peficitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
Janus kinase inhibitors, antineoplastics 5481 944118-01-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • peficitinib
  • peficitinib hydrobromide
  • smyraf
  • ASP015K
  • JNJ-54781532
Peficitinib inhibits the signal transduction of cytokines important for the pathological condition of RA as it inhibits the kinase activity of the JAK family (JAK1, JAK2, JAK3, and TYK2) and their signal transduction mediated by IL-2.
  • Molecular weight: 326.40
  • Formula: C18H22N4O2
  • CLOGP: 2.22
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 104.03
  • ALOGS: -3.31
  • ROTB: 3

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 26, 2019 PMDA ASTELLAS PHARMA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AA49 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Rheumatoid arthritis indication 69896004 DOID:7148
Hepatic failure contraindication 59927004
Pregnancy contraindication 289908002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 9.15 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 8.41 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 8.30 DRUG LABEL DRUG LABEL
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 8.32 DRUG LABEL DRUG LABEL

External reference:

IDSource
HPH1166CKX UNII
C4505522 UMLSCUI
9T6 PDB_CHEM_ID
CHEMBL3137308 ChEMBL_ID
57928403 PUBCHEM_CID
DB11708 DRUGBANK_ID
CHEMBL3137329 ChEMBL_ID
8315 IUPHAR_LIGAND_ID
D10653 KEGG_DRUG
C000608065 MESH_SUPPLEMENTAL_RECORD_UI
9910 INN_ID
1353219-05-2 SECONDARY_CAS_RN

Pharmaceutical products:

None