Department of Internal Medicine, Diabetology and Nephrology, Faculty of Medical Sciences in Zabrze, Medical University of Silesia, Poniatowskiegostr., 40-055 Katowice, Poland.
Int J Environ Res Public Health. 2021 Feb 8;18(4):1612. doi: 10.3390/ijerph18041612.
In patients with chronic kidney disease (CKD), anemia develops gradually, which is primarily due to an inadequate synthesis of erythropoietin by the kidneys, as well as to iron disorders in the body, blood loss, shortened erythrocyte survival and inflammation. The currently accepted treatment employs iron, vitamin B12, folic acid supplementation and the use of erythropoiesis stimulants, which are administered only parenterally. Research is currently underway on the new erythropoiesis drugs that can be orally administered, i.e., hypoxia-inducible factor-propyl hydroxylase inhibitor (HIF-PHI) inhibitors which temporarily block propyl hydroxylase [PHD] catalysis and promote a transient increase in the expression of genes regulated by HIF, including kidney and liver erythropoietin [EPO]. Roxadustat is the first oral drug in this class and a potent HIF-PHD inhibitor, exerted to treat anemia in patients with CKD. In phase 1, 2 and 3 studies with CKD-affected patients, roxadustat was more effective to stimulate erythropoiesis for anemia correction than previously used drugs. Roxadustat can be orally given, unlike other erythropoiesis drugs with parenteral administration only, which grants roxadustat a considerable advantage. Our paper presents the results of studies with roxadustat applied for the treatment of anemia in CKD patients with or without dialysis. We are currently not yet able to know the exact role of roxadustat in the treatment of anemia in patients with CKD, but time will tell. It is possible that roxadustat has benefits an iron metabolism and cardiovascular risk.
在慢性肾脏病(CKD)患者中,贫血逐渐发展,这主要是由于肾脏促红细胞生成素合成不足,以及体内铁紊乱、失血、红细胞寿命缩短和炎症所致。目前公认的治疗方法是使用铁、维生素 B12、叶酸补充剂和促红细胞生成刺激剂,这些药物只能通过注射给药。目前正在研究新的促红细胞生成药物,这些药物可以口服,即低氧诱导因子脯氨酰羟化酶抑制剂(HIF-PHI)抑制剂,它们暂时阻断脯氨酰羟化酶[PHD]的催化作用,并促进受 HIF 调节的基因表达短暂增加,包括肾脏和肝脏促红细胞生成素[EPO]。罗沙司他是该类药物中的第一个口服药物,也是一种有效的 HIF-PHI 抑制剂,用于治疗 CKD 患者的贫血。在 1 期、2 期和 3 期对 CKD 患者的研究中,罗沙司他在刺激红细胞生成以纠正贫血方面比以前使用的药物更有效。与其他仅通过注射给药的促红细胞生成药物不同,罗沙司他可以口服给药,这使罗沙司他具有相当大的优势。我们的论文介绍了罗沙司他用于治疗有或无透析的 CKD 患者贫血的研究结果。我们目前还不能确切了解罗沙司他在治疗 CKD 患者贫血中的作用,但时间会证明一切。罗沙司他可能对铁代谢和心血管风险有益。