Su Kaijun, Zhihong Li, Yu Yancheng
May 4, 2020
Citations
1
Influential Citations
16
Citations
Quality indicators
Journal
Drug discovery today
Abstract
TEASER This review presents recent advances in potential clinical applications of the representative prolyl hydroxylase inhibitor roxadustat and summarizes the overall research and development process, from target discovery to marketing. 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.