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Abrocitinib

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Also known as CibinqoPf-04965842US9035074, 2

Summary

Abrocitinib (CHEMBL3655081) is an approved small molecule (ATC D11AH08) targeting JAK1 and JAK2; indicated across 10 conditions including atopic eczema and psoriasis.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: D11AH08
  • Targets: 2 (JAK1, JAK2)
  • Indications: 10 conditions
  • Clinical trials: 50
  • Chemistry: 323.42 Da · C14H21N5O2S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3655081
NameAbrocitinib
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID78323835
ATCD11AH08
Molecular formulaC14H21N5O2S
Molecular weight323.42
InChIKeyIUEWXNHSKRWHDY-UHFFFAOYSA-N

SMILES: CCCS(=O)(=O)NC1CC(C1)N(C)C2=NC=NC3=C2C=CN3

IUPAC name: N-[3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl]propane-1-sulfonamide

Also known as: Abrocitinib, Cibinqo, Pf-04965842, PF-04965842, ABROCITINIB, US9035074, 2

Patent coverage: 445 distinct patent families (1,037 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 973 (94%) 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 1Inhibition7.542.8%P23458
JAK2Janus kinase 2Inhibition6.10.7%O60674

Broader ChEMBL bioactivity targets: 11 (assay-derived). Sample: Amine oxidase [flavin-containing] A, Tyrosine-protein kinase JAK3, Vascular endothelial growth factor receptor 2, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, JAK3/JAK1, JAK2/JAK1, JAK1/JAK2/TYK2, JAK1/TYK2, JAK2/TYK2.

Bioactivity

ChEMBL activities: 35 potent at pChembl ≥ 5 of 36 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
JAK18.29IC505.1nMCHEMBL_ACT_20638874
JAK17.7IC5020nMCHEMBL_ACT_25452150
JAK17.54IC5029nMCHEMBL_ACT_16330867
JAK17.54IC5029nMCHEMBL_ACT_18106915
JAK17.54IC5029nMCHEMBL_ACT_24788529
JAK17.54IC5029nMCHEMBL_ACT_26123565
JAK17.54IC5029nMCHEMBL_ACT_28297628
JAK27.44IC5036nMCHEMBL_ACT_20638912
JAK17.33IC5047nMCHEMBL_ACT_25452198
JAK17.05IC5090nMCHEMBL_ACT_25452222
TYK26.8IC50160nMCHEMBL_ACT_20638983
JAK26.79IC50163nMCHEMBL_ACT_18107325
JAK26.79IC50163nMCHEMBL_ACT_18107326
JAK16.75IC50180nMCHEMBL_ACT_20639097
JAK16.72IC50189nMCHEMBL_ACT_18107044
JAK26.57IC50271nMCHEMBL_ACT_18107330
JAK16.55IC50284nMCHEMBL_ACT_25452210
JAK26.38IC50412nMCHEMBL_ACT_25452162
JAK36.32IC50480nMCHEMBL_ACT_20638950
JAK16.29IC50511nMCHEMBL_ACT_18107329
TYK26.26IC50549nMCHEMBL_ACT_25452186
JAK36.22IC50605nMCHEMBL_ACT_18107302
JAK26.09IC50803nMCHEMBL_ACT_16279631
JAK26.09IC50803nMCHEMBL_ACT_18106958
JAK26.09IC50803nMCHEMBL_ACT_26123566
JAK26.09IC50803nMCHEMBL_ACT_28297631
KDR5.92IC501200nMCHEMBL_ACT_18107305
TYK25.9IC501250nMCHEMBL_ACT_16304959
TYK25.9IC501250nMCHEMBL_ACT_28297637
JAK15.89IC501298nMCHEMBL_ACT_18107328

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

10 indications (2 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
atopic eczema4MONDO:0004980EFO:0000274
psoriasis2MONDO:0005083EFO:0000676
granuloma annulare2MONDO:0006554EFO:1000704
type 1 diabetes mellitus2MONDO:0005147MONDO:0005147
sarcoidosis2MONDO:0019338MONDO:0019338
liver disorder1MONDO:0005154EFO:0001421
kidney disorder1MONDO:0005240EFO:0003086
food allergy1MONDO:0700226EFO:1001890
toxic epidermal necrolysis0MONDO:0019810EFO:0004775

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

Clinical trials

Total trials: 50.

Phase distribution

PhaseTrials
PHASE118
PHASE310
Not specified10
PHASE29
PHASE42
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07352566PHASE4NOT_YET_RECRUITINGUtilization of a Microdevice for Psoriasis and Atopic Dermatitis
NCT05602207PHASE4COMPLETEDEffects of Abrocitinib in Subjects With Atopic Dermatitis With an Unsatisfactory Response After Treatment With Dupilumab
NCT06807268PHASE3RECRUITINGA Study of the Medicine Called Abrocitinib in Children 6 to Less Than 12 Years of Age With Moderate-to-Severe Eczema
NCT06807281PHASE3RECRUITINGA Long-term Study of the Medicine Called Abrocitinib in Children Aged 2 Years and Older With Moderate to Severe Eczema
NCT03349060PHASE3COMPLETEDStudy to Evaluate Efficacy and Safety of PF-04965842 in Subjects Aged 12 Years And Older With Moderate to Severe Atopic Dermatitis
NCT03422822PHASE3COMPLETEDStudy to Evaluate Efficacy and Safety of PF-04965842 With or Without Topical Medications in Subjects Aged 12 Years and Older With Moderate to Severe Atopic Dermatitis
NCT03575871PHASE3COMPLETEDStudy Evaluating Efficacy and Safety of PF-04965842 in Subjects Aged 12 Years And Older With Moderate to Severe Atopic Dermatitis
NCT03627767PHASE3COMPLETEDStudy to Investigate Efficacy and Safety of PF-04965842 in Subjects Aged 12 Years and Over With Moderate to Severe Atopic Dermatitis With the Option of Rescue Treatment in Flaring Subjects
NCT03720470PHASE3COMPLETEDStudy Evaluating Efficacy and Safety of PF-04965842 and Dupilumab in Adult Subjects With Moderate to Severe Atopic Dermatitis on Background Topical Therapy
NCT03796676PHASE3COMPLETEDJAK1 Inhibitor With Medicated Topical Therapy in Adolescents With Atopic Dermatitis
NCT04345367PHASE3COMPLETEDStudy of Abrocitinib Compared With Dupilumab in Adults With Moderate to Severe Atopic Dermatitis on Background Topical Therapy
NCT05375929PHASE3COMPLETEDA Study to Learn About Abrocitinib Tablets in People With Atopic Dermatitis in India
NCT05650736PHASE2ACTIVE_NOT_RECRUITINGJanus Kinase Inhibition in Granuloma Annulare
NCT06597396PHASE2ACTIVE_NOT_RECRUITINGStudy to Investigate the Efficacy of Abrocitinib in Adult Participants With Severe Fatigue From Post COVID Condition/Long COVID
NCT07242638PHASE2RECRUITINGTreatment of Atopic Dermatitis and Alopecia Areata With Abrocitinib in Individuals With Down Syndrome
NCT02201524PHASE2TERMINATEDStudy to Evaluate PF-04965842 in Patients With Moderate to Severe Psoriasis
NCT02780167PHASE2COMPLETEDStudy To Evaluate Pf-04965842 In Subjects With Moderate To Severe Atopic Dermatitis
NCT03915496PHASE2COMPLETEDStudy Evaluating the Mechanism of Action of PF-04965842 Monotherapy for Moderate-to-severe Atopic Dermatitis
NCT05038982PHASE2COMPLETEDEfficacy of Abrocitinib for Reducing Pruritus in Adults With Prurigo Nodularis and Chronic Pruritus of Unknown Origin
NCT05696795PHASE2COMPLETEDJanus Kinase Inhibition in Sarcoidosis
NCT06283550PHASE2COMPLETEDEfficacy, Safety, and Tolerability of Abrocitinib in Subjects With Moderate to Severe Chronic Hand Eczema Refractory to Corticosteroid Therapy
NCT01835197PHASE1COMPLETEDFirst-in-Human Study to Evaluate Safety and Tolerability of Single and Multiple Ascending Doses of Janus Kinase-1 Inhibitor PF-04965842 in Healthy Western and Japanese Subjects
NCT02163161PHASE1COMPLETEDAStudy to Evaluate the Bioavailability of PF 04965842 in Healthy Subjects
NCT03250039PHASE1COMPLETEDAbsorption, Metabolism, Excretion and Absolute Bioavailability
NCT03386279PHASE1COMPLETEDA Study To Determine The Effect Of Single-dose PF-04965842 On QTc Interval In Healthy Volunteers Compared With Placebo and Moxifloxacin
NCT03626415PHASE1COMPLETEDA Hepatic Impairment Study for PF-04965842.
NCT03634345PHASE1COMPLETEDDrug Drug Interaction Study Evaluating the Effect of Fluvoxamine or Fluconazole on PK and Safety of PF-04965842.
NCT03637790PHASE1COMPLETEDDrug Interaction Study Evaluating the Effect of Rifampin on PK and Safety of PF 04965842.
NCT03647670PHASE1COMPLETEDA Study to Determine the Effects of PF-04965842 on Midazolam PK in Healthy Volunteers
NCT03660241PHASE1COMPLETEDA Renal Impairment Study for PF-04965842
NCT03662516PHASE1COMPLETEDA Study to Determine the Effects of PF-04965842 on the Pharmacokinetics of Oral Contraceptive Steroids in Healthy Female Subjects
NCT03742336PHASE1COMPLETEDStudy of PF-04965842 Effect on Dabigatran Pharmacokinetics in Healthy Participants
NCT03796182PHASE1COMPLETEDStudy of PF 04965842 Effect on MATE1/2K Activity in Healthy Participants
NCT03806101PHASE1COMPLETEDStudy of PF-04965842 Effect on Rosuvastatin Pharmacokinetics in Healthy Participants
NCT03937258PHASE1COMPLETEDA Study to Assess Pharmacokinetics of PF-04965842 and Its Metabolites and Effect of Probenecid in Healthy Participants
NCT04099563PHASE1COMPLETEDStudy to Assess Pharmacokinetics, Safety and Tolerability of PF-04965842 in Chinese Healthy Participants
NCT04903093PHASE1COMPLETEDA Study Evaluating Relative Bioavailability of an Oral Suspension of Abrocitinib and Effect of an Acid Reducing Agent on the Bioavailability of Abrocitinib and Assessing the Taste of Abrocitinib Oral Formulations.
NCT05067439PHASE1COMPLETEDA Study to Estimate the Effect of Multiple Dose Abrocitinib on Caffeine, Efavirenz, and Omeprazole in Healthy Participants
NCT05069831PHASE1COMPLETEDJAK Inhibition in Food Allergy
NCT06119490EARLY_PHASE1RECRUITINGEvaluation of the Efficacy and Safety of Methylprednisolone Combined With the JAK Inhibitors in the Treatment of Toxic Epidermal Necrolysis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 1 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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
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
ITACITINIBChEMBLPhase 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.

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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