Zhu Xiaoyu, Jiang Lili, Wei Xuejiao, Long Mengtuan, Du Yujun
Department of Nephrology, The First Hospital of Jilin University, Changchun, Jilin, China.
Physical Examination Center, The First Hospital of Jilin University, Changchun, Jilin, China.
Front Pharmacol. 2022 Aug 29;13:971795. doi: 10.3389/fphar.2022.971795. eCollection 2022.
Roxadustat is a recently approved hypoxia-inducible factor prolyl hydroxylase inhibitor that has demonstrated favorable safety and efficacy in the treatment of renal anemia. Recent studies found it also has potential for the treatment of other hypoxia-related diseases. Although clinical studies have not yet found significant adverse or off-target effects of roxadustat, clinicians must be vigilant about these possible effects. Hypoxia-inducible factor regulates the expression of many genes and physiological processes in response to a decreased level of oxygen, but its role in the pathogenesis of different diseases is complex and controversial. In addition to increasing the expression of hypoxia-inducible factor, roxadustat also has some effects that may be HIF-independent, indicating some potential off-target effects. This article reviews the pharmacological characteristics of roxadustat, its current status in the treatment of renal anemia, and its possible effects on other pathological mechanisms.
罗沙司他是一种最近获批的缺氧诱导因子脯氨酰羟化酶抑制剂,已在肾性贫血治疗中显示出良好的安全性和疗效。最近的研究发现它在治疗其他缺氧相关疾病方面也具有潜力。尽管临床研究尚未发现罗沙司他有显著的不良或脱靶效应,但临床医生必须对这些可能的效应保持警惕。缺氧诱导因子可响应氧气水平降低来调节许多基因的表达和生理过程,但其在不同疾病发病机制中的作用复杂且存在争议。除了增加缺氧诱导因子的表达外,罗沙司他还具有一些可能与缺氧诱导因子无关的效应,提示存在一些潜在的脱靶效应。本文综述了罗沙司他的药理学特性、其在肾性贫血治疗中的现状以及它对其他病理机制可能产生的影响。