Janković Slobodan M, Janković Snežana V
Faculty of Medical Sciences, University of Kragujevac, Svetozara Markovića Street, 69, 34000, Kragujevac, Serbia.
Eur J Drug Metab Pharmacokinet. 2025 May 2. doi: 10.1007/s13318-025-00947-2.
Vadadustat is an innovative drug that inhibits prolyl hydroxylase and has been approved for the treatment of anemia in patients with chronic kidney disease. Its pharmacokinetics are linear, i.e., vadadustat's absorption, distribution, and elimination are predictable. Vadadustat is well absorbed from the gastrointestinal tract, with over 99% of the drug bound to plasma proteins. The majority of the drug is conjugated with glucuronic acid in the liver, and these conjugates are primarily excreted through urine, with a smaller portion eliminated through stool. Only 1% of the unchanged drug is found in the urine, while 9% appears in the stool. In clinical trials, vadadustat demonstrated clear effectiveness compared with placebo, significantly increasing hemoglobin levels in patients with anemia due to chronic kidney disease, with an average increase of 1.43 ± 0.05 g/dL after 6 months of treatment. However, its effectiveness is somewhat lower than that of erythropoietin. The rates and severity of adverse events with vadadustat and erythropoietin are similar. Given that vadadustat is taken orally and has a beneficial efficacy and safety profile, it represents a meaningful addition to the standard treatment for anemia associated with renal failure, working alongside erythropoietin.
伐达他司是一种抑制脯氨酰羟化酶的创新药物，已被批准用于治疗慢性肾病患者的贫血。其药代动力学呈线性，即伐达他司的吸收、分布和消除是可预测的。伐达他司从胃肠道吸收良好，超过99%的药物与血浆蛋白结合。大部分药物在肝脏中与葡萄糖醛酸结合，这些结合物主要通过尿液排泄，一小部分通过粪便排出。尿液中仅发现1%的原形药物，而9%出现在粪便中。在临床试验中，与安慰剂相比，伐达他司显示出明显的疗效，显著提高了慢性肾病所致贫血患者的血红蛋白水平，治疗6个月后平均升高1.43±0.05 g/dL。然而，其疗效略低于促红细胞生成素。伐达他司和促红细胞生成素的不良事件发生率和严重程度相似。鉴于伐达他司为口服给药，且具有良好的疗效和安全性，它是肾衰竭相关贫血标准治疗的一个有意义的补充，可与促红细胞生成素协同作用。
