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Atlas / Drug / Ivarmacitinib

Ivarmacitinib

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Also known as SHR-0302 FREE BASESHR0302 FREE BASESHR0302 base

Summary

Ivarmacitinib (CHEMBL5095398) is a phase-3 clinical-stage small molecule targeting JAK1 and JAK2; indicated across 2 conditions including autoimmune disease.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 2 (JAK1, JAK2)
  • Indications: 2 conditions
  • Clinical trials: 9
  • Chemistry: 414.5 Da · C18H22N8O2S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL5095398
NameIvarmacitinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID71622431
Molecular formulaC18H22N8O2S
Molecular weight414.5
InChIKeyDNBCBAXDWNDRNO-FOSCPWQOSA-N

SMILES: CN(C1C[C@@H]2CN(C[C@@H]2C1)C(=O)NC3=NC(=NS3)OC)C4=NC=NC5=C4C=CN5

IUPAC name: (3aS,6aR)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-2-carboxamide

Also known as: Ivarmacitinib, SHR-0302 FREE BASE, SHR0302 FREE BASE, SHR0302 base, IVARMACITINIB

Parent form; salt/anhydrous children: CHEMBL5095399

Patent coverage: 39 distinct patent families (104 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 70 (67%) 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 1Inhibition8.72.8%P23458
JAK2Janus kinase 2Inhibition8.30.7%O60674

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2.

Bioactivity

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

TargetpChemblTypeValueUnitActivity ID
JAK18.7IC502nMCHEMBL_ACT_26672315
JAK18.7IC502nMCHEMBL_ACT_26751197
JAK18.7IC502nMCHEMBL_ACT_27755666
JAK28.3IC505nMCHEMBL_ACT_26672480
JAK28.3IC505nMCHEMBL_ACT_26751362
JAK28.3IC505nMCHEMBL_ACT_27755831

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

2 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
autoimmune disease1MONDO:0007179EFO:0005809

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

Clinical trials

Total trials: 9.

Phase distribution

PhaseTrials
PHASE24
PHASE42
Not specified2
PHASE1/PHASE21

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07451665PHASE4NOT_YET_RECRUITINGEfficacy and Safety of Vunakizumab and Ivarmacitinib in the Treatment of Active Takayasu’s Arteritis
NCT07452445PHASE4NOT_YET_RECRUITINGEfficacy and Safety of Ivarmacitinib Monotherapy in the Treatment of csDMARDs-IR Rheumatoid Arthritis
NCT06731153PHASE2NOT_YET_RECRUITINGJAK1 Inhibitor Ivarmacitinib Reversing Immunotherapy Resistance in TNBC
NCT07313202PHASE2NOT_YET_RECRUITINGIvarmacitinib in Advanced Solid Tumors: A Prospective, Two-Cohort, Two-Phase Exploratory Study in Patients Discontinued Due to Immune Intolerance
NCT07381114PHASE1/PHASE2NOT_YET_RECRUITINGA Clinical Study on the Efficacy and Safety of Ivarmacitinib in Preventing aGVHD After HLA-matched Transplantation
NCT07505186PHASE2NOT_YET_RECRUITINGCamrelizumab, Chemotherapy and Ivarmacitinib in Patients With Resectable Esophageal Squamous Cell Carcinoma
NCT07570745PHASE2RECRUITINGLow-Dose ATG/PTCy Plus Ivarmacitinib for aGVHD Prevention in Haplo-PBSCT From Parous Female Donors
NCT07266168Not specifiedNOT_YET_RECRUITINGEfficacy and Safety of Ivarmacitinib in the Treatment of Patients With Polymyalgia Rheumatica
NCT07270003Not specifiedRECRUITINGA Prospective, Single-arm, Open-label Clinical Trial to Evaluate the Efficacy and Safety of Ivarmacitinib in the Treatment of Palmoplantar Pustulosis

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
ITACITINIBChEMBLPhase 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
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot