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]
Rheumatoid arthritis	FA20	Phase 2	[2]

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	[3]
Janus kinase 3 (JAK-3)	TTT7PJU	JAK3_HUMAN	Inhibitor	[4]
Tyrosine-protein kinase (PTK)	TTJSQEF	NOUNIPROTAC	Inhibitor	[2]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Sulfotransferase 2A1 (SULT2A1)	DE0P6LK	ST2A1_HUMAN	Phase 4	[5]
Nicotinamide N-methyltransferase (NNMT)	DECVGJ3	NNMT_HUMAN	Phase 4	[5]

------------------------------------------------------------------------------------

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	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	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).
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: 2049).
5	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.