peficitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.207 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 6.592 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 33.189 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 8.690 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 33.750 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 56.580 % High 1
herg hERG pIC50 4.405 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 12.706 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 8.414 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 27.410 % High 1
kinase-safety-class AAK1,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CHEK2,CLK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK15,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MST1R,MTOR,NTRK1,NTRK2,NTRK3,NUAK1,PAK4,PAK5,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CD,PIK3CG,PIM2,PIM3,PRKAA1,PRKAA2,PRKCA,PRKCD,PRKD1,PRKDC,RET,RIPK3,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK17A,STK3,STK33,STK4,SYK,TBK1,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1 148
kinase-selectivity-class AAK1,ACVR2B,AURKA,AURKB,AURKC,AXL,CAMK2D,CDK1,CDK2,CDK7,CDK9,CLK2,CLK4,CSF1R,DYRK1B,EGFR,EIF2AK3,FLT3,GSK3B,HASPIN,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,LRRK2,MAP2K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MARK4,NTRK1,NTRK3,NUAK1,PDK1,PIK3CA,PIK3CD,PRKDC,ROCK1,ROCK2,SIK2,SIK3,STK17A,STK33,STK4,SYK,TNIK,TYRO3,ULK1,ULK2 56
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 15.885 High 1
mh-clint Mouse hepatocyte intrinsic clearance 31.189 High 1
mppb Mouse plasma protein binding (% unbound) 27.920 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 14.289 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 42.120 % High 1
rh-clint Rat hepatocyte intrinsic clearance 49.774 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 77.130 % High 1
rppb Rat plasma protein binding (% unbound) 29.230 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 114.815 uM High 1

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 L04AF06 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Janus-associated kinase (JAK) inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

L04AF Janus-associated kinase (JAK) inhibitors 7 drugs

Drug Use | Suggest Off label Use Form| |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
1353219-05-2 SECONDARY_CAS_RN
C4505522 UMLSCUI
CHEBI:755142 CHEBI
9T6 PDB_CHEM_ID
CHEMBL3137308 ChEMBL_ID
57928403 PUBCHEM_CID
DB11708 DRUGBANK_ID
CHEMBL3137329 ChEMBL_ID
9910 INN_ID
C000608065 MESH_SUPPLEMENTAL_RECORD_UI
8315 IUPHAR_LIGAND_ID
D10653 KEGG_DRUG
HPH1166CKX INXIGHT DRUGS

Pharmaceutical products:

None