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Brepocitinib

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Also known as Pf-06700841

Summary

Brepocitinib (CHEMBL4297477) is a phase-3 clinical-stage small molecule targeting JAK1, JAK2, and JAK3; indicated across 12 conditions including dermatomyositis and atopic eczema.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 4 (JAK1, JAK2, JAK3…)
  • Indications: 12 conditions
  • Clinical trials: 24
  • Chemistry: 389.4 Da · C18H21F2N7O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4297477
NameBrepocitinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID118878093
Molecular formulaC18H21F2N7O
Molecular weight389.4
InChIKeyBUWBRTXGQRBBHG-MJBXVCDLSA-N

SMILES: CN1C=C(C=N1)NC2=NC=CC(=N2)N3C[C@H]4CC[C@@H](C3)N4C(=O)[C@@H]5CC5(F)F

IUPAC name: [(1S)-2,2-difluorocyclopropyl]-[(1R,5S)-3-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone

Also known as: Brepocitinib, Pf-06700841, PF-06700841, BREPOCITINIB

Parent form; salt/anhydrous children: CHEMBL4298160

Patent coverage: 200 distinct patent families (568 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 1Inhibition7.772.8%P23458
JAK2Janus kinase 2Inhibition7.110.7%O60674
JAK3Janus kinase 3Inhibition5.190.6%P52333
TYK2tyrosine kinase 2Inhibition7.640.8%P29597

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Tyrosine-protein kinase JAK3, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, Non-receptor tyrosine-protein kinase TYK2.

Bioactivity

ChEMBL activities: 17 potent at pChembl ≥ 5 of 17 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
JAK17.77IC5017nMCHEMBL_ACT_25483758
JAK17.77IC5017nMCHEMBL_ACT_27789326
JAK17.77IC5017nMCHEMBL_ACT_28316024
JAK17.77IC5017nMCHEMBL_ACT_28561172
TYK27.64IC5023nMCHEMBL_ACT_25483764
TYK27.64IC5023nMCHEMBL_ACT_27225986
TYK27.64IC5023nMCHEMBL_ACT_27789323
TYK27.64IC5023nMCHEMBL_ACT_28316021
TYK27.64IC5023nMCHEMBL_ACT_28561169
JAK27.11IC5077nMCHEMBL_ACT_25483760
JAK27.11IC5077nMCHEMBL_ACT_27789329
JAK27.11IC5077nMCHEMBL_ACT_28316027
JAK27.11IC5077nMCHEMBL_ACT_28561175
JAK35.19IC506494nMCHEMBL_ACT_25483762
JAK35.19IC506494nMCHEMBL_ACT_27789332
JAK35.19IC506494nMCHEMBL_ACT_28316030
JAK35.19IC506494nMCHEMBL_ACT_28561178

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

12 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
dermatomyositis3MONDO:0016367EFO:0000398
atopic eczema2MONDO:0004980EFO:0000274
Crohn disease2MONDO:0005011EFO:0000384
psoriasis2MONDO:0005083EFO:0000676
ulcerative colitis2MONDO:0005101EFO:0000729
psoriatic arthritis2MONDO:0011849EFO:0003778
alopecia areata2MONDO:0005340EFO:0004192
hidradenitis suppurativa2MONDO:0006559EFO:1000710
alopecia2MONDO:0004907EFO:1002028
systemic lupus erythematosus2MONDO:0007915MONDO:0007915
kidney disorder1MONDO:0005240EFO:0003086
immune system disorder1MONDO:0005046EFO:0000540

Clinical trials

Total trials: 24.

Phase distribution

PhaseTrials
PHASE213
PHASE19
PHASE31
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05437263PHASE3ACTIVE_NOT_RECRUITINGA Study to Investigate the Efficacy and Safety of Brepocitinib in Adults With Dermatomyositis
NCT07532603PHASE2/PHASE3RECRUITINGA Phase 2/3 Study of Brepocitinib in Adults With Lichen Planopilaris
NCT06978725PHASE2RECRUITINGA Phase 2 Study of the Safety and Efficacy of Brepocitinib in Adults With Cutaneous Sarcoidosis (BEACON)
NCT02958865PHASE2COMPLETEDStudy to Compare Oral PF-06651600, PF-06700841 and Placebo in Subjects With Moderate to Severe Ulcerative Colitis
NCT02969018PHASE2COMPLETEDStudy To Evaluate Safety And Efficacy Of PF-06700841 In Subjects With Moderate To Severe Plaque Psoriasis
NCT02974868PHASE2COMPLETEDStudy To Evaluate The Efficacy And Safety Profile Of PF-06651600 And PF-06700841 In Subjects With Alopecia Areata
NCT03395184PHASE2COMPLETEDStudy To Evaluate The Efficacy And Safety Of Oral PF-06651600 And PF-06700841 In Subjects With Moderate To Severe Crohn’s Disease
NCT03845517PHASE2COMPLETEDA DOSE-RANGING STUDY TO EVALUATE EFFICACY AND SAFETY OF PF-06700841 IN SYSTEMIC LUPUS ERYTHEMATOSUS (SLE)
NCT03850483PHASE2COMPLETEDDose Ranging Study To Assess Efficacy, Safety and Tolerability Of PF-06700841 Topical Cream In Psoriasis
NCT03903822PHASE2COMPLETEDDose Ranging Study to Assess Efficacy, Safety, Tolerability and Pharmacokinetics of PF-06700841 Topical Cream in Participants With Mild or Moderate Atopic Dermatitis
NCT03963401PHASE2COMPLETEDA Study to Evaluate the Efficacy and Safety of PF-06700841 in Subjects With Active Psoriatic Arthritis
NCT04092452PHASE2COMPLETEDA Study to Evaluate the Safety and Efficacy of PF-06650833, PF-06700841, and PF 06826647 in Adults With Hidradenitis Suppurativa
NCT05076006PHASE2COMPLETEDDual JAK1/TYK2 Inhibitor for Cicatricial Alopecia
NCT05523765PHASE2COMPLETEDA Study of Brepocitinib in Adults With Active Non-Infectious Non-Anterior Uveitis
NCT06433999PHASE2COMPLETEDA 12-Week Open-Label Study to Investigate the Efficacy and Safety of Brepocitinib in Adults With Skin-Predominant Dermatomyositis
NCT02310750PHASE1COMPLETEDA Safety, Tolerability, Pharmacokinetics And Pharmacodynamics Study Of PF-06700841, With Bioavailability/Food Effect Investigation
NCT03236493PHASE1COMPLETEDSafety and Pharmacokinetic Study of PF-06700841 in Japanese Healthy Volunteers
NCT03656952PHASE1COMPLETEDA Study to Evaluate the PF-06700841 Effect on QTc Interval in Healthy Volunteers
NCT03770039PHASE1COMPLETEDSingle Dose Study With Unlabeled Dose and 14C-labeled Microdose of PF-06700841 in Healthy Male Subjects
NCT03916250PHASE1COMPLETEDEvaluation of Skin Irritation Potential With PF-06700841 Cream Formulation Using Negative Control in Adult Japanese Healthy Participants
NCT04090047PHASE1COMPLETEDA Study to Investigate the Effect of Multiple Doses of Itraconazole on the Pharmacokinetics of PF-06700841 in Healthy Participants
NCT04260464PHASE1COMPLETEDRenal Impairment Study of PF-06700841
NCT04267250PHASE1COMPLETEDEffect Of Multiple Dose PF-06700841 On The Pharmacokinetics Of Single Dose Oral Contraceptive Steroids
NCT04580797PHASE1COMPLETEDClinical Study to Evaluate Pharmacokinetics and Safety of PF-06700841 After Single and Multiple Oral Doses as Modified Release Formulations

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
FILGOTINIBChEMBLPhase 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
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

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