Reaction: Daprodustat to 1 product

Reaction
Reaction type
oxidation
Direction
Major circulating metabolite?
Yes
Spontaneous?
No
Activity
active
References
  1. Licea Perez H, Knecht D, Evans CA: Overcoming bioanalytical challenges associated with the separation and quantitation of GSK1278863, a HIF-prolyl hydroxylase inhibitor, and its 14 stereoisomeric metabolites. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Jan 15;1009-1010:7-16. doi: 10.1016/j.jchromb.2015.11.057. Epub 2015 Dec 4. [Article]
  2. Johnson BM, Stier BA, Caltabiano S: Effect of food and gemfibrozil on the pharmacokinetics of the novel prolyl hydroxylase inhibitor GSK1278863. Clin Pharmacol Drug Dev. 2014 Mar;3(2):109-17. doi: 10.1002/cpdd.83. Epub 2013 Oct 22. [Article]
  3. Mahar KM, Caltabiano S, Andrews S, Ramanjineyulu B, Chen L, Young G, Pereira A, Lindsay AC, van den Berg F, Cobitz AR: Clinical Pharmacokinetics of Daprodustat: Results of an Absorption, Distribution, and Excretion Study With Intravenous Microtracer and Concomitant Oral Doses for Bioavailability Determination. Clin Pharmacol Drug Dev. 2021 Dec;10(12):1419-1431. doi: 10.1002/cpdd.1029. Epub 2021 Oct 28. [Article]
  4. FDA Approved Drug Products: JESDUVROQ (daprodustat) tablets, for oral use [Link]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
Cytochrome P450 2C8Not AvailableNot Availableimplied
Cytochrome P450 3A4Not AvailableNot Availableimplied