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Itacitinib

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Also known as Incb-039110Incb-39110INCB039110Incb39110

Summary

Itacitinib (CHEMBL3622820) is a phase-3 clinical-stage small molecule (ATC L04AF05) targeting JAK1 and JAK2; indicated across 29 conditions including graft versus host disease and hodgkins lymphoma.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • ATC class: L04AF05
  • Targets: 2 (JAK1, JAK2)
  • Indications: 29 conditions
  • Clinical trials: 52
  • Chemistry: 553.5 Da · C26H23F4N9O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3622820
NameItacitinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID53380437
ATCL04AF05
Molecular formulaC26H23F4N9O
Molecular weight553.5
InChIKeyKTBSXLIQKWEBRB-UHFFFAOYSA-N

SMILES: C1CN(CCC1N2CC(C2)(CC#N)N3C=C(C=N3)C4=C5C=CNC5=NC=N4)C(=O)C6=C(C(=NC=C6)C(F)(F)F)F

IUPAC name: 2-[1-[1-[3-fluoro-2-(trifluoromethyl)pyridine-4-carbonyl]piperidin-4-yl]-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile

Also known as: Incb-039110, INCB-039110, Incb-39110, INCB039110, Incb39110, Itacitinib, ITACITINIB, itacitinib

Parent form; salt/anhydrous children: CHEMBL3707409, CHEMBL3947131, CHEMBL3948879

Patent coverage: 804 distinct patent families (2,274 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 1,829 (80%) of the total. 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 1Inhibition8.32.8%P23458
JAK2Janus kinase 2Inhibition70.7%O60674

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Tyrosine-protein kinase JAK3, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, Non-receptor tyrosine-protein kinase TYK2, Tyrosine-protein kinase receptor UFO, Tyrosine-protein kinase receptor TYRO3, Tyrosine-protein kinase Mer.

Bioactivity

ChEMBL activities: 25 potent at pChembl ≥ 5 of 26 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
JAK18.7IC502nMCHEMBL_ACT_24788527
JAK18.7IC502nMCHEMBL_ACT_25044296
JAK18.7IC502nMCHEMBL_ACT_25848294
JAK18.7IC502nMCHEMBL_ACT_29156692
JAK18.47IC503.4nMCHEMBL_ACT_25839844
JAK27.97Kd10.7nMCHEMBL_ACT_25839915
JAK27.6IC5025nMCHEMBL_ACT_27672101
JAK27.6IC5025nMCHEMBL_ACT_27672131
JAK27.6IC5025nMCHEMBL_ACT_27672137
JAK27.58Kd26nMCHEMBL_ACT_25839814
JAK17.29Kd51nMCHEMBL_ACT_25839804
JAK27.27IC5054nMCHEMBL_ACT_25839854
JAK27.2IC5063nMCHEMBL_ACT_25044280
JAK27.12IC5075nMCHEMBL_ACT_28003553
JAK27.12IC5075nMCHEMBL_ACT_28003583
JAK27.12IC5075nMCHEMBL_ACT_28003589
AXL6.52IC50300nMCHEMBL_ACT_26791277
MERTK6.52IC50300nMCHEMBL_ACT_26791283
JAK36.49Kd324nMCHEMBL_ACT_25839824
TYK26.42Kd385nMCHEMBL_ACT_25839834
JAK26.31IC50488nMCHEMBL_ACT_25839926
TYRO36.12IC50750nMCHEMBL_ACT_26791280
TYK26.1IC50795nMCHEMBL_ACT_25044301
JAK35.7IC502000nMCHEMBL_ACT_25044288
TYK25.39IC504095nMCHEMBL_ACT_25839874

Target pathways

Aggregated over 2 target gene(s): JAK1, JAK2.

Top Reactome pathways

84 total, by targets touching each:

PathwayTargetsGenes
Interleukin-6 signaling2JAK1, JAK2
MAPK3 (ERK1) activation2JAK1, JAK2
RAF-independent MAPK1/3 activation2JAK1, JAK2
MAPK1 (ERK2) activation2JAK1, JAK2
Cytokine Signaling in Immune system2JAK1, JAK2
Signal Transduction2JAK1, JAK2
Disease2JAK1, JAK2
Immune System2JAK1, JAK2
Interleukin-12 family signaling2JAK1, JAK2
Signaling by Interleukins2JAK1, JAK2
Interleukin-2 family signaling2JAK1, JAK2
Interleukin-3, Interleukin-5 and GM-CSF signaling2JAK1, JAK2
Infectious disease2JAK1, JAK2
RAF/MAP kinase cascade2JAK1, JAK2
MAPK family signaling cascades2JAK1, JAK2
MAPK1/MAPK3 signaling2JAK1, JAK2
Interleukin-6 family signaling2JAK1, JAK2
Interleukin-4 and Interleukin-13 signaling2JAK1, JAK2
IL-6-type cytokine receptor ligand interactions2JAK1, JAK2
Interferon gamma signaling2JAK1, JAK2
Regulation of IFNG signaling2JAK1, JAK2
Interleukin-20 family signaling2JAK1, JAK2
Interleukin-35 Signalling2JAK1, JAK2
Interleukin-12 signaling2JAK1, JAK2
Interleukin-27 signaling2JAK1, JAK2
Interleukin receptor SHC signaling2JAK1, JAK2
Interferon Signaling2JAK1, JAK2
Signaling by CSF3 (G-CSF)2JAK1, JAK2
Potential therapeutics for SARS2JAK1, JAK2
SARS-CoV Infections2JAK1, JAK2

Dominant GO biological processes

GO termTargets
protein phosphorylation2
cell surface receptor signaling pathway via JAK-STAT2
cytokine-mediated signaling pathway2
cell differentiation2
intracellular signal transduction2
response to antibiotic2
type II interferon-mediated signaling pathway2
growth hormone receptor signaling pathway via JAK-STAT2
interleukin-6-mediated signaling pathway2
cellular response to virus2
regulation of cell-cell adhesion2
positive regulation of homotypic cell-cell adhesion1
interleukin-15-mediated signaling pathway1
interleukin-4-mediated signaling pathway1
interleukin-2-mediated signaling pathway1

Indications & clinical

Indications

29 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
graft versus host disease3MONDO:0013730EFO:0004599
Hodgkins lymphoma2MONDO:0004952EFO:0000183
neoplasm2MONDO:0005070EFO:0000616
psoriasis2MONDO:0005083EFO:0000676
rheumatoid arthritis2MONDO:0008383EFO:0000685
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
ulcerative colitis2MONDO:0005101EFO:0000729
hematopoietic and lymphoid system neoplasm2MONDO:0002334MONDO:0044881
systemic sclerosis2MONDO:0005100EFO:0000717
primary myelofibrosis2MONDO:0009692MONDO:0044903
diffuse large B-cell lymphoma2MONDO:0018905EFO:0000403
melanoma1MONDO:0005105EFO:0000756
exocrine pancreatic carcinoma1MONDO:0005192EFO:0002618
lymphoma1MONDO:0005062EFO:0000574
bronchiolitis obliterans syndrome1MONDO:0015265EFO:0007183
T-cell prolymphocytic leukemia1MONDO:0019468EFO:1000560
hepatocellular carcinoma1MONDO:0007256EFO:0000182
breast neoplasm1MONDO:0021100MONDO:0007254
lung neoplasm1MONDO:0021117MONDO:0008903
endometrium neoplasm1MONDO:0021251MONDO:0011962
hematologic disorder1MONDO:0005570EFO:0005803

8 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 52.

Phase distribution

PhaseTrials
PHASE225
PHASE114
PHASE1/PHASE210
PHASE31
PHASE2/PHASE31
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03139604PHASE3COMPLETEDGRAVITAS-301: A Study of Itacitinib or Placebo in Combination With Corticosteroids for Treatment of Acute Graft-Versus-Host Disease
NCT03584516PHASE2/PHASE3TERMINATEDGRAVITAS-309: Itacitinib and Corticosteroids as Initial Treatment for Chronic Graft-Versus-Host Disease
NCT03697408PHASE1/PHASE2ACTIVE_NOT_RECRUITINGItacitinib + Everolimus in Hodgkin Lymphoma
NCT04061421PHASE1/PHASE2RECRUITINGActive Myeloid Target Compound Combinations in MDS/MPN Overlap Syndromes Overlap Syndromes (ABNL-MARRO)
NCT04509700PHASE2ACTIVE_NOT_RECRUITINGRollover Study to Provide Continued Treatment for Participants With B-Cell Malignancies Previously Enrolled in Studies of Parsaclisib (INCB050465)
NCT04640025PHASE2ACTIVE_NOT_RECRUITINGA Rollover Study to Provide Continued Treatment for Participants Previously Enrolled in Studies of Itacitinib
NCT04789850PHASE2RECRUITINGSafety and Efficacy of Itacitinib in Adults With Systemic Sclerosis
NCT04859946PHASE2ACTIVE_NOT_RECRUITINGItacitinib for the Prevention of Graft Versus Host Disease
NCT05364762PHASE2ACTIVE_NOT_RECRUITINGAdding Itacitinib to Cyclophosphamide and Tacrolimus for the Prevention of Graft Versus Host Disease in Patients Undergoing Hematopoietic Stem Cell Transplants
NCT05757219PHASE2RECRUITINGItacitinib Pre-modulation in DLBCL Receiving CAR T Cell Therapy
NCT01626573PHASE2COMPLETEDA Study Exploring the Safety, Tolerability, and Efficacy of a 28 Day Course Followed by an Additional 56 Day Course of Itacitinib in Subjects With Active Rheumatoid Arthritis
NCT01633372PHASE2COMPLETEDAn Open Label Study of Itacitinib Administered Orally in Patients With Myelofibrosis
NCT01634087PHASE2COMPLETEDA Study of Escalating Doses of Itacitinib Administered Orally in Patients With Plaque Psoriasis
NCT01858883PHASE1/PHASE2COMPLETEDSafety Study of Itacitinib (INCB039110) in Combination With Gemcitabine and Nab-Paclitaxel in Subjects With Advanced Solid Tumors
NCT02018861PHASE1/PHASE2COMPLETEDA Phase 1/2, Open-Label, Dose Escalation, Safety and Tolerability Study of INCB050465 and Itacitinib in Subjects With Previously Treated B-Cell Malignancies (CITADEL-101)
NCT02257619PHASE2TERMINATEDStudy of Itacitinib in Combination With Docetaxel in Subjects With Non-Small Cell Lung Cancer
NCT02265510PHASE1/PHASE2TERMINATEDAn Open-Label Study of a Novel JAK-inhibitor, INCB052793, Given to Patients With Advanced Malignancies
NCT02355431PHASE2WITHDRAWNItacitinib in Combination With Erlotinib in Non Small Cell Lung Cancer Patients With Epidermal Growth Factor Receptor (EGFR) Activating Mutations
NCT02456675PHASE2TERMINATEDINCB040093 and INCB040093 Combined With Itacitinib (INCB039110) in Relapsed/Refractory Hodgkin Lymphoma
NCT02760485PHASE1/PHASE2COMPLETEDA Study of Itacitinib (INCB039110) in Combination With Ibrutinib in Subjects With Relapsed or Refractory Diffuse Large B-Cell Lymphoma
NCT02909569PHASE2WITHDRAWNRelieving Chronic Itch: Oral Medication
NCT02917993PHASE1/PHASE2COMPLETEDAn Open-Label Phase 1/2 Study of Itacitinib in Combination With Osimertinib in Subjects With Non-Small Cell Lung Cancer
NCT03144687PHASE2COMPLETEDA Study of Itacitinib in Combination With Low-Dose Ruxolitinib or Itacitinib Alone Following Ruxolitinib in Participants With Myelofibrosis
NCT03425006PHASE2TERMINATEDPembrolizumab and Itacitinib (INCB039110) for Non-Small Cell Lung Cancer
NCT03627052PHASE2WITHDRAWNA Study to Evaluate the Safety and Efficacy of Itacitinib in Moderate to Severe Ulcerative Colitis
NCT03721965PHASE1/PHASE2TERMINATEDSafety and Efficacy of Itacitinib in Combination With Corticosteroids for Treatment of Graft-Versus-Host Disease in Pediatric Subjects
NCT03846479PHASE2COMPLETEDItacitinib for Low Risk GVHD
NCT03978637PHASE1/PHASE2TERMINATEDSafety and Efficacy of Itacitinib in Participants With Bronchiolitis Obliterans Syndrome Following Lung Transplantation
NCT04071366PHASE2COMPLETEDA Study of Itacitinib for the Prevention of Cytokine Release Syndrome Induced by Immune Effector Cell Therapy
NCT04127721PHASE2WITHDRAWNItacitinib for the Prevention of Graft Versus Host Disease in Patients Undergoing Donor Stem Cell Transplantation
NCT04200365PHASE2TERMINATEDA Study of Itacitinib for the Treatment of Chronic Graft Versus Host Disease (cGVHD)
NCT04220632PHASE1/PHASE2TERMINATEDA Study of IBI377 in Combination With Corticosteroids for the Treatment of First-Line Acute Graft-Versus-Host Disease
NCT04446182PHASE2TERMINATEDItacitinib (INCB039110) and Extracorporeal Photopheresis (ECP) for First-Line Treatment in Chronic GVHD
NCT04591431PHASE2UNKNOWNThe Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy
NCT04629508PHASE2COMPLETEDTo Assess the Safety, Tolerability and Efficacy of Itacitinib Immediate Release Tablets in Participants With Primary or Secondary Myelofibrosis Who Have Received Prior Ruxolitinib and/or Fedratinib Monotherapy (LIMBER-213)
NCT05063110PHASE2COMPLETEDTreatment of Non Severe Hemophagocytosis Lymphohistiocytosis With ITACITINIB
NCT05660421PHASE2WITHDRAWNItacitinib for the Treatment Steroid Refractory Immune Related Adverse Events Arising From Immune Checkpoint Inhibitors
NCT05823571PHASE1ACTIVE_NOT_RECRUITINGItacitinib With High-dose Posttransplantation Cyclophosphamide in Older Patients
NCT01905813PHASE1COMPLETEDStudy of INCB040093 in Subjects With Previously Treated B-Cell Malignancies
NCT02559492PHASE1TERMINATEDItacitinib Combined With INCB024360 and/or Itacitinib Combined With INCB050465 in Advanced Solid Tumors

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

104 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)JAK1, JAK2
DEUCRAVACITINIBChEMBL + PubChemPhase 4 (approved)JAK1, JAK2
PazopanibChEMBL + PubChemPhase 4 (approved)JAK1, JAK2
RITLECITINIBChEMBL + PubChemPhase 4 (approved)JAK1, JAK2
ABROCITINIBChEMBLPhase 4 (approved)JAK1, JAK2
BARICITINIBChEMBLPhase 4 (approved)JAK1, JAK2
CERITINIBChEMBLPhase 4 (approved)JAK1, JAK2
ENTRECTINIBChEMBLPhase 4 (approved)JAK1, JAK2
FEDRATINIBChEMBLPhase 4 (approved)JAK1, JAK2
FILGOTINIBChEMBLPhase 4 (approved)JAK1, JAK2
MIDOSTAURINChEMBLPhase 4 (approved)JAK1, JAK2
MOMELOTINIBChEMBLPhase 4 (approved)JAK1, JAK2
NINTEDANIBChEMBLPhase 4 (approved)JAK1, JAK2
PACRITINIBChEMBLPhase 4 (approved)JAK1, JAK2
PEFICITINIBChEMBLPhase 4 (approved)JAK1, JAK2
PONATINIBChEMBLPhase 4 (approved)JAK1, JAK2
RUXOLITINIBChEMBLPhase 4 (approved)JAK1, JAK2
SUNITINIBChEMBLPhase 4 (approved)JAK1, JAK2
TOFACITINIBChEMBLPhase 4 (approved)JAK1, JAK2
UPADACITINIBChEMBLPhase 4 (approved)JAK1, JAK2
ABIVERTINIBChEMBLPhase 3JAK1, JAK2
BREPOCITINIBChEMBLPhase 3JAK1, JAK2
DELGOCITINIBChEMBLPhase 3JAK1, JAK2
DOVITINIBChEMBLPhase 3JAK1, JAK2
IVARMACITINIBChEMBLPhase 3JAK1, JAK2
LESTAURTINIBChEMBLPhase 3JAK1, JAK2
POVORCITINIBChEMBLPhase 3JAK1, JAK2
AT-9283ChEMBLPhase 2JAK1, JAK2
ATINVICITINIBChEMBLPhase 2JAK1, JAK2
AZD-1480ChEMBLPhase 2JAK1, JAK2
BMS-911543ChEMBLPhase 2JAK1, JAK2
CC-401ChEMBLPhase 2JAK1, JAK2
CERDULATINIBChEMBLPhase 2JAK1, JAK2
DECERNOTINIBChEMBLPhase 2JAK1, JAK2
GANDOTINIBChEMBLPhase 2JAK1, JAK2
GOLIDOCITINIBChEMBLPhase 2JAK1, JAK2
GUSACITINIBChEMBLPhase 2JAK1, JAK2
IFIDANCITINIBChEMBLPhase 2JAK1, JAK2
IZENCITINIBChEMBLPhase 2JAK1, JAK2
LONDAMOCITINIBChEMBLPhase 2JAK1, JAK2
NEZULCITINIBChEMBLPhase 2JAK1, JAK2
NS-018ChEMBLPhase 2JAK1, JAK2
OCLACITINIBChEMBLPhase 2JAK1, JAK2
R-406ChEMBLPhase 2JAK1, JAK2
REBASTINIBChEMBLPhase 2JAK1, JAK2
ROPSACITINIBChEMBLPhase 2JAK1, JAK2
SOLCITINIBChEMBLPhase 2JAK1, JAK2
SU-014813ChEMBLPhase 2JAK1, JAK2
TOZASERTIBChEMBLPhase 2JAK1, JAK2
ZOTIRACICLIBChEMBLPhase 2JAK1, JAK2
AfatinibPubChemApprovedJAK1, JAK2
FostamatinibPubChemApprovedJAK1, JAK2
GefitinibPubChemApprovedJAK1, JAK2
IdelalisibPubChemApprovedJAK1, JAK2
ImatinibPubChemApprovedJAK1, JAK2
SelumetinibPubChemApprovedJAK1, JAK2
TrametinibPubChemApprovedJAK1, JAK2
AXITINIBChEMBLPhase 4 (approved)JAK2
BOSUTINIBChEMBLPhase 4 (approved)JAK2
BRIGATINIBChEMBLPhase 4 (approved)JAK2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
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Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot