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

Stem definitionDrug idCAS RN
Janus kinase inhibitors, antineoplastics 5426 1263774-59-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • delgocitinib
  • JTE-052
  • JTE-052A
  • LEO 124249
  • LEO 124249A
  • LP0133
  • corectim
Delgocitinib, a janus kinase (JAK) inhibitor, is being approved for the treatment of inflammatory skin conditions. Delgocitinib inhibited the activation of inflammatory cells, such as T cells, B cells, monocytes and mast cells, in vitro and inhibited Th1-, Th2- and Th17-type cytokine production from both T cells and non-T cells.
  • Molecular weight: 310.36
  • Formula: C16H18N6O
  • CLOGP: 1
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 88.91
  • ALOGS: -2.75
  • ROTB: 2

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class AAK1,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FGFR1,FLT3,GRK1,GRK2,GRK3,GSK3B,IGF1R,IKBKB,IRAK1,ITK,JAK1,JAK2,JAK3,KIT,LCK,LRRK2,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K2,MAP3K21,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK3,MAPK7,MAPK9,MARK4,MELK,MET,MINK1,NTRK1,NUAK1,PAK4,PDK1,PDK2,PIK3CD,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKDC,PRKG1,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2 88
kinase-selectivity-class AAK1,ACVR2B,AKT1,AURKA,AURKB,AXL,CAMK2B,CAMK2D,CDK9,CHEK1,CLK2,CLK4,CSF1R,DYRK1B,EGFR,FGFR1,FLT3,HASPIN,IRAK1,JAK1,JAK2,JAK3,LRRK2,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MARK3,MARK4,MELK,NTRK1,NUAK1,PDK1,PRKAA1,PRKAA2,PRKACA,PRKCD,ROCK1,ROCK2,SIK2,SIK3,STK33,SYK,ULK1 47
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 23, 2020 PMDA Japan Tobacco

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Product use in unapproved indication 102.34 94.69 29 64 447348 110141858

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D11AH11 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Agents for dermatitis, excluding corticosteroids
MeSH PA D000075242 Janus Kinase Inhibitors
MeSH PA D003879 Dermatologic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA MoA N0000190857 Janus Kinase Inhibitors
FDA EPC N0000190858 Janus Kinase Inhibitor
CHEBI has role CHEBI:35472 anti-inflammatory drug
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:59010 antiseborrheic
CHEBI has role CHEBI:76617 EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor

Related Drugs by ATC class:

D11AH Agents for dermatitis, excluding corticosteroids 11 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Atopic dermatitis indication 24079001 DOID:3310




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
2% ANZUPGO LEO PHARMA AS N219155 July 23, 2025 RX CREAM TOPICAL 8609647 Sept. 19, 2031 METHOD OF INHIBITING JANUS KINASE 2 OR JANUS KINASE 3 TO TREAT MODERATE TO SEVERE CHRONIC HAND ECZEMA (CHE) IN ADULTS WHO HAVE HAD AN INADEQUATE RESPONSE TO, OR FOR WHOM TOPICAL CORTICOSTEROIDS ARE NOT ADVISABLE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
2% ANZUPGO LEO PHARMA AS N219155 July 23, 2025 RX CREAM TOPICAL July 23, 2030 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 7.89 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 8.55 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 8.58 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 7.24 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Signal transducer and activator of transcription 3 Transcription factor IC50 7.75 CHEMBL
Rho-associated protein kinase 2 Kinase INHIBITOR IC50 6.58 SCIENTIFIC LITERATURE
Tyrosine-protein kinase Lck Kinase IC50 5.24 CHEMBL

External reference:

IDSource
D11046 KEGG_DRUG
9L0Q8KK220 UNII
C5226741 UMLSCUI
CHEBI:167600 CHEBI
CHEMBL4297507 ChEMBL_ID
50914062 PUBCHEM_CID
DB16133 DRUGBANK_ID
10574 INN_ID
C000621572 MESH_SUPPLEMENTAL_RECORD_UI
9619 IUPHAR_LIGAND_ID
567841000202108 SNOMEDCT_US
4044148 VANDF
FHX PDB_CHEM_ID
44276 MMSL
019994 NDDF
2721163 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Anzupgo HUMAN PRESCRIPTION DRUG LABEL 1 50222-280 CREAM 20 mg TOPICAL NDA 27 sections