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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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.
|Molidustat (BAY 85-3934)
Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2.
MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively.
PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor.
BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
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