Prolyl hydroxylase (PHD) inhibitors, such as roxadustat, can stabilize hypoxia-inducible factor (HIF)-2α and induce erythropoietin (EPO) production under normal conditions. Roxadustat was recently approved as a first-in-class orally active drug for the treatment of renal anemia. In addition, it has garnered growing therapeutic interest for use against various diseases, such as carcinoma, neurological diseases, ocular diseases, and tissue and organ injuries. In this review, we systemically review target validation, hit identification, and further key clinical trials of roxadustat. The prospective clinical applications of PHD inhibitors are then discussed based on this marketed drug.

脯氨酰羟化酶 (PHD) 抑制剂，如罗沙司他，可在正常条件下稳定缺氧诱导因子 (HIF)-2α 并诱导促红细胞生成素 (EPO) 的产生。罗沙司他最近被批准为治疗肾性贫血的一流口服活性药物。此外，它已获得越来越多的治疗兴趣，用于治疗各种疾病，如癌症、神经系统疾病、眼部疾病以及组织和器官损伤。在这篇综述中，我们系统地回顾了罗沙司他的靶点验证、命中识别和进一步的关键临床试验。然后基于该上市药物讨论PHD抑制剂的前瞻性临床应用。