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delgocitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Janus kinase inhibitors, antineoplastics | 5426 | 1263774-59-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 2% | ANZUPGO | LEO PHARMA AS | N219155 | July 23, 2025 | RX | CREAM | TOPICAL | July 23, 2030 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Anzupgo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50222-280 | CREAM | 20 mg | TOPICAL | NDA | 27 sections |