In vitro activity: Daprodustat (formerly known as GSK1278863) is a novel orally bioavailable hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI) that is being developed for treatment of anemia associated with chronic kidney disease. GSK1278863 induced an effective EPO response and stimulated non-EPO mechanisms for erythropoiesis in anemic non-dialysis-dependent and dialysis-dependent patients with CKD. In a clinical study conducted in Japanese population to evaluate the pharmacokinetics (PK), pharmacodynamics (PD) and safety of GSK1278863, GSK1278863 was found to be well tolerated, with dose-proportional increases in exposure observed in both groups. There was no evidence of ethnic differences between Japanese and Caucasian with regard to PK or PD.

Kinase Assay: Daprodustat (formerly known as GSK1278863) is a novel orally bioavailable hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI) that is being developed for treatment of anemia associated with chronic kidney disease.

Cell Assay: GSK1278863 is an orally administered small-molecule PHI, and stimulates endogenous EPO synthesis and induce effective erythropoiesis[1]. GSK1278863 has been shown to increase erythropoietin levels, leading to increases in hemoglobin, hematocrit and red blood cell numbers.