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

FieldValue
ChEMBL IDCHEMBL3301607
NameFilgotinib
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID49831257
ATCL04AF04
Molecular formulaC21H23N5O3S
Molecular weight425.5
InChIKeyRIJLVEAXPNLDTC-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).

GeneTargetActionpAffinityCancer dependencyUniProt
JAK1Janus kinase 1Inhibition7.962.8%P23458
JAK2Janus kinase 2Inhibition5.620.7%O60674
JAK3Janus kinase 3Inhibition6.520.6%P52333
TYK2tyrosine kinase 2Inhibition5.590.8%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):

TargetpChemblTypeValueUnitActivity ID
JAK18.95IC501.13nMCHEMBL_ACT_26279130
JAK18IC5010nMCHEMBL_ACT_15112128
JAK18IC5010nMCHEMBL_ACT_15747173
JAK18IC5010nMCHEMBL_ACT_18722535
JAK18IC5010nMCHEMBL_ACT_24788519
JAK18IC5010nMCHEMBL_ACT_24954209
JAK18IC5010nMCHEMBL_ACT_25044315
JAK18IC5010nMCHEMBL_ACT_25555172
JAK18IC5010nMCHEMBL_ACT_25848292
JAK18IC5010nMCHEMBL_ACT_26279080
JAK17.96Kd11nMCHEMBL_ACT_24958046
JAK17.96Kd11nMCHEMBL_ACT_26279084
JAK17.78IC5016.5nMCHEMBL_ACT_25675095
JAK27.6IC5025nMCHEMBL_ACT_15747169
JAK27.6IC5025nMCHEMBL_ACT_26279081
JAK17.58IC5026.2nMCHEMBL_ACT_22809389
JAK27.55IC5028nMCHEMBL_ACT_18722582
JAK27.55IC5028nMCHEMBL_ACT_24788497
JAK27.55IC5028nMCHEMBL_ACT_24954210
JAK27.55IC5028nMCHEMBL_ACT_25044316
JAK27.55IC5028nMCHEMBL_ACT_25555173
JAK27.55IC5028nMCHEMBL_ACT_25848298
JAK27.5IC5031.37nMCHEMBL_ACT_16308961
JAK27.5Kd32nMCHEMBL_ACT_24958047
JAK27.5Kd32nMCHEMBL_ACT_26279085
JAK27.5IC5031.4nMCHEMBL_ACT_28337330
JAK17.48IC5033nMCHEMBL_ACT_24875751
JAK27.39IC5041.16nMCHEMBL_ACT_16264194
JAK17.34IC5046nMCHEMBL_ACT_28650065
JAK17.33IC5047.07nMCHEMBL_ACT_16329737
JAK17.33IC5047.1nMCHEMBL_ACT_28337297
JAK17.32IC5048.29nMCHEMBL_ACT_16320054
JAK17.3IC5050.1nMCHEMBL_ACT_16272805
JAK17.3IC5050nMCHEMBL_ACT_26981407
JAK17.3IC5050nMCHEMBL_ACT_28012808
JAK17.3IC5050nMCHEMBL_ACT_28111484
JAK17.3IC5050.3nMCHEMBL_ACT_28249775
JAK17.3IC5050nMCHEMBL_ACT_28568312
JAK27.26IC5055.49nMCHEMBL_ACT_16336150
JAK27.26IC5055nMCHEMBL_ACT_28650068
JAK17.25IC5055.66nMCHEMBL_ACT_16260032
TYK27.18IC5065.3nMCHEMBL_ACT_22809518
TYK27.14IC5072.7nMCHEMBL_ACT_16312063
TYK27.14IC5072.7nMCHEMBL_ACT_28337366
TYK27.13IC5073.75nMCHEMBL_ACT_16329115
JAK27.13IC5074nMCHEMBL_ACT_20687210
JAK27.13IC5074nMCHEMBL_ACT_28012811
JAK27.13IC5073.4nMCHEMBL_ACT_28249778
TYK27.11IC5078nMCHEMBL_ACT_28249784
TYK27.1IC5079.07nMCHEMBL_ACT_16309230
TYK27.06IC5086.77nMCHEMBL_ACT_16265865
TYK26.95IC50113nMCHEMBL_ACT_24875865
TYK26.95IC50111.7nMCHEMBL_ACT_25675068
TYK26.94IC50116nMCHEMBL_ACT_15747161
TYK26.94IC50116nMCHEMBL_ACT_18722634
JAK16.94IC50115nMCHEMBL_ACT_20687196
TYK26.94IC50116nMCHEMBL_ACT_24958049
TYK26.94IC50116nMCHEMBL_ACT_24958050
TYK26.94IC50116nMCHEMBL_ACT_25044318
TYK26.94IC50116nMCHEMBL_ACT_25555175
TYK26.94IC50116nMCHEMBL_ACT_25848306
TYK26.94IC50116nMCHEMBL_ACT_26279083
JAK26.91IC50122nMCHEMBL_ACT_24875789
JAK16.83IC50148nMCHEMBL_ACT_15116678
JAK36.83IC50149.3nMCHEMBL_ACT_16351799
JAK16.83IC50148nMCHEMBL_ACT_26279092
JAK36.83IC50149nMCHEMBL_ACT_28337357
JAK16.81IC50154nMCHEMBL_ACT_15116677
JAK16.81IC50154nMCHEMBL_ACT_26279089
JAK26.78IC50167.3nMCHEMBL_ACT_16338363
JAK26.77IC50171nMCHEMBL_ACT_22809433
JAK16.75IC50178nMCHEMBL_ACT_24953747
JAK16.75IC50177.8nMCHEMBL_ACT_26279090
JAK36.75IC50180nMCHEMBL_ACT_28012814
JAK36.75IC50180nMCHEMBL_ACT_28249781
JAK36.73IC50187.3nMCHEMBL_ACT_16292529
JAK26.73IC50184.9nMCHEMBL_ACT_25675135
JAK36.72IC50189.3nMCHEMBL_ACT_16275767
JAK36.71IC50194.7nMCHEMBL_ACT_16291702
JAK36.69IC50203nMCHEMBL_ACT_26279091
FLT46.56IC50274nMCHEMBL_ACT_15116721
FLT46.56IC50274nMCHEMBL_ACT_24958045
FLT46.56IC50274nMCHEMBL_ACT_26279194
JAK36.52Kd300nMCHEMBL_ACT_24958048
JAK36.52Kd300nMCHEMBL_ACT_26279086
JAK16.51IC50306.2nMCHEMBL_ACT_24876145
FLT36.47IC50338nMCHEMBL_ACT_15116720
FLT36.47IC50338nMCHEMBL_ACT_24958044
FLT36.47IC50338nMCHEMBL_ACT_26279193
JAK16.46IC50346.7nMCHEMBL_ACT_26279093
JAK16.44IC50363nMCHEMBL_ACT_14751995
JAK26.39IC50407.4nMCHEMBL_ACT_24876139
JAK16.36IC50436nMCHEMBL_ACT_15116679
JAK16.36IC50436nMCHEMBL_ACT_26279094
JAK26.34IC50460nMCHEMBL_ACT_26981410
JAK26.34IC50460nMCHEMBL_ACT_28111487
JAK26.34IC50460nMCHEMBL_ACT_28568315
JAK16.33IC50467.7nMCHEMBL_ACT_26279095
CSF1R6.31IC50489nMCHEMBL_ACT_15116722
CSF1R6.31IC50488.9nMCHEMBL_ACT_24958043

Target pathways

Aggregated over 4 target gene(s): JAK1, JAK2, JAK3, TYK2.

Top Reactome pathways

86 total, by targets touching each:

PathwayTargetsGenes
Interleukin-4 and Interleukin-13 signaling4JAK1, JAK2, JAK3, TYK2
Interleukin-20 family signaling4JAK1, JAK2, JAK3, TYK2
Potential therapeutics for SARS4JAK1, JAK2, JAK3, TYK2
Interleukin-6 signaling3JAK1, JAK2, TYK2
MAPK3 (ERK1) activation3JAK1, JAK2, TYK2
MAPK1 (ERK2) activation3JAK1, JAK2, TYK2
Cytokine Signaling in Immune system3JAK1, JAK2, JAK3
Signal Transduction3JAK1, JAK2, JAK3
Disease3JAK1, JAK2, JAK3
Immune System3JAK1, JAK2, JAK3
Signaling by Interleukins3JAK1, JAK2, JAK3
Interleukin-2 family signaling3JAK1, JAK2, JAK3
Interleukin-3, Interleukin-5 and GM-CSF signaling3JAK1, JAK2, JAK3
Infectious disease3JAK1, JAK2, JAK3
RAF/MAP kinase cascade3JAK1, JAK2, JAK3
MAPK family signaling cascades3JAK1, JAK2, JAK3
MAPK1/MAPK3 signaling3JAK1, JAK2, JAK3
IL-6-type cytokine receptor ligand interactions3JAK1, JAK2, TYK2
Interleukin-35 Signalling3JAK1, JAK2, TYK2
Interleukin-12 signaling3JAK1, JAK2, TYK2
Interleukin-27 signaling3JAK1, JAK2, TYK2
Interleukin receptor SHC signaling3JAK1, JAK2, JAK3
Signaling by CSF3 (G-CSF)3JAK1, JAK2, TYK2
SARS-CoV Infections3JAK1, JAK2, JAK3
Inactivation of CSF3 (G-CSF) signaling3JAK1, JAK2, TYK2
Viral Infection Pathways3JAK1, JAK2, JAK3
Activation of STAT3 by cadherin engagement3JAK1, JAK2, TYK2
RAF-independent MAPK1/3 activation2JAK1, JAK2
Interleukin-7 signaling2JAK1, JAK3
Interleukin-12 family signaling2JAK1, JAK2
Other interleukin signaling2JAK1, TYK2
Interleukin-6 family signaling2JAK1, JAK2
Interleukin-10 signaling2JAK1, TYK2
Interferon gamma signaling2JAK1, JAK2
Regulation of IFNG signaling2JAK1, JAK2
Interleukin-15 signaling2JAK1, JAK3
Interleukin-9 signaling2JAK1, JAK3
Signaling by Receptor Tyrosine Kinases2JAK2, JAK3
Interleukin-2 signaling2JAK1, JAK3
Interleukin-23 signaling2JAK2, TYK2
Interleukin-21 signaling2JAK1, JAK3
Interferon alpha/beta signaling2JAK1, TYK2
Regulation of IFNA/IFNB signaling2JAK1, TYK2
Interferon Signaling2JAK1, JAK2
SARS-CoV-2 activates/modulates innate and adaptive immune responses2JAK1, TYK2
IFNG signaling activates MAPKs2JAK1, JAK2
Evasion by RSV of host interferon responses2JAK1, TYK2
Hemostasis1JAK2
ISG15 antiviral mechanism1JAK1
Antimicrobial mechanism of IFN-stimulated genes1JAK1

Dominant GO biological processes

GO termTargets
protein phosphorylation4
cell surface receptor signaling pathway via JAK-STAT4
cytokine-mediated signaling pathway4
cell differentiation4
intracellular signal transduction4
growth hormone receptor signaling pathway via JAK-STAT4
regulation of cell-cell adhesion4
type II interferon-mediated signaling pathway3
cellular response to virus3
regulation of receptor signaling pathway via JAK-STAT3
regulation of alpha-beta T cell activation3
interleukin-15-mediated signaling pathway2
interleukin-4-mediated signaling pathway2
interleukin-2-mediated signaling pathway2
interleukin-7-mediated signaling pathway2

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)PhaseMONDOEFO
rheumatoid arthritis3MONDO:0008383EFO:0000685
Crohn disease3MONDO:0005011EFO:0000384
ulcerative colitis3MONDO:0005101EFO:0000729
psoriatic arthritis3MONDO:0011849EFO:0003778
ankylosing spondylitis3MONDO:0005306EFO:0003898
spondyloarthropathy3MONDO:0005095EFO:0000706
Sjogren syndrome2MONDO:0010030EFO:0000699
cutaneous lupus erythematosus2MONDO:0005282EFO:0003834
uveitis2MONDO:0020283EFO:1001231
inflammatory bowel disease2MONDO:0005265EFO:0003767
systemic lupus erythematosus2MONDO:0007915MONDO:0007915
kidney disorder1MONDO:0005240EFO:0003086
juvenile idiopathic arthritis1MONDO:0011429EFO:0002609

Clinical trials

Total trials: 53.

Phase distribution

PhaseTrials
PHASE219
PHASE318
PHASE19
PHASE44
Not specified3

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04985435PHASE4RECRUITINGBetter After CHoosing. Randomly Allocated or Patient Preference Based Treatment With Filgotinib or TNFi in RA (BACH)
NCT06527534PHASE4RECRUITINGFilgotinib Effect on Proteomic Profile and Micro-RNA Expression in Patients With Active Rheumatoid Arthritis (RA)
NCT06687551PHASE4NOT_YET_RECRUITINGJAK Inhibitor Dose TAPering Strategy Study
NCT05502731PHASE4UNKNOWNJanuse Kinase Inhibition With Filgotinib to Silence Autoreactive B Cells in Rheumatoid Arthritis
NCT02914535PHASE3ACTIVE_NOT_RECRUITINGFilgotinib in Long-Term Extension Study of Adults With Ulcerative Colitis
NCT05785611PHASE3ACTIVE_NOT_RECRUITINGA Study Evaluating the Effect of Filgotinib in Participants With Active Axial Spondyloarthritis
NCT06865417PHASE3RECRUITINGA Study Evaluating the Effects of Filgotinib in Children and Teenagers With Ulcerative Colitis
NCT07553182PHASE3RECRUITINGOLE Study With Filgotinib in JIA
NCT07554495PHASE3NOT_YET_RECRUITINGSafety, Tolerability, Pharmacokinetics, and Efficacy of Filgotinib for the Treatment of Polyarticular-course Juvenile Idiopathic Arthritis in Children and Adolescents
NCT02873936PHASE3COMPLETEDFilgotinib Versus Placebo in Adults With Active Rheumatoid Arthritis (RA) Who Have an Inadequate Response to Biologic Disease-modifying Anti-rheumatic Drug(s) (DMARDs) Treatment
NCT02886728PHASE3COMPLETEDFilgotinib Alone and in Combination With Methotrexate (MTX) in Adults With Moderately to Severely Active Rheumatoid Arthritis Who Are Naive to MTX Therapy
NCT02889796PHASE3COMPLETEDFilgotinib in Combination With Methotrexate in Adults With Moderately to Severely Active Rheumatoid Arthritis Who Have an Inadequate Response to Methotrexate
NCT02914522PHASE3COMPLETEDStudy to Evaluate the Efficacy and Safety of Filgotinib in the Induction and Maintenance of Remission in Adults With Moderately to Severely Active Ulcerative Colitis
NCT02914561PHASE3COMPLETEDFilgotinib in the Induction and Maintenance of Remission in Adults With Moderately to Severely Active Crohn’s Disease
NCT02914600PHASE3TERMINATEDFilgotinib in Long-Term Extension Study of Adults With Crohn’s Disease
NCT03025308PHASE3COMPLETEDLong Term Extension Study to Assess the Safety and Efficacy of Filgotinib in Adults With Rheumatoid Arthritis
NCT04115748PHASE3TERMINATEDStudy to Evaluate the Efficacy and Safety of Filgotinib in Participants With Active Psoriatic Arthritis Who Are Naive to Biologic DMARD Therapy
NCT04115839PHASE3TERMINATEDStudy 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
NCT04483687PHASE3WITHDRAWNStudy 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
NCT04483700PHASE3WITHDRAWNStudy to Evaluate the Efficacy and Safety of Filgotinib in Participants With Active Ankylosing Spondylitis Who Are Naive to Biologic Disease-Modifying Antirheumatic Drug Therapy
NCT05090410PHASE3UNKNOWNEfficacy and Safety of Selective JAK 1 Inhibitor Filgotinib in Active Rheumatoid Arthritis Patients With Inadequate Response to Methotrexate
NCT05479058PHASE3TERMINATEDA Study Evaluating the Effect of Filgotinib Dose De-escalation in Participants With Ulcerative Colitis (UC) in Remission
NCT06285539PHASE2RECRUITINGDrug Rediscovery for Rare Immune Mediated Inflammatory Diseases
NCT01384422PHASE2COMPLETEDSafety and Preliminary Efficacy of GLPG0634 in Methotrexate-refractory Active Rheumatoid Arthritis Patients
NCT01668641PHASE2COMPLETEDDose-ranging Study With GLPG0634 in Methotrexate-refractory Active Rheumatoid Arthritis Patients
NCT01888874PHASE2COMPLETEDDose-finding Study of GLPG0634 as add-on to Methotrexate in Active Rheumatoid Arthritis Participants (DARWIN1)
NCT01894516PHASE2COMPLETEDDose-finding Study of GLPG0634 as Monotherapy in Active Rheumatoid Arthritis (RA) Participants (DARWIN2)
NCT02048618PHASE2COMPLETEDEfficacy and Safety of GLPG0634 in Subjects With Active Crohn’s Disease
NCT02065700PHASE2COMPLETEDLong-term Follow-up Study of GLPG0634 in Active Rheumatoid Arthritis Participants
NCT02885181PHASE2COMPLETEDSafety, Tolerability, and Efficacy of GS-9876 in Participants With Active Rheumatoid Arthritis on Background Therapy With Methotrexate
NCT03046056PHASE2COMPLETEDStudy to Evaluate the Efficacy and Safety of Filgotinib in the Treatment of Small Bowel Crohn’s Disease (SBCD)
NCT03077412PHASE2COMPLETEDStudy to Evaluate the Efficacy and Safety of Filgotinib in the Treatment of Perianal Fistulizing Crohn’s Disease
NCT03100942PHASE2COMPLETEDStudy to Assess Safety and Efficacy of Filgotinib, Lanraplenib and Tirabrutinib in Adults With Active Sjogren’s Syndrome
NCT03101670PHASE2COMPLETEDA Study to Assess Efficacy and Safety of Filgotinib in Active Psoriatic Arthritis
NCT03117270PHASE2COMPLETEDA Study to Assess Efficacy and Safety of Filgotinib in Ankylosing Spondylitis
NCT03134222PHASE2COMPLETEDStudy to Evaluate Safety and Efficacy of Filgotinib and Lanraplenib in Females With Moderately-to-Severely Active Cutaneous Lupus Erythematosus (CLE)
NCT03201445PHASE2TERMINATEDStudy to Evaluate the Testicular Safety of Filgotinib in Adult Males With Moderately to Severely Active Inflammatory Bowel Disease
NCT03207815PHASE2TERMINATEDStudy to Evaluate the Efficacy and Safety of Filgotinib in Adults With Active Noninfectious Uveitis
NCT03285711PHASE2COMPLETEDStudy to Evaluate the Safety and Efficacy of Filgotinib and Lanraplenib in Adults With Lupus Membranous Nephropathy (LMN)
NCT03320876PHASE2TERMINATEDAn Open-label, Long-term Extension Study With Filgotinib in Active Psoriatic Arthritis.
NCT03926195PHASE2COMPLETEDStudy 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
NCT06222034PHASE1RECRUITINGStudy to Measure Filgotinib in the Blood of Children and Teenagers With Arthritis Taking Filgotinib (SCALESIA)
NCT01179581PHASE1COMPLETEDFirst-in-Human Single Ascending and Multiple Dose of GLPG0634
NCT01419990PHASE1COMPLETEDSafety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Oral Doses of GLPG0634 in Healthy Subjects
NCT01798979PHASE1COMPLETEDA Phase I, Open Interaction Study Between GLPG0634 and Midazolam in Healthy Subjects
NCT02084199PHASE1COMPLETEDStudy to Evaluate GLPG0634 in Subjects With Renal Impairment Compared to Healthy Subjects
NCT02162355PHASE1COMPLETEDMultiple Ascending Dose Study of GLPG0634 in Japanese and Caucasian Healthy Subjects
NCT03417778PHASE1COMPLETEDStudy to Evaluate the Pharmacokinetics of Filgotinib in Participants With Impaired Hepatic Function
NCT04608344PHASE1COMPLETEDStudy to Evaluate Organic Anion Transporting Polypeptide (OATP) Transporter-Mediated Drug-Drug Interactions Between Filgotinib and Statins as Probe Drugs in Healthy Participants
NCT06043739PHASE1COMPLETEDRelative Bioavailability and Effect of Food Study With an Oral Mini-tablet Formulation of Filgotinib in Healthy Subjects
NCT04871919Not specifiedACTIVE_NOT_RECRUITINGProspective Observational Study of Filgotinib in Subjects With Rheumatoid Arthritis
NCT05817942Not specifiedACTIVE_NOT_RECRUITINGProspective Observational Study of Effectiveness and Safety of Filgotinib in Participants With Ulcerative Colitis (UC)
NCT05323591Not specifiedCOMPLETEDProspective Observational Study of Filgotinib in Participants With Rheumatoid Arthritis in France

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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:

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
DEUCRAVACITINIBChEMBL + PubChemPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
PazopanibChEMBL + PubChemPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
RITLECITINIBChEMBL + PubChemPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
ABROCITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
BARICITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
FEDRATINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
MIDOSTAURINChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
MOMELOTINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
NINTEDANIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
PACRITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
PEFICITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
RUXOLITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
SUNITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
TOFACITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
UPADACITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3, TYK2
BREPOCITINIBChEMBLPhase 3JAK1, JAK2, JAK3, TYK2
DELGOCITINIBChEMBLPhase 3JAK1, JAK2, JAK3, TYK2
DOVITINIBChEMBLPhase 3JAK1, JAK2, JAK3, TYK2
ITACITINIBChEMBLPhase 3JAK1, JAK2, JAK3, TYK2
LESTAURTINIBChEMBLPhase 3JAK1, JAK2, JAK3, TYK2
AT-9283ChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
ATINVICITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
AZD-1480ChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
BMS-911543ChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
CC-401ChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
CERDULATINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
DECERNOTINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
GANDOTINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
GOLIDOCITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
GUSACITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
IFIDANCITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
IZENCITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
NEZULCITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
NS-018ChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
OCLACITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
R-406ChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
ROPSACITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
SOLCITINIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
SU-014813ChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
TOZASERTIBChEMBLPhase 2JAK1, JAK2, JAK3, TYK2
AfatinibPubChemApprovedJAK1, JAK2, JAK3, TYK2
GefitinibPubChemApprovedJAK1, JAK2, JAK3, TYK2
IdelalisibPubChemApprovedJAK1, JAK2, JAK3, TYK2
SelumetinibPubChemApprovedJAK1, JAK2, JAK3, TYK2
dacomitinibChEMBL + PubChemPhase 4 (approved)JAK1, JAK3, TYK2
IMATINIBChEMBL + PubChemPhase 4 (approved)JAK1, JAK2, TYK2
AXITINIBChEMBLPhase 4 (approved)JAK2, JAK3, TYK2
BOSUTINIBChEMBLPhase 4 (approved)JAK2, JAK3, TYK2
CERITINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3
DASATINIBChEMBLPhase 4 (approved)JAK2, JAK3, TYK2
ENTRECTINIBChEMBLPhase 4 (approved)JAK1, JAK2, JAK3
ERLOTINIBChEMBLPhase 4 (approved)JAK2, JAK3, TYK2
ABIVERTINIBChEMBLPhase 3JAK1, JAK2, JAK3
ALVOCIDIBChEMBLPhase 3JAK2, JAK3, TYK2
DEFACTINIBChEMBLPhase 3JAK2, JAK3, TYK2
BMS-919373ChEMBLPhase 2JAK2, JAK3, TYK2
CENISERTIBChEMBLPhase 2JAK2, JAK3, TYK2
LONDAMOCITINIBChEMBLPhase 2JAK1, JAK2, TYK2
belumosudilPubChemApprovedJAK2, JAK3, TYK2
FostamatinibPubChemApprovedJAK1, JAK2, TYK2
TrametinibPubChemApprovedJAK1, JAK2, TYK2
CRAVACITINIBChEMBLPhase 4 (approved)JAK2, TYK2
INFIGRATINIBChEMBLPhase 4 (approved)JAK2, TYK2
PONATINIBChEMBLPhase 4 (approved)JAK1, JAK2
IVARMACITINIBChEMBLPhase 3JAK1, JAK2
POVORCITINIBChEMBLPhase 3JAK1, JAK2
ADAVOSERTIBChEMBLPhase 2JAK2, JAK3
FORETINIBChEMBLPhase 2JAK2, TYK2
ILORASERTIBChEMBLPhase 2JAK2, TYK2
LAUROGUADINEChEMBLPhase 2JAK2, JAK3
LEPZACITINIBChEMBLPhase 2JAK1, JAK3
PELITINIBChEMBLPhase 2JAK2, JAK3
PICTILISIBChEMBLPhase 2JAK1, TYK2
REBASTINIBChEMBLPhase 2JAK1, JAK2
SOTRASTAURINChEMBLPhase 2JAK1, JAK3
SPEBRUTINIBChEMBLPhase 2JAK2, JAK3
TG100-115ChEMBLPhase 2JAK1, TYK2
ZOTIRACICLIBChEMBLPhase 2JAK1, JAK2
BinimetinibPubChemApprovedJAK1, TYK2
regorafenibPubChemApprovedJAK1, TYK2
ACALABRUTINIBChEMBLPhase 4 (approved)JAK3
BRIGATINIBChEMBLPhase 4 (approved)JAK2
DABRAFENIBChEMBLPhase 4 (approved)JAK2
IBRUTINIBChEMBLPhase 4 (approved)JAK3
LORLATINIBChEMBLPhase 4 (approved)JAK2
NERATINIBChEMBLPhase 4 (approved)JAK3
NICLOSAMIDEChEMBLPhase 4 (approved)JAK2
OSIMERTINIBChEMBLPhase 4 (approved)JAK3
PALBOCICLIBChEMBLPhase 4 (approved)JAK3
PRALSETINIBChEMBLPhase 4 (approved)JAK2
REPOTRECTINIBChEMBLPhase 4 (approved)JAK2
SORAFENIBChEMBLPhase 4 (approved)JAK3
TRIAMTERENEChEMBLPhase 4 (approved)JAK2
ZANUBRUTINIBChEMBLPhase 4 (approved)JAK3
CANERTINIBChEMBLPhase 3JAK3
DACTOLISIBChEMBLPhase 3JAK3
ENTOSPLETINIBChEMBLPhase 3JAK2
ENZASTAURINChEMBLPhase 3JAK3
MOTESANIBChEMBLPhase 3JAK1