Daprodustat (GSK1278863) is a novel, orally active HIF-prolyl hydroxylase inhibitor. It is developed for treatment of anemia associated with chronic kidney disease. GSK1278863 stimulates endogenous EPO synthesis and induce effective erythropoiesis. Daprodustat (GSK1278863) has been shown to increase erythropoietin levels, leading to increases in hemoglobin, hematocrit and red blood cell numbers.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 10 mg/mL warmed|
A Novel Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor (GSK1278863) for Anemia in CKD: A 28-Day, Phase 2A Randomized Trial.
Brigandi RA, et al. Am J Kidney Dis. 2016 Jun;67(6):861-71. PMID: 26827289.
Pharmacokinetics, pharmacodynamics and safety of single, oral doses of GSK1278863, a novel HIF-prolyl hydroxylase inhibitor, in healthy Japanese and Caucasian subjects.
Hara K, et al. Drug Metab Pharmacokinet. 2015 Dec;30(6):410-8. PMID: 26643993.
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Desidustat is an inhibitor of HIF hydroxylase.
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Enarodustat (JTZ-951) is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM.
PT2385 is an orally active, selective inhibitor of hypoxia inducible factor (HIF)-2alpha, with a Ki value of less than 50 nM.
JNJ-42041935 is a potent, competitive, reversible, and selective inhibitor of PHD with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09 for PHD1, PHD2, and PHD3, respectively.
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