Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMZ1UOI)

Drug Name
Asp-015K Drug Info
Synonyms
Peficitinib; ASP015K; UNII-HPH1166CKX; 944118-01-8; ASP-015K; HPH1166CKX; 4-[[(1R,3S)-5-hydroxy-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; 4-[[(1S,3R)-5-oxidanyl-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide; Peficitinib [USAN:INN]; ASP 015K; JNJ-54781532; 9T6; Peficitinib (USAN/INN); SCHEMBL1154421; SCHEMBL9990248; SCHEMBL4447032; GTPL8315; SCHEMBL9990240; SCHEMBL1154418; CHEMBL3137308; SCHEMBL17645135; BCP18465; BDBM50124208; SB16834; DB11708; SC-17960; ASP015K; JNJ-54781532; D10653; Peficitinib pound A
Indication
Disease Entry ICD 11 Status REF
Psoriasis vulgaris EA90 Phase 3 [1] , [2]
Rheumatoid arthritis FA20 Phase 2 [3]
Cross-matching ID
PubChem CID
57928403
CAS Number
CAS 944118-01-8
TTD Drug ID
DMZ1UOI
INTEDE Drug ID
DR1774

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Janus kinase 1 (JAK-1) TT6DM01 JAK1_HUMAN Inhibitor [4]
Janus kinase 3 (JAK-3) TTT7PJU JAK3_HUMAN Inhibitor [5]
Tyrosine-protein kinase (PTK) TTJSQEF NOUNIPROTAC Inhibitor [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Sulfotransferase 2A1 (SULT2A1) DE0P6LK ST2A1_HUMAN Phase 4 [6]
Nicotinamide N-methyltransferase (NNMT) DECVGJ3 NNMT_HUMAN Phase 4 [6]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Janus kinase 3 (JAK-3) DTT JAK3 2.104 3.248 2.848 4.485
Janus kinase 1 (JAK-1) DTT JAK1 8.621 9.012 9.168 8.535
Sulfotransferase 2A1 (SULT2A1) DME SULT2A1 9.177 3.42 3.591 7.614
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Psoriasis vulgaris
ICD Disease Classification EA90
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Janus kinase 3 (JAK-3) DTT JAK3 4.94E-03 0.28 1.41
Nicotinamide N-methyltransferase (NNMT) DME NNMT 2.73E-02 -1.27E-01 -4.45E-01
Nicotinamide N-methyltransferase (NNMT) DME NNMT 1.75E-03 -4.71E-01 -1.97E+00
Sulfotransferase 2A1 (SULT2A1) DME SULT2A1 5.88E-01 3.51E-02 3.36E-01
Sulfotransferase 2A1 (SULT2A1) DME SULT2A1 2.71E-04 -2.83E-01 -2.39E+00
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8315).
2 ClinicalTrials.gov (NCT02308163) A Study to Evaluate Safety and Efficacy of ASP015K in Patients With Rheumatoid Arthritis (RA) Who Had an Inadequate Response to DMARDs. U.S. National Institutes of Health.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2047).
5 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2049).
6 Human mass balance, metabolite profile and identification of metabolic enzymes of [14C]ASP015K, a novel oral janus kinase inhibitor. Xenobiotica. 2015;45(10):887-902.