Filgotinib
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Also known as G-146034G146034Glpg-0634GLPG0634GS-6034 FREE BASEG-146034_101FILGOTINIB HYDROCHLORIDEFILGOTINIB (GLPG0634)SID174006711US8563545, 1
Summary
Filgotinib (CHEMBL3301607) is an approved small molecule (ATC L04AF04) targeting JAK1, JAK2, and JAK3; indicated across 13 conditions including rheumatoid arthritis and crohn disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L04AF04
- Targets: 4 (JAK1, JAK2, JAK3…)
- Indications: 13 conditions
- Clinical trials: 53
- Chemistry: 425.5 Da · C21H23N5O3S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3301607 |
| Name | Filgotinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 49831257 |
| ATC | L04AF04 |
| Molecular formula | C21H23N5O3S |
| Molecular weight | 425.5 |
| InChIKey | RIJLVEAXPNLDTC-UHFFFAOYSA-N |
SMILES: C1CC1C(=O)NC2=NN3C(=N2)C=CC=C3C4=CC=C(C=C4)CN5CCS(=O)(=O)CC5
IUPAC name: N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
Also known as: Filgotinib, G-146034, G146034, Glpg-0634, GLPG0634, GS-6034 FREE BASE, FILGOTINIB, GLPG-0634, G-146034_101, FILGOTINIB HYDROCHLORIDE, FILGOTINIB (GLPG0634), SID174006711
Parent form; salt/anhydrous children: CHEMBL3301602, CHEMBL4298167
Patent coverage: 1,082 distinct patent families (2,905 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| JAK1 | Janus kinase 1 | Inhibition | 7.96 | 2.8% | P23458 |
| JAK2 | Janus kinase 2 | Inhibition | 5.62 | 0.7% | O60674 |
| JAK3 | Janus kinase 3 | Inhibition | 6.52 | 0.6% | P52333 |
| TYK2 | tyrosine kinase 2 | Inhibition | 5.59 | 0.8% | P29597 |
Broader ChEMBL bioactivity targets: 29 (assay-derived). Sample: Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Vascular endothelial growth factor receptor 1, Vascular endothelial growth factor receptor 3, Receptor-type tyrosine-protein kinase FLT3, Tyrosine-protein kinase JAK3, Voltage-gated inwardly rectifying potassium channel KCNH2, Mitogen-activated protein kinase 10, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, JAK3/JAK1, JAK2/JAK1, JAK1/JAK2/TYK2, JAK1/TYK2, JAK2/TYK2, Cytochrome P450 1A2, Interleukin-1 receptor-associated kinase 1, Non-receptor tyrosine-protein kinase TYK2, Cytochrome P450 2C19, AP2-associated protein kinase 1.
Bioactivity
ChEMBL activities: 167 potent at pChembl ≥ 5 of 178 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| JAK1 | 8.95 | IC50 | 1.13 | nM | CHEMBL_ACT_26279130 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_15112128 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_15747173 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_18722535 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_24788519 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_24954209 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_25044315 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_25555172 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_25848292 |
| JAK1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_26279080 |
| JAK1 | 7.96 | Kd | 11 | nM | CHEMBL_ACT_24958046 |
| JAK1 | 7.96 | Kd | 11 | nM | CHEMBL_ACT_26279084 |
| JAK1 | 7.78 | IC50 | 16.5 | nM | CHEMBL_ACT_25675095 |
| JAK2 | 7.6 | IC50 | 25 | nM | CHEMBL_ACT_15747169 |
| JAK2 | 7.6 | IC50 | 25 | nM | CHEMBL_ACT_26279081 |
| JAK1 | 7.58 | IC50 | 26.2 | nM | CHEMBL_ACT_22809389 |
| JAK2 | 7.55 | IC50 | 28 | nM | CHEMBL_ACT_18722582 |
| JAK2 | 7.55 | IC50 | 28 | nM | CHEMBL_ACT_24788497 |
| JAK2 | 7.55 | IC50 | 28 | nM | CHEMBL_ACT_24954210 |
| JAK2 | 7.55 | IC50 | 28 | nM | CHEMBL_ACT_25044316 |
| JAK2 | 7.55 | IC50 | 28 | nM | CHEMBL_ACT_25555173 |
| JAK2 | 7.55 | IC50 | 28 | nM | CHEMBL_ACT_25848298 |
| JAK2 | 7.5 | IC50 | 31.37 | nM | CHEMBL_ACT_16308961 |
| JAK2 | 7.5 | Kd | 32 | nM | CHEMBL_ACT_24958047 |
| JAK2 | 7.5 | Kd | 32 | nM | CHEMBL_ACT_26279085 |
| JAK2 | 7.5 | IC50 | 31.4 | nM | CHEMBL_ACT_28337330 |
| JAK1 | 7.48 | IC50 | 33 | nM | CHEMBL_ACT_24875751 |
| JAK2 | 7.39 | IC50 | 41.16 | nM | CHEMBL_ACT_16264194 |
| JAK1 | 7.34 | IC50 | 46 | nM | CHEMBL_ACT_28650065 |
| JAK1 | 7.33 | IC50 | 47.07 | nM | CHEMBL_ACT_16329737 |
| JAK1 | 7.33 | IC50 | 47.1 | nM | CHEMBL_ACT_28337297 |
| JAK1 | 7.32 | IC50 | 48.29 | nM | CHEMBL_ACT_16320054 |
| JAK1 | 7.3 | IC50 | 50.1 | nM | CHEMBL_ACT_16272805 |
| JAK1 | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_26981407 |
| JAK1 | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_28012808 |
| JAK1 | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_28111484 |
| JAK1 | 7.3 | IC50 | 50.3 | nM | CHEMBL_ACT_28249775 |
| JAK1 | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_28568312 |
| JAK2 | 7.26 | IC50 | 55.49 | nM | CHEMBL_ACT_16336150 |
| JAK2 | 7.26 | IC50 | 55 | nM | CHEMBL_ACT_28650068 |
| JAK1 | 7.25 | IC50 | 55.66 | nM | CHEMBL_ACT_16260032 |
| TYK2 | 7.18 | IC50 | 65.3 | nM | CHEMBL_ACT_22809518 |
| TYK2 | 7.14 | IC50 | 72.7 | nM | CHEMBL_ACT_16312063 |
| TYK2 | 7.14 | IC50 | 72.7 | nM | CHEMBL_ACT_28337366 |
| TYK2 | 7.13 | IC50 | 73.75 | nM | CHEMBL_ACT_16329115 |
| JAK2 | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_20687210 |
| JAK2 | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_28012811 |
| JAK2 | 7.13 | IC50 | 73.4 | nM | CHEMBL_ACT_28249778 |
| TYK2 | 7.11 | IC50 | 78 | nM | CHEMBL_ACT_28249784 |
| TYK2 | 7.1 | IC50 | 79.07 | nM | CHEMBL_ACT_16309230 |
| TYK2 | 7.06 | IC50 | 86.77 | nM | CHEMBL_ACT_16265865 |
| TYK2 | 6.95 | IC50 | 113 | nM | CHEMBL_ACT_24875865 |
| TYK2 | 6.95 | IC50 | 111.7 | nM | CHEMBL_ACT_25675068 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_15747161 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_18722634 |
| JAK1 | 6.94 | IC50 | 115 | nM | CHEMBL_ACT_20687196 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_24958049 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_24958050 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_25044318 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_25555175 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_25848306 |
| TYK2 | 6.94 | IC50 | 116 | nM | CHEMBL_ACT_26279083 |
| JAK2 | 6.91 | IC50 | 122 | nM | CHEMBL_ACT_24875789 |
| JAK1 | 6.83 | IC50 | 148 | nM | CHEMBL_ACT_15116678 |
| JAK3 | 6.83 | IC50 | 149.3 | nM | CHEMBL_ACT_16351799 |
| JAK1 | 6.83 | IC50 | 148 | nM | CHEMBL_ACT_26279092 |
| JAK3 | 6.83 | IC50 | 149 | nM | CHEMBL_ACT_28337357 |
| JAK1 | 6.81 | IC50 | 154 | nM | CHEMBL_ACT_15116677 |
| JAK1 | 6.81 | IC50 | 154 | nM | CHEMBL_ACT_26279089 |
| JAK2 | 6.78 | IC50 | 167.3 | nM | CHEMBL_ACT_16338363 |
| JAK2 | 6.77 | IC50 | 171 | nM | CHEMBL_ACT_22809433 |
| JAK1 | 6.75 | IC50 | 178 | nM | CHEMBL_ACT_24953747 |
| JAK1 | 6.75 | IC50 | 177.8 | nM | CHEMBL_ACT_26279090 |
| JAK3 | 6.75 | IC50 | 180 | nM | CHEMBL_ACT_28012814 |
| JAK3 | 6.75 | IC50 | 180 | nM | CHEMBL_ACT_28249781 |
| JAK3 | 6.73 | IC50 | 187.3 | nM | CHEMBL_ACT_16292529 |
| JAK2 | 6.73 | IC50 | 184.9 | nM | CHEMBL_ACT_25675135 |
| JAK3 | 6.72 | IC50 | 189.3 | nM | CHEMBL_ACT_16275767 |
| JAK3 | 6.71 | IC50 | 194.7 | nM | CHEMBL_ACT_16291702 |
| JAK3 | 6.69 | IC50 | 203 | nM | CHEMBL_ACT_26279091 |
| FLT4 | 6.56 | IC50 | 274 | nM | CHEMBL_ACT_15116721 |
| FLT4 | 6.56 | IC50 | 274 | nM | CHEMBL_ACT_24958045 |
| FLT4 | 6.56 | IC50 | 274 | nM | CHEMBL_ACT_26279194 |
| JAK3 | 6.52 | Kd | 300 | nM | CHEMBL_ACT_24958048 |
| JAK3 | 6.52 | Kd | 300 | nM | CHEMBL_ACT_26279086 |
| JAK1 | 6.51 | IC50 | 306.2 | nM | CHEMBL_ACT_24876145 |
| FLT3 | 6.47 | IC50 | 338 | nM | CHEMBL_ACT_15116720 |
| FLT3 | 6.47 | IC50 | 338 | nM | CHEMBL_ACT_24958044 |
| FLT3 | 6.47 | IC50 | 338 | nM | CHEMBL_ACT_26279193 |
| JAK1 | 6.46 | IC50 | 346.7 | nM | CHEMBL_ACT_26279093 |
| JAK1 | 6.44 | IC50 | 363 | nM | CHEMBL_ACT_14751995 |
| JAK2 | 6.39 | IC50 | 407.4 | nM | CHEMBL_ACT_24876139 |
| JAK1 | 6.36 | IC50 | 436 | nM | CHEMBL_ACT_15116679 |
| JAK1 | 6.36 | IC50 | 436 | nM | CHEMBL_ACT_26279094 |
| JAK2 | 6.34 | IC50 | 460 | nM | CHEMBL_ACT_26981410 |
| JAK2 | 6.34 | IC50 | 460 | nM | CHEMBL_ACT_28111487 |
| JAK2 | 6.34 | IC50 | 460 | nM | CHEMBL_ACT_28568315 |
| JAK1 | 6.33 | IC50 | 467.7 | nM | CHEMBL_ACT_26279095 |
| CSF1R | 6.31 | IC50 | 489 | nM | CHEMBL_ACT_15116722 |
| CSF1R | 6.31 | IC50 | 488.9 | nM | CHEMBL_ACT_24958043 |
Target pathways
Aggregated over 4 target gene(s): JAK1, JAK2, JAK3, TYK2.
Top Reactome pathways
86 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Interleukin-4 and Interleukin-13 signaling | 4 | JAK1, JAK2, JAK3, TYK2 |
| Interleukin-20 family signaling | 4 | JAK1, JAK2, JAK3, TYK2 |
| Potential therapeutics for SARS | 4 | JAK1, JAK2, JAK3, TYK2 |
| Interleukin-6 signaling | 3 | JAK1, JAK2, TYK2 |
| MAPK3 (ERK1) activation | 3 | JAK1, JAK2, TYK2 |
| MAPK1 (ERK2) activation | 3 | JAK1, JAK2, TYK2 |
| Cytokine Signaling in Immune system | 3 | JAK1, JAK2, JAK3 |
| Signal Transduction | 3 | JAK1, JAK2, JAK3 |
| Disease | 3 | JAK1, JAK2, JAK3 |
| Immune System | 3 | JAK1, JAK2, JAK3 |
| Signaling by Interleukins | 3 | JAK1, JAK2, JAK3 |
| Interleukin-2 family signaling | 3 | JAK1, JAK2, JAK3 |
| Interleukin-3, Interleukin-5 and GM-CSF signaling | 3 | JAK1, JAK2, JAK3 |
| Infectious disease | 3 | JAK1, JAK2, JAK3 |
| RAF/MAP kinase cascade | 3 | JAK1, JAK2, JAK3 |
| MAPK family signaling cascades | 3 | JAK1, JAK2, JAK3 |
| MAPK1/MAPK3 signaling | 3 | JAK1, JAK2, JAK3 |
| IL-6-type cytokine receptor ligand interactions | 3 | JAK1, JAK2, TYK2 |
| Interleukin-35 Signalling | 3 | JAK1, JAK2, TYK2 |
| Interleukin-12 signaling | 3 | JAK1, JAK2, TYK2 |
| Interleukin-27 signaling | 3 | JAK1, JAK2, TYK2 |
| Interleukin receptor SHC signaling | 3 | JAK1, JAK2, JAK3 |
| Signaling by CSF3 (G-CSF) | 3 | JAK1, JAK2, TYK2 |
| SARS-CoV Infections | 3 | JAK1, JAK2, JAK3 |
| Inactivation of CSF3 (G-CSF) signaling | 3 | JAK1, JAK2, TYK2 |
| Viral Infection Pathways | 3 | JAK1, JAK2, JAK3 |
| Activation of STAT3 by cadherin engagement | 3 | JAK1, JAK2, TYK2 |
| RAF-independent MAPK1/3 activation | 2 | JAK1, JAK2 |
| Interleukin-7 signaling | 2 | JAK1, JAK3 |
| Interleukin-12 family signaling | 2 | JAK1, JAK2 |
| Other interleukin signaling | 2 | JAK1, TYK2 |
| Interleukin-6 family signaling | 2 | JAK1, JAK2 |
| Interleukin-10 signaling | 2 | JAK1, TYK2 |
| Interferon gamma signaling | 2 | JAK1, JAK2 |
| Regulation of IFNG signaling | 2 | JAK1, JAK2 |
| Interleukin-15 signaling | 2 | JAK1, JAK3 |
| Interleukin-9 signaling | 2 | JAK1, JAK3 |
| Signaling by Receptor Tyrosine Kinases | 2 | JAK2, JAK3 |
| Interleukin-2 signaling | 2 | JAK1, JAK3 |
| Interleukin-23 signaling | 2 | JAK2, TYK2 |
| Interleukin-21 signaling | 2 | JAK1, JAK3 |
| Interferon alpha/beta signaling | 2 | JAK1, TYK2 |
| Regulation of IFNA/IFNB signaling | 2 | JAK1, TYK2 |
| Interferon Signaling | 2 | JAK1, JAK2 |
| SARS-CoV-2 activates/modulates innate and adaptive immune responses | 2 | JAK1, TYK2 |
| IFNG signaling activates MAPKs | 2 | JAK1, JAK2 |
| Evasion by RSV of host interferon responses | 2 | JAK1, TYK2 |
| Hemostasis | 1 | JAK2 |
| ISG15 antiviral mechanism | 1 | JAK1 |
| Antimicrobial mechanism of IFN-stimulated genes | 1 | JAK1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 4 |
| cell surface receptor signaling pathway via JAK-STAT | 4 |
| cytokine-mediated signaling pathway | 4 |
| cell differentiation | 4 |
| intracellular signal transduction | 4 |
| growth hormone receptor signaling pathway via JAK-STAT | 4 |
| regulation of cell-cell adhesion | 4 |
| type II interferon-mediated signaling pathway | 3 |
| cellular response to virus | 3 |
| regulation of receptor signaling pathway via JAK-STAT | 3 |
| regulation of alpha-beta T cell activation | 3 |
| interleukin-15-mediated signaling pathway | 2 |
| interleukin-4-mediated signaling pathway | 2 |
| interleukin-2-mediated signaling pathway | 2 |
| interleukin-7-mediated signaling pathway | 2 |
Indications & clinical
Indications
13 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| rheumatoid arthritis | 3 | MONDO:0008383 | EFO:0000685 |
| Crohn disease | 3 | MONDO:0005011 | EFO:0000384 |
| ulcerative colitis | 3 | MONDO:0005101 | EFO:0000729 |
| psoriatic arthritis | 3 | MONDO:0011849 | EFO:0003778 |
| ankylosing spondylitis | 3 | MONDO:0005306 | EFO:0003898 |
| spondyloarthropathy | 3 | MONDO:0005095 | EFO:0000706 |
| Sjogren syndrome | 2 | MONDO:0010030 | EFO:0000699 |
| cutaneous lupus erythematosus | 2 | MONDO:0005282 | EFO:0003834 |
| uveitis | 2 | MONDO:0020283 | EFO:1001231 |
| inflammatory bowel disease | 2 | MONDO:0005265 | EFO:0003767 |
| systemic lupus erythematosus | 2 | MONDO:0007915 | MONDO:0007915 |
| kidney disorder | 1 | MONDO:0005240 | EFO:0003086 |
| juvenile idiopathic arthritis | 1 | MONDO:0011429 | EFO:0002609 |
Clinical trials
Total trials: 53.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 19 |
| PHASE3 | 18 |
| PHASE1 | 9 |
| PHASE4 | 4 |
| Not specified | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04985435 | PHASE4 | RECRUITING | Better After CHoosing. Randomly Allocated or Patient Preference Based Treatment With Filgotinib or TNFi in RA (BACH) |
| NCT06527534 | PHASE4 | RECRUITING | Filgotinib Effect on Proteomic Profile and Micro-RNA Expression in Patients With Active Rheumatoid Arthritis (RA) |
| NCT06687551 | PHASE4 | NOT_YET_RECRUITING | JAK Inhibitor Dose TAPering Strategy Study |
| NCT05502731 | PHASE4 | UNKNOWN | Januse Kinase Inhibition With Filgotinib to Silence Autoreactive B Cells in Rheumatoid Arthritis |
| NCT02914535 | PHASE3 | ACTIVE_NOT_RECRUITING | Filgotinib in Long-Term Extension Study of Adults With Ulcerative Colitis |
| NCT05785611 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Effect of Filgotinib in Participants With Active Axial Spondyloarthritis |
| NCT06865417 | PHASE3 | RECRUITING | A Study Evaluating the Effects of Filgotinib in Children and Teenagers With Ulcerative Colitis |
| NCT07553182 | PHASE3 | RECRUITING | OLE Study With Filgotinib in JIA |
| NCT07554495 | PHASE3 | NOT_YET_RECRUITING | Safety, Tolerability, Pharmacokinetics, and Efficacy of Filgotinib for the Treatment of Polyarticular-course Juvenile Idiopathic Arthritis in Children and Adolescents |
| NCT02873936 | PHASE3 | COMPLETED | Filgotinib Versus Placebo in Adults With Active Rheumatoid Arthritis (RA) Who Have an Inadequate Response to Biologic Disease-modifying Anti-rheumatic Drug(s) (DMARDs) Treatment |
| NCT02886728 | PHASE3 | COMPLETED | Filgotinib Alone and in Combination With Methotrexate (MTX) in Adults With Moderately to Severely Active Rheumatoid Arthritis Who Are Naive to MTX Therapy |
| NCT02889796 | PHASE3 | COMPLETED | Filgotinib in Combination With Methotrexate in Adults With Moderately to Severely Active Rheumatoid Arthritis Who Have an Inadequate Response to Methotrexate |
| NCT02914522 | PHASE3 | COMPLETED | Study to Evaluate the Efficacy and Safety of Filgotinib in the Induction and Maintenance of Remission in Adults With Moderately to Severely Active Ulcerative Colitis |
| NCT02914561 | PHASE3 | COMPLETED | Filgotinib in the Induction and Maintenance of Remission in Adults With Moderately to Severely Active Crohn’s Disease |
| NCT02914600 | PHASE3 | TERMINATED | Filgotinib in Long-Term Extension Study of Adults With Crohn’s Disease |
| NCT03025308 | PHASE3 | COMPLETED | Long Term Extension Study to Assess the Safety and Efficacy of Filgotinib in Adults With Rheumatoid Arthritis |
| NCT04115748 | PHASE3 | TERMINATED | Study to Evaluate the Efficacy and Safety of Filgotinib in Participants With Active Psoriatic Arthritis Who Are Naive to Biologic DMARD Therapy |
| NCT04115839 | PHASE3 | TERMINATED | Study to Evaluate the Efficacy and Safety of Filgotinib in Participants With Active Psoriatic Arthritis Who Have an Inadequate Response or Are Intolerant to Biologic DMARD Therapy |
| NCT04483687 | PHASE3 | WITHDRAWN | Study to Evaluate the Efficacy and Safety of Filgotinib in Participants With Active Ankylosing Spondylitis Who Have an Inadequate Response to Biologic Disease-Modifying Antirheumatic Drug Therapy |
| NCT04483700 | PHASE3 | WITHDRAWN | Study to Evaluate the Efficacy and Safety of Filgotinib in Participants With Active Ankylosing Spondylitis Who Are Naive to Biologic Disease-Modifying Antirheumatic Drug Therapy |
| NCT05090410 | PHASE3 | UNKNOWN | Efficacy and Safety of Selective JAK 1 Inhibitor Filgotinib in Active Rheumatoid Arthritis Patients With Inadequate Response to Methotrexate |
| NCT05479058 | PHASE3 | TERMINATED | A Study Evaluating the Effect of Filgotinib Dose De-escalation in Participants With Ulcerative Colitis (UC) in Remission |
| NCT06285539 | PHASE2 | RECRUITING | Drug Rediscovery for Rare Immune Mediated Inflammatory Diseases |
| NCT01384422 | PHASE2 | COMPLETED | Safety and Preliminary Efficacy of GLPG0634 in Methotrexate-refractory Active Rheumatoid Arthritis Patients |
| NCT01668641 | PHASE2 | COMPLETED | Dose-ranging Study With GLPG0634 in Methotrexate-refractory Active Rheumatoid Arthritis Patients |
| NCT01888874 | PHASE2 | COMPLETED | Dose-finding Study of GLPG0634 as add-on to Methotrexate in Active Rheumatoid Arthritis Participants (DARWIN1) |
| NCT01894516 | PHASE2 | COMPLETED | Dose-finding Study of GLPG0634 as Monotherapy in Active Rheumatoid Arthritis (RA) Participants (DARWIN2) |
| NCT02048618 | PHASE2 | COMPLETED | Efficacy and Safety of GLPG0634 in Subjects With Active Crohn’s Disease |
| NCT02065700 | PHASE2 | COMPLETED | Long-term Follow-up Study of GLPG0634 in Active Rheumatoid Arthritis Participants |
| NCT02885181 | PHASE2 | COMPLETED | Safety, Tolerability, and Efficacy of GS-9876 in Participants With Active Rheumatoid Arthritis on Background Therapy With Methotrexate |
| NCT03046056 | PHASE2 | COMPLETED | Study to Evaluate the Efficacy and Safety of Filgotinib in the Treatment of Small Bowel Crohn’s Disease (SBCD) |
| NCT03077412 | PHASE2 | COMPLETED | Study to Evaluate the Efficacy and Safety of Filgotinib in the Treatment of Perianal Fistulizing Crohn’s Disease |
| NCT03100942 | PHASE2 | COMPLETED | Study to Assess Safety and Efficacy of Filgotinib, Lanraplenib and Tirabrutinib in Adults With Active Sjogren’s Syndrome |
| NCT03101670 | PHASE2 | COMPLETED | A Study to Assess Efficacy and Safety of Filgotinib in Active Psoriatic Arthritis |
| NCT03117270 | PHASE2 | COMPLETED | A Study to Assess Efficacy and Safety of Filgotinib in Ankylosing Spondylitis |
| NCT03134222 | PHASE2 | COMPLETED | Study to Evaluate Safety and Efficacy of Filgotinib and Lanraplenib in Females With Moderately-to-Severely Active Cutaneous Lupus Erythematosus (CLE) |
| NCT03201445 | PHASE2 | TERMINATED | Study to Evaluate the Testicular Safety of Filgotinib in Adult Males With Moderately to Severely Active Inflammatory Bowel Disease |
| NCT03207815 | PHASE2 | TERMINATED | Study to Evaluate the Efficacy and Safety of Filgotinib in Adults With Active Noninfectious Uveitis |
| NCT03285711 | PHASE2 | COMPLETED | Study to Evaluate the Safety and Efficacy of Filgotinib and Lanraplenib in Adults With Lupus Membranous Nephropathy (LMN) |
| NCT03320876 | PHASE2 | TERMINATED | An Open-label, Long-term Extension Study With Filgotinib in Active Psoriatic Arthritis. |
| NCT03926195 | PHASE2 | COMPLETED | Study to Evaluate the Effect of Filgotinib on Semen Parameters in Adult Males With Active Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, or Non-radiographic Axial Spondyloarthritis |
| NCT06222034 | PHASE1 | RECRUITING | Study to Measure Filgotinib in the Blood of Children and Teenagers With Arthritis Taking Filgotinib (SCALESIA) |
| NCT01179581 | PHASE1 | COMPLETED | First-in-Human Single Ascending and Multiple Dose of GLPG0634 |
| NCT01419990 | PHASE1 | COMPLETED | Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Oral Doses of GLPG0634 in Healthy Subjects |
| NCT01798979 | PHASE1 | COMPLETED | A Phase I, Open Interaction Study Between GLPG0634 and Midazolam in Healthy Subjects |
| NCT02084199 | PHASE1 | COMPLETED | Study to Evaluate GLPG0634 in Subjects With Renal Impairment Compared to Healthy Subjects |
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Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
126 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| DEUCRAVACITINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| Pazopanib | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| RITLECITINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| ABROCITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| BARICITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| MOMELOTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| PACRITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| PEFICITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| RUXOLITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| SUNITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| TOFACITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| UPADACITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3, TYK2 |
| BREPOCITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| DELGOCITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| DOVITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| ITACITINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| LESTAURTINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3, TYK2 |
| AT-9283 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| ATINVICITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| AZD-1480 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| BMS-911543 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| CC-401 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| CERDULATINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| DECERNOTINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GANDOTINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GOLIDOCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| GUSACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| IFIDANCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| IZENCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| NEZULCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| NS-018 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| OCLACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| R-406 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| ROPSACITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| SOLCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| SU-014813 | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| TOZASERTIB | ChEMBL | Phase 2 | JAK1, JAK2, JAK3, TYK2 |
| Afatinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Gefitinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Idelalisib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| Selumetinib | PubChem | Approved | JAK1, JAK2, JAK3, TYK2 |
| dacomitinib | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK3, TYK2 |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | JAK1, JAK2, TYK2 |
| AXITINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| CERITINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3 |
| DASATINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2, JAK3 |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | JAK2, JAK3, TYK2 |
| ABIVERTINIB | ChEMBL | Phase 3 | JAK1, JAK2, JAK3 |
| ALVOCIDIB | ChEMBL | Phase 3 | JAK2, JAK3, TYK2 |
| DEFACTINIB | ChEMBL | Phase 3 | JAK2, JAK3, TYK2 |
| BMS-919373 | ChEMBL | Phase 2 | JAK2, JAK3, TYK2 |
| CENISERTIB | ChEMBL | Phase 2 | JAK2, JAK3, TYK2 |
| LONDAMOCITINIB | ChEMBL | Phase 2 | JAK1, JAK2, TYK2 |
| belumosudil | PubChem | Approved | JAK2, JAK3, TYK2 |
| Fostamatinib | PubChem | Approved | JAK1, JAK2, TYK2 |
| Trametinib | PubChem | Approved | JAK1, JAK2, TYK2 |
| CRAVACITINIB | ChEMBL | Phase 4 (approved) | JAK2, TYK2 |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | JAK2, TYK2 |
| PONATINIB | ChEMBL | Phase 4 (approved) | JAK1, JAK2 |
| IVARMACITINIB | ChEMBL | Phase 3 | JAK1, JAK2 |
| POVORCITINIB | ChEMBL | Phase 3 | JAK1, JAK2 |
| ADAVOSERTIB | ChEMBL | Phase 2 | JAK2, JAK3 |
| FORETINIB | ChEMBL | Phase 2 | JAK2, TYK2 |
| ILORASERTIB | ChEMBL | Phase 2 | JAK2, TYK2 |
| LAUROGUADINE | ChEMBL | Phase 2 | JAK2, JAK3 |
| LEPZACITINIB | ChEMBL | Phase 2 | JAK1, JAK3 |
| PELITINIB | ChEMBL | Phase 2 | JAK2, JAK3 |
| PICTILISIB | ChEMBL | Phase 2 | JAK1, TYK2 |
| REBASTINIB | ChEMBL | Phase 2 | JAK1, JAK2 |
| SOTRASTAURIN | ChEMBL | Phase 2 | JAK1, JAK3 |
| SPEBRUTINIB | ChEMBL | Phase 2 | JAK2, JAK3 |
| TG100-115 | ChEMBL | Phase 2 | JAK1, TYK2 |
| ZOTIRACICLIB | ChEMBL | Phase 2 | JAK1, JAK2 |
| Binimetinib | PubChem | Approved | JAK1, TYK2 |
| regorafenib | PubChem | Approved | JAK1, TYK2 |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | JAK3 |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | JAK2 |
| DABRAFENIB | ChEMBL | Phase 4 (approved) | JAK2 |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | JAK3 |
| LORLATINIB | ChEMBL | Phase 4 (approved) | JAK2 |
| NERATINIB | ChEMBL | Phase 4 (approved) | JAK3 |
| NICLOSAMIDE | ChEMBL | Phase 4 (approved) | JAK2 |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | JAK3 |
| PALBOCICLIB | ChEMBL | Phase 4 (approved) | JAK3 |
| PRALSETINIB | ChEMBL | Phase 4 (approved) | JAK2 |
| REPOTRECTINIB | ChEMBL | Phase 4 (approved) | JAK2 |
| SORAFENIB | ChEMBL | Phase 4 (approved) | JAK3 |
| TRIAMTERENE | ChEMBL | Phase 4 (approved) | JAK2 |
| ZANUBRUTINIB | ChEMBL | Phase 4 (approved) | JAK3 |
| CANERTINIB | ChEMBL | Phase 3 | JAK3 |
| DACTOLISIB | ChEMBL | Phase 3 | JAK3 |
| ENTOSPLETINIB | ChEMBL | Phase 3 | JAK2 |
| ENZASTAURIN | ChEMBL | Phase 3 | JAK3 |
| MOTESANIB | ChEMBL | Phase 3 | JAK1 |
Related Atlas pages
- Genes: JAK1, JAK2, JAK3, TYK2
- In clinical trials for: rheumatoid arthritis, Crohn disease, ulcerative colitis, psoriatic arthritis, ankylosing spondylitis, spondyloarthropathy, Sjogren syndrome, cutaneous lupus erythematosus, uveitis, inflammatory bowel disease, systemic lupus erythematosus
- Drugs: Crizotinib, Deucravacitinib, Pazopanib, Ritlecitinib, Abrocitinib, Baricitinib, Fedratinib, Midostaurin, Momelotinib, Nintedanib, Pacritinib, Peficitinib, Ruxolitinib, Sunitinib, Tofacitinib, Upadacitinib, Brepocitinib, Delgocitinib, Dovitinib, Itacitinib, Lestaurtinib, Afatinib, Gefitinib, Idelalisib, Selumetinib, dacomitinib, Imatinib, Axitinib, Bosutinib, Ceritinib, Dasatinib, Entrectinib, Erlotinib, Abivertinib, Alvocidib, Defactinib, belumosudil, Fostamatinib, Trametinib, Infigratinib, Ponatinib, Ivarmacitinib, Povorcitinib, Binimetinib, regorafenib, Acalabrutinib, Brigatinib, Dabrafenib, Ibrutinib, Lorlatinib, Neratinib, Niclosamide, Osimertinib, Palbociclib, Pralsetinib, Repotrectinib, Sorafenib, Triamterene, Zanubrutinib, Canertinib, Dactolisib, Entospletinib, Enzastaurin, Motesanib