molecules of the month


oral, once-daily, pan-PHD inhibitor

FDA-approved for anemia in CKD patients

designed PHD cofactor mimetic

FDA approval, February 1, 2023

GSK, PLC, London, UK

daprodustat, oral, once-daily, pan-PHD inhibitor FDA-approved for anemia in CKD patients, GSK, PLC, LONDON, UK
5 mins read

The first and only HIF prolyl hydroxylase inhibitor approved in the US. Erythropoetin (EPO) stimulates red blood cell production (erythropoeisis). Recombinant erythropoetin (e.g. Amgen’s epoetin alfa) is therefore a treatment for anemia (lack of healthy red blood cells) and was one of the first biotech products to be approved (in 1989) and subsequently exploited by athletes like Lance Armstrong as a performance-enhancing drug. Prolyl hydroxylase domains (PHDs) have been attractive targets for treating anemia, especially in chronic kidney disease (CKD) patients, as they regulate levels of hypoxia-inducible factors (HIFs) including HIF-2, which induces erythropoietin production in the kidney and liver. Inhibition of PHDs prevents the proteosomal degradation of HIFs, promoting erythropoetin gene transcription among other positive effects. Daprodustat’s FDA approval…

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