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Zasocitinib

drug
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Also known as Ndi-034858NDI034858Tak-279TAK279

Summary

Zasocitinib (CHEMBL5314423) is a phase-3 clinical-stage small molecule targeting TYK2; indicated across 8 conditions including psoriasis and psoriatic arthritis.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 1 (TYK2)
  • Indications: 8 conditions
  • Clinical trials: 22
  • Chemistry: 460.5 Da · C23H24N8O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL5314423
NameZasocitinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID137441492
Molecular formulaC23H24N8O3
Molecular weight460.5
InChIKeyBWINBHTTZLVXGT-NVXWUHKLSA-N

SMILES: CNC1=CC(=NC2=C(C=NN12)C(=O)N[C@@H]3CC[C@H]3OC)NC4=CC=CN(C4=O)C5=CC=CC=N5

IUPAC name: N-[(1R,2R)-2-methoxycyclobutyl]-7-(methylamino)-5-[(2-oxo-1-pyridin-2-yl-3-pyridinyl)amino]pyrazolo[1,5-a]pyrimidine-3-carboxamide

Also known as: Ndi-034858, NDI-034858, NDI034858, Tak-279, TAK-279, TAK279, Zasocitinib, ZASOCITINIB

Parent form; salt/anhydrous children: CHEMBL5401575

Patent coverage: 10 distinct patent families (27 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 21 (78%) 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
TYK2tyrosine kinase 2Inhibition70.8%P29597

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Tyrosine-protein kinase JAK1.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
JAK15.3Kd5000nMCHEMBL_ACT_25627497
JAK15.3Kd5000nMCHEMBL_ACT_25695933

Target pathways

Aggregated over 1 target gene(s): TYK2.

Top Reactome pathways

21 total, by targets touching each:

PathwayTargetsGenes
Interleukin-6 signaling1TYK2
MAPK3 (ERK1) activation1TYK2
MAPK1 (ERK2) activation1TYK2
Other interleukin signaling1TYK2
Interleukin-10 signaling1TYK2
Interleukin-4 and Interleukin-13 signaling1TYK2
IL-6-type cytokine receptor ligand interactions1TYK2
Interleukin-20 family signaling1TYK2
Interleukin-35 Signalling1TYK2
Interleukin-12 signaling1TYK2
Interleukin-23 signaling1TYK2
Interleukin-27 signaling1TYK2
Interferon alpha/beta signaling1TYK2
Regulation of IFNA/IFNB signaling1TYK2
Signaling by CSF3 (G-CSF)1TYK2
Potential therapeutics for SARS1TYK2
Inactivation of CSF3 (G-CSF) signaling1TYK2
SARS-CoV-2 activates/modulates innate and adaptive immune responses1TYK2
Signaling by ALK fusions and activated point mutants1TYK2
Evasion by RSV of host interferon responses1TYK2
Activation of STAT3 by cadherin engagement1TYK2

Dominant GO biological processes

GO termTargets
protein phosphorylation1
immune response1
cell surface receptor signaling pathway via JAK-STAT1
cell population proliferation1
cytokine-mediated signaling pathway1
cell differentiation1
positive regulation of type II interferon production1
positive regulation of interleukin-17 production1
positive regulation of natural killer cell proliferation1
intracellular signal transduction1
interleukin-12-mediated signaling pathway1
interleukin-23-mediated signaling pathway1
type III interferon-mediated signaling pathway1
positive regulation of T cell proliferation1
positive regulation of receptor signaling pathway via JAK-STAT1

Indications & clinical

Indications

8 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
psoriasis3MONDO:0005083EFO:0000676
psoriatic arthritis2MONDO:0011849EFO:0003778
Crohn disease2MONDO:0005011EFO:0000384
ulcerative colitis2MONDO:0005101EFO:0000729
liver disorder1MONDO:0005154EFO:0001421
kidney disorder1MONDO:0005240EFO:0003086

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

Clinical trials

Total trials: 22.

Phase distribution

PhaseTrials
PHASE39
PHASE17
PHASE26

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06323356PHASE3ACTIVE_NOT_RECRUITINGA Study of TAK-279 in Adult Participants With Generalized Pustular Psoriasis or Erythrodermic Psoriasis
NCT06550076PHASE3ACTIVE_NOT_RECRUITINGA Study of TAK-279 in Participants With Moderate-to-Severe Plaque Psoriasis
NCT06671483PHASE3RECRUITINGA Study of Zasocitinib in Adults With Psoriatic Arthritis Who Have Not Taken Biologic Medicines
NCT06671496PHASE3RECRUITINGA Study of Zasocitinib in Adults With Psoriatic Arthritis Who Have or Have Not Been Treated With Biologic Medicines
NCT07250802PHASE3RECRUITINGA Long-Term Study of Zasocitinib in Children and Teenagers With Plaque Psoriasis
NCT07286058PHASE3RECRUITINGContinuation Study of Zasocitinib in Adults With Psoriatic Arthritis
NCT06088043PHASE3COMPLETEDA Study About How Well TAK-279 Works and Its Safety in Participants With Moderate-to-severe Plaque Psoriasis During 52 Weeks of Treatment
NCT06108544PHASE3COMPLETEDA Study About How Well TAK-279 Works and Its Safety in Participants With Moderate-to-severe Plaque Psoriasis During 60 Weeks of Treatment With a Withdrawal and Retreatment Period
NCT06973291PHASE3COMPLETEDA Study Comparing Zasocitinib (TAK-279) With Deucravacitinib in Adults With Plaque Psoriasis
NCT06233461PHASE2RECRUITINGA Study on the Safety of TAK-279 and Whether it Can Reduce Inflammation in the Bowel of Participants With Moderately to Severely Active Crohn’s Disease
NCT06254950PHASE2ACTIVE_NOT_RECRUITINGA Study on the Safety of TAK-279 and Whether it Can Reduce Inflammation in the Bowel of Participants With Moderately to Severely Active Ulcerative Colitis
NCT06764615PHASE2RECRUITINGA Continuation Study of TAK-279 in Adults With Ulcerative Colitis (UC) and Crohn’s Disease (CD)
NCT07108283PHASE2RECRUITINGA Study of Zasocitinib in Adults With Nonsegmental Vitiligo
NCT07403968PHASE2NOT_YET_RECRUITINGA Study of Zasocitinib (TAK-279) in Adults With Active Crohn’s Disease
NCT05153148PHASE2COMPLETEDA Study to Evaluate the Efficacy, Safety, and Tolerability of NDI-034858 in Participants With Active Psoriatic Arthritis
NCT05976321PHASE1COMPLETEDA Study of TAK-279 in Adults With or Without Liver Damage
NCT05992155PHASE1COMPLETEDA Study of TAK-279 in Adults With or Without Kidney Problems
NCT05995249PHASE1COMPLETEDA Study of the Interaction of TAK-279 With Substances That Have an Impact on Metabolism in Healthy Adults
NCT06111547PHASE1COMPLETEDA Study of TAK-279 in Healthy Chinese Adults
NCT06258265PHASE1COMPLETEDA Study of TAK-279 in Healthy Adults on the Effect on ECG Measurements
NCT06290050PHASE1COMPLETEDA Study of the Interaction of Other Drugs With TAK-279 in Healthy Adults
NCT06793943PHASE1COMPLETEDA Study of Interaction of Zasocitinib (TAK-279) With Other Medicines in Healthy Adults

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.

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

MoleculeSourceStatusShared targets
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)TYK2
DEUCRAVACITINIBChEMBL + PubChemPhase 4 (approved)TYK2
PAZOPANIBChEMBL + PubChemPhase 4 (approved)TYK2
ABROCITINIBChEMBLPhase 4 (approved)TYK2
AXITINIBChEMBLPhase 4 (approved)TYK2
BARICITINIBChEMBLPhase 4 (approved)TYK2
BOSUTINIBChEMBLPhase 4 (approved)TYK2
CRAVACITINIBChEMBLPhase 4 (approved)TYK2
DASATINIBChEMBLPhase 4 (approved)TYK2
ERLOTINIBChEMBLPhase 4 (approved)TYK2
FEDRATINIBChEMBLPhase 4 (approved)TYK2
FILGOTINIBChEMBLPhase 4 (approved)TYK2
IMATINIBChEMBLPhase 4 (approved)TYK2
INFIGRATINIBChEMBLPhase 4 (approved)TYK2
MIDOSTAURINChEMBLPhase 4 (approved)TYK2
MOMELOTINIBChEMBLPhase 4 (approved)TYK2
NINTEDANIBChEMBLPhase 4 (approved)TYK2
PACRITINIBChEMBLPhase 4 (approved)TYK2
PEFICITINIBChEMBLPhase 4 (approved)TYK2
RUXOLITINIBChEMBLPhase 4 (approved)TYK2
SUNITINIBChEMBLPhase 4 (approved)TYK2
TOFACITINIBChEMBLPhase 4 (approved)TYK2
UPADACITINIBChEMBLPhase 4 (approved)TYK2
ALVOCIDIBChEMBLPhase 3TYK2
BREPOCITINIBChEMBLPhase 3TYK2
DEFACTINIBChEMBLPhase 3TYK2
DELGOCITINIBChEMBLPhase 3TYK2
DOVITINIBChEMBLPhase 3TYK2
ITACITINIBChEMBLPhase 3TYK2
LESTAURTINIBChEMBLPhase 3TYK2
AT-9283ChEMBLPhase 2TYK2
ATINVICITINIBChEMBLPhase 2TYK2
AZD-1480ChEMBLPhase 2TYK2
BMS-911543ChEMBLPhase 2TYK2
BMS-919373ChEMBLPhase 2TYK2
CC-401ChEMBLPhase 2TYK2
CENISERTIBChEMBLPhase 2TYK2
CERDULATINIBChEMBLPhase 2TYK2
DECERNOTINIBChEMBLPhase 2TYK2
ENMD-2076ChEMBLPhase 2TYK2
FORETINIBChEMBLPhase 2TYK2
GANDOTINIBChEMBLPhase 2TYK2
GOLIDOCITINIBChEMBLPhase 2TYK2
GUSACITINIBChEMBLPhase 2TYK2
IFIDANCITINIBChEMBLPhase 2TYK2
ILORASERTIBChEMBLPhase 2TYK2
IZENCITINIBChEMBLPhase 2TYK2
LONDAMOCITINIBChEMBLPhase 2TYK2
NEZULCITINIBChEMBLPhase 2TYK2
NS-018ChEMBLPhase 2TYK2
OCLACITINIBChEMBLPhase 2TYK2
PICTILISIBChEMBLPhase 2TYK2
R-406ChEMBLPhase 2TYK2
RAF-265ChEMBLPhase 2TYK2
ROPSACITINIBChEMBLPhase 2TYK2
SILMITASERTIBChEMBLPhase 2TYK2
SOLCITINIBChEMBLPhase 2TYK2
SU-014813ChEMBLPhase 2TYK2
TG100-115ChEMBLPhase 2TYK2
TOZASERTIBChEMBLPhase 2TYK2

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