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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5419 1206161-97-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • filgotinib
  • filgotinib maleate
  • jyseleca
  • filgotinib hydrochloride
  • G-146034
  • G-146034-101
  • GLPG-0634
Filgotinib is an adenosine triphosphate (ATP)-competitive and reversible inhibitor of the JAK family. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane. JAK1 is important in mediating inflammatory cytokine signals, JAK2 in mediating myelopoiesis and erythropoiesis and JAK3 plays critical roles in immune homeostasis and lymphopoiesis. Within the signalling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs) which modulate intracellular activity including gene expression. Filgotinib modulates these signalling pathways by preventing the phosphorylation and activation of STATs.
  • Molecular weight: 425.51
  • Formula: C21H23N5O3S
  • CLOGP: 2.16
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 96.67
  • ALOGS: -3.38
  • ROTB: 5

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 24, 2020 EMA Gilead Sciences Ireland UC
Sept. 25, 2020 PMDA Gilead Sciences

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 L04AA45 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Rheumatoid arthritis indication 69896004 DOID:7148
Active tuberculosis contraindication 427099000




🐶 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 JAK1 Kinase INHIBITOR IC50 8 SCIENTIFIC LITERATURE DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3 Kinase IC50 6.47 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase IC50 6.56 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase IC50 6.31 CHEMBL
Mitogen-activated protein kinase 10 Kinase Kd 5.67 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 5.30 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.72 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 5.18 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 5.03 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.07 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 5.33 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 5.36 CHEMBL
Uncharacterized aarF domain-containing protein kinase 1 Kinase Kd 5.69 CHEMBL
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 6.09 SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 7.55 SCIENTIFIC LITERATURE
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 6.94 SCIENTIFIC LITERATURE
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.44 CHEMBL
Jak1 protein Unclassified IC50 7.54 CHEMBL

External reference:

IDSource
D11106 KEGG_DRUG
3XVL385Q0M UNII
C4310256 UMLSCUI
2HB PDB_CHEM_ID
CHEMBL3301607 ChEMBL_ID
49831257 PUBCHEM_CID
DB14845 DRUGBANK_ID
CHEMBL4298167 ChEMBL_ID
CHEMBL3301602 ChEMBL_ID
7913 IUPHAR_LIGAND_ID
018759 NDDF
018760 NDDF
C584571 MESH_SUPPLEMENTAL_RECORD_UI
9720 INN_ID
1802998-75-9 SECONDARY_CAS_RN
1540859-07-1 SECONDARY_CAS_RN

Pharmaceutical products:

None