Filgotinib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Filgotinib is a drug catalogued in DrugCentral. It was first approved by the EMA in 2020. DrugCentral lists 23 molecular targets, including JAK1, JAK2 and Jak1. Recorded indications include Rheumatoid arthritis and Ulcerative colitis.

• Molecular targets: JAK1, JAK2, Jak1 and TYK2 (23 listed in DrugCentral).
• Indications: Rheumatoid arthritis and Ulcerative colitis.
• ATC code: L04AF04 (Janus-associated kinase (JAK) inhibitors).
• Molecular formula: C21H23N5O3S; molecular weight 425.51 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Rheumatoid arthritis
• Ulcerative colitis

Contraindications (1)

• Active tuberculosis

Mechanism & targets

Molecular targets (23)

Target	Gene	Action	Activity
Tyrosine-protein kinase JAK1	JAK1	inhibitor	IC50 8.00
Tyrosine-protein kinase JAK2	JAK2	inhibitor	IC50 7.55
Jak1 protein	Jak1	unknown	IC50 7.54
Non-receptor tyrosine-protein kinase TYK2	TYK2	inhibitor	IC50 6.94
Vascular endothelial growth factor receptor 3	FLT4	unknown	IC50 6.56
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	IC50 6.47
Macrophage colony-stimulating factor 1 receptor	CSF1R	unknown	IC50 6.31
Signal transducer and activator of transcription 1-alpha/beta	STAT1	unknown	IC50 6.20
Tyrosine-protein kinase JAK3	JAK3	inhibitor	IC50 6.09
Tyrosine-protein kinase Mer	MERTK	unknown	IC50 5.89
Vascular endothelial growth factor receptor 1	FLT1	unknown	IC50 5.88
Serine/threonine-protein kinase TBK1	TBK1	unknown	IC50 5.75
Serine/threonine-protein kinase 10	STK10	unknown	Kd 5.72
Uncharacterized aarF domain-containing protein kinase 1	ADCK1	unknown	Kd 5.69
Mitogen-activated protein kinase 10	MAPK10	unknown	Kd 5.67
Tyrosine-protein kinase ABL1	ABL1	unknown	IC50 5.64
Calcium/calmodulin-dependent protein kinase kinase 2	CAMKK2	unknown	Kd 5.44
Uncharacterized protein FLJ45252	—	unknown	Kd 5.36
Interleukin-1 receptor-associated kinase 1	IRAK1	unknown	Kd 5.33
AP2-associated protein kinase 1	AAK1	unknown	Kd 5.30

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2020-09-25	PMDA	—	Gilead Sciences
2020-09-24	EMA	—	Gilead Sciences Ireland UC

ATC classification

ATC code	Therapeutic hierarchy
L04AF04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Janus-associated kinase (JAK) inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Angiolymphoid hyperplasia with eosinophilia	87.1
Diarrhoea haemorrhagic	73.4
Rhesus antigen positive	71.0
Enteropathic spondylitis	57.4
Large intestine erosion	49.7
Jugular vein thrombosis	46.6
Blood albumin increased	44.5

Chemical structure

• Molecular formula: C₂₁H₂₃N₅O₃S
• Molecular weight: 425.51 g/mol
• CAS number: 1206161-97-8
• InChIKey: RIJLVEAXPNLDTC-UHFFFAOYSA-N
• PubChem CID: 49831257

C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Filgotinib used for?

DrugCentral lists the following indications for Filgotinib: Rheumatoid arthritis and Ulcerative colitis.

How does Filgotinib work?

Its molecular targets in DrugCentral include JAK1 (inhibitor), JAK2 (inhibitor), Jak1 and TYK2 (inhibitor).

When was Filgotinib first approved?

Filgotinib was first approved by the EMA in 2020.

What is the chemical formula of Filgotinib?

Filgotinib has the molecular formula C21H23N5O3S and a molecular weight of 425.51 g/mol.

Sources

• DrugCentral drug card 5419 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3301602 — compound record and bioactivity
• PubChem CID 49831257 — chemical identifiers
• DrugBank DB14845 — drug record
• FDA UNII 3XVL385Q0M — substance identity
• UniProt P23458 (JAK1) — target protein
• UniProt O60674 (JAK2) — target protein
• UniProt P29597 (TYK2) — target protein
• UniProt P35916 (FLT4) — target protein
• UniProt P36888 (FLT3) — target protein
• UniProt P07333 (CSF1R) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.