The development of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIFPHIs), such as Roxadustat (ROX), Enarodustat (ENA), Desidustat (DES), Vadadustat (VAD), Molidustat (MOL), and Daprodustat (DAP), has significant effects on anemia in chronic kidney disease. This review presents comprehensive information about the synthesis, pharmacology, and analysis of HIF-PHIs across several matrices. The literature has presented several approaches for quantifying HIF-PHIs in diverse sample matrices. Furthermore, HIF-PHIs exhibit similar modes of action, demonstrating distinct pharmacokinetic parameters. The pharmacological insights encompass their half-life, mechanism of action, absorption, distribution, metabolism, excretion, and therapeutic uses. Research indicates that most studies concentrate on hyphenated methodologies for drug estimation in various biological fluids. Consequently, this study assesses the biological efficacy of HIF-PHIs and elucidates the analytical methodologies currently employed for measurement across various matrices.

摘要

缺氧诱导因子脯氨酰羟化酶抑制剂(HIFPHIs)的研发,如罗沙司他(ROX)、恩那司他(ENA)、达司他(DES)、伐达司他(VAD)、莫利司他(MOL)和达普司他(DAP),对慢性肾脏病贫血具有显著影响。本综述提供了有关HIF-PHIs在多种基质中的合成、药理学及分析的全面信息。文献中介绍了多种在不同样品基质中定量HIF-PHIs的方法。此外,HIF-PHIs表现出相似的作用模式,具有不同的药代动力学参数。药理学见解包括它们的半衰期、作用机制、吸收、分布、代谢、排泄及治疗用途。研究表明,大多数研究集中于采用联用技术测定各种生物流体中的药物。因此,本研究评估了HIF-PHIs的生物学疗效,并阐明了目前用于各种基质测量的分析方法。

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A multianalyte LC-MS/MS method for accurate quantification of Nitrosamines in Olmesartan tablets.一种用于奥沙坦片剂中硝胺类物质准确定量的多分析物 LC-MS/MS 方法。
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Efficacy and safety of vadadustat compared to darbepoetin alfa on anemia in patients with chronic kidney disease: a meta-analysis.与达依泊汀α相比,瓦达他司他治疗慢性肾脏病患者贫血的疗效和安全性:一项荟萃分析。
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Liquid chromatography-tandem mass spectrometry methods for quantification of roxadustat (FG-4592) in human plasma and urine and the applications in two clinical pharmacokinetic studies.液相色谱-串联质谱法测定人血浆和尿液中罗沙司他(FG-4592)的浓度及其在两项临床药代动力学研究中的应用。
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Daprodustat prevents cyclosporine-A-mediated anemia and peritubular capillary loss.达普司他可预防环孢素 A 引起的贫血和肾小管周毛细血管丢失。
Kidney Int. 2022 Oct;102(4):750-765. doi: 10.1016/j.kint.2022.04.025. Epub 2022 May 26.
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