General Information of the Drug (ID: M6APDG03043)
Name
GSK-1278863
Synonyms
Daprodustat; Daprodustat (GSK1278863); Daprodustat (JAN/USAN/INN); Daprodustat [USAN:INN]; Daprodustat(GSK1278863); JVR38ZM64B; ZINC231226004; 2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinan-5-yl)formamido]acetic acid; 960539-70-2; AKOS027439964; BCP16766; CHEMBL3544988; EX-A1121; GSK 1278863; GSK-1278863; GSK1278863; GTPL8455; KS-00000M8Z; MFCD29924726; N-((1,3-Dicyclohexylhexahydro-2,4,6-trioxopyrimidin-5-yl)carbonyl)glycine; UNII-JVR38ZM64B; s8171
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Status
Phase 2
Structure
Formula
C19H27N3O6
InChI
1S/C19H27N3O6/c23-14(24)11-20-16(25)15-17(26)21(12-7-3-1-4-8-12)19(28)22(18(15)27)13-9-5-2-6-10-13/h12-13,15H,1-11H2,(H,20,25)(H,23,24)
InChIKey
RUEYEZADQJCKGV-UHFFFAOYSA-N
PubChem CID
91617630
INTEDE Drug ID
DR1824
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Cytochrome P450 2C8 (CYP2C8)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for GSK-1278863. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of GSK-1278863 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for GSK-1278863. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of GSK-1278863 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for GSK-1278863. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GSK-1278863 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for GSK-1278863. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of GSK-1278863 through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
References
Ref 1 Methylation of adenosine at the N(6) position post-transcriptionally regulates hepatic P450s expression. Biochem Pharmacol. 2020 Jan;171:113697. doi: 10.1016/j.bcp.2019.113697. Epub 2019 Nov 7.
Ref 2 Pharmacokinetics, pharmacodynamics and safety of single, oral doses of GSK1278863, a novel HIF-prolyl hydroxylase inhibitor, in healthy Japanese and Caucasian subjects. Drug Metab Pharmacokinet. 2015 Dec;30(6):410-8. doi: 10.1016/j.dmpk.2015.08.004. Epub 2015 Aug 28.