Enarodustat (For research purpose only) 1262132-81-9

Enarodustat (JTZ-951) is an effective oral active HIF prolyl hydroxylase inhibitor with an IC50 value of 0.22 μ M for PHD2 and an EC50 value of 5.7 μ M for EPO release from Hep3B cells. Enalodustat has the potential to treat renal anemia.

It is a new generation of hypoxia inducible factor prolyl hydroxylase inhibitor (HIF-PHI) drug, which is currently on the market in Japan. In December 2019, Xinlitai invested $87.5 million to introduce it from Japan Tobacco. According to a press release from Xinlitai, as a new generation HIF-PHI drug, Ennadustat has a more reasonable and moderate regulation of HIF targets, stimulates the generation of endogenous EPO (erythropoietin) that is closer to physiological concentrations, steadily and controllably increases hemoglobin, and overall has good safety. In addition, it also has the advantages of once a day oral administration, good medication compliance, no need for weight adjustment, and low risk of drug interactions.

The Phase 3 clinical data of Ennadustat reported at the 2023 ASN conference in China indicate that the new generation HIF-PHI drug Ennadustat has good efficacy and safety. Ennadustat is highly effective in initially increasing Hb levels in subjects, with long-lasting and stable therapeutic effects. It can also significantly reduce ferritin and improve iron absorption and utilization. In addition, meeting clinical needs such as fewer medication adjustments and ensuring medication safety may help achieve long-term management of renal anemia, making it the preferred treatment for renal anemia.