Department of Nephrology and Dialysis, Alessandro Manzoni Hospital ASST-Lecco, Lecco, Italy.
Nephrol Dial Transplant. 2020 Jun 1;35(6):926-932. doi: 10.1093/ndt/gfz031.
Prolyl-hydroxylase (PHD) inhibitors (PHD-I) are the most appealing drugs undergoing clinical development for the treatment of anaemia in patients with chronic kidney disease. PHD inhibition mimics the exposure of the body to hypoxia and activates the hypoxia-inducible factor system. Among many other pathways, this activation promotes the production of endogenous erythropoietin (EPO) and the absorption and mobilization of iron. PHD-I are given orally and, differing from erythropoiesis-stimulating agents (ESAs), they correct and maintain haemoglobin levels by stimulating endogenous EPO production. Their efficacy and safety are supported by several Phases I and II studies with relatively short follow-up. This class of drugs has the potential to have a better safety profile than ESAs and there may be additional advantages for cardiovascular disease (CVD), osteoporosis and metabolism. However, possible adverse outcomes are feared. These span from the worsening or occurrence of new cancer, to eye complications or pulmonary hypertension. The data from the ongoing Phase III studies are awaited to better clarify the long-term safety and possible advantages of PHD-I.
脯氨酰羟化酶(PHD)抑制剂(PHD-I)是最具吸引力的药物,正在进行临床开发,用于治疗慢性肾脏病患者的贫血。PHD 抑制模拟了机体暴露于缺氧环境,并激活了缺氧诱导因子系统。在许多其他途径中,这种激活促进了内源性促红细胞生成素(EPO)的产生以及铁的吸收和动员。PHD-I 通过口服给药,与红细胞生成刺激剂(ESA)不同,通过刺激内源性 EPO 的产生来纠正和维持血红蛋白水平。它们的疗效和安全性得到了多项 I 期和 II 期研究的支持,这些研究的随访时间相对较短。与 ESA 相比,这类药物具有更好的安全性,并且可能对心血管疾病(CVD)、骨质疏松症和代谢有额外的益处。然而,人们担心可能会出现不良后果。这些后果从新癌症的恶化或发生,到眼部并发症或肺动脉高压都有涉及。正在进行的 III 期研究的数据有望更好地阐明 PHD-I 的长期安全性和可能的优势。