Delgocitinib

Summary

Delgocitinib (CHEMBL4297507) is a phase-3 clinical-stage small-molecule EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor (ATC D11AH11) targeting JAK1, JAK2, and JAK3; indicated across 5 conditions including atopic eczema and psoriasis.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: D11AH11
• Targets: 4 (JAK1, JAK2, JAK3…)
• Indications: 5 conditions
• Clinical trials: 21
• Chemistry: 310.35 Da · C16H18N6O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297507
Name	Delgocitinib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	50914062
ChEBI	CHEBI:167600
ATC	D11AH11
Molecular formula	C16H18N6O
Molecular weight	310.35
InChIKey	LOWWYYZBZNSPDT-ZBEGNZNMSA-N

SMILES: C[C@H]1CN([C@]12CCN(C2)C3=NC=NC4=C3C=CN4)C(=O)CC#N

IUPAC name: 3-[(3S,4R)-3-methyl-7-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,7-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile

ChEBI definition: A pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine substituted by a (3S,4R)-1-(cyanoacetyl)-3-methyl-1,6-diazaspiro[3.4]octan-6-yl group at position 4. It is a pan-Janus kinase (JAK) inhibitor and is approved for treatment of atopic dermatitis (AD) in Japan.

Pharmacological roles (ChEBI): EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, anti-inflammatory drug, antipsoriatic, antiseborrheic.

Also known as: Delgocitinib, JTE-052, JTE-052A, LEO 124249, LEO 124249A, LEO-124249, LEO-124249A, DELGOCITINIB

Patent coverage: 295 distinct patent families (767 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 655 (85%) 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
JAK1	Janus kinase 1	Inhibition	8.55	2.8%	P23458
JAK2	Janus kinase 2	Inhibition	8.59	0.7%	O60674
JAK3	Janus kinase 3	Inhibition	7.89	0.6%	P52333
TYK2	tyrosine kinase 2	Inhibition	7.24	0.8%	P29597

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Tyrosine-protein kinase JAK3, Tyrosine-protein kinase Lck, Tyrosine-protein kinase JAK1, Tyrosine-protein kinase JAK2, JAK3/JAK1, JAK2/JAK1, JAK1/TYK2, JAK2/TYK2, Non-receptor tyrosine-protein kinase TYK2, Signal transducer and activator of transcription 3.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
JAK2	8.59	IC50	2.6	nM	CHEMBL_ACT_20714962
JAK2	8.59	IC50	2.6	nM	CHEMBL_ACT_24788505
JAK2	8.59	IC50	2.6	nM	CHEMBL_ACT_25044267
JAK2	8.59	IC50	2.6	nM	CHEMBL_ACT_25848302
JAK1	8.55	IC50	2.8	nM	CHEMBL_ACT_20714960
JAK1	8.55	IC50	2.8	nM	CHEMBL_ACT_24788526
JAK1	8.55	IC50	2.8	nM	CHEMBL_ACT_25044266
JAK1	8.55	IC50	2.8	nM	CHEMBL_ACT_25848301
JAK1	8.05	IC50	9	nM	CHEMBL_ACT_25452153
JAK1	8.05	IC50	9	nM	CHEMBL_ACT_25452201
JAK3	7.89	IC50	13	nM	CHEMBL_ACT_20714792
JAK3	7.89	IC50	13	nM	CHEMBL_ACT_24788516
JAK3	7.89	IC50	13	nM	CHEMBL_ACT_25044268
JAK3	7.89	IC50	13	nM	CHEMBL_ACT_25848303
JAK1	7.75	IC50	18	nM	CHEMBL_ACT_20714970
STAT3	7.75	IC50	18	nM	CHEMBL_ACT_25044310
JAK2	7.6	IC50	25	nM	CHEMBL_ACT_20714967
JAK1	7.52	IC50	30	nM	CHEMBL_ACT_25069522
JAK1	7.52	IC50	30	nM	CHEMBL_ACT_25452225
JAK2	7.48	IC50	33	nM	CHEMBL_ACT_20714966
STAT3	7.48	IC50	33	nM	CHEMBL_ACT_25044307
JAK2	7.43	IC50	37	nM	CHEMBL_ACT_25452165
JAK1	7.4	IC50	40	nM	CHEMBL_ACT_20714965
STAT3	7.4	IC50	40	nM	CHEMBL_ACT_25044306
JAK1	7.38	IC50	42	nM	CHEMBL_ACT_25069514
JAK1	7.38	IC50	42	nM	CHEMBL_ACT_25452213
TYK2	7.24	IC50	58	nM	CHEMBL_ACT_20714964
TYK2	7.24	IC50	58	nM	CHEMBL_ACT_25044269
TYK2	7.24	IC50	58	nM	CHEMBL_ACT_25848304
JAK2	7.08	IC50	84	nM	CHEMBL_ACT_20714968

Target pathways

Aggregated over 4 target gene(s): JAK1, JAK2, JAK3, TYK2.

Top Reactome pathways

86 total, by targets touching each:

Pathway	Targets	Genes
Interleukin-4 and Interleukin-13 signaling	4	JAK1, JAK2, JAK3, TYK2
Interleukin-20 family signaling	4	JAK1, JAK2, JAK3, TYK2
Potential therapeutics for SARS	4	JAK1, JAK2, JAK3, TYK2
Interleukin-6 signaling	3	JAK1, JAK2, TYK2
MAPK3 (ERK1) activation	3	JAK1, JAK2, TYK2
MAPK1 (ERK2) activation	3	JAK1, JAK2, TYK2
Cytokine Signaling in Immune system	3	JAK1, JAK2, JAK3
Signal Transduction	3	JAK1, JAK2, JAK3
Disease	3	JAK1, JAK2, JAK3
Immune System	3	JAK1, JAK2, JAK3
Signaling by Interleukins	3	JAK1, JAK2, JAK3
Interleukin-2 family signaling	3	JAK1, JAK2, JAK3
Interleukin-3, Interleukin-5 and GM-CSF signaling	3	JAK1, JAK2, JAK3
Infectious disease	3	JAK1, JAK2, JAK3
RAF/MAP kinase cascade	3	JAK1, JAK2, JAK3
MAPK family signaling cascades	3	JAK1, JAK2, JAK3
MAPK1/MAPK3 signaling	3	JAK1, JAK2, JAK3
IL-6-type cytokine receptor ligand interactions	3	JAK1, JAK2, TYK2
Interleukin-35 Signalling	3	JAK1, JAK2, TYK2
Interleukin-12 signaling	3	JAK1, JAK2, TYK2
Interleukin-27 signaling	3	JAK1, JAK2, TYK2
Interleukin receptor SHC signaling	3	JAK1, JAK2, JAK3
Signaling by CSF3 (G-CSF)	3	JAK1, JAK2, TYK2
SARS-CoV Infections	3	JAK1, JAK2, JAK3
Inactivation of CSF3 (G-CSF) signaling	3	JAK1, JAK2, TYK2
Viral Infection Pathways	3	JAK1, JAK2, JAK3
Activation of STAT3 by cadherin engagement	3	JAK1, JAK2, TYK2
RAF-independent MAPK1/3 activation	2	JAK1, JAK2
Interleukin-7 signaling	2	JAK1, JAK3
Interleukin-12 family signaling	2	JAK1, JAK2

Dominant GO biological processes

GO term	Targets
protein phosphorylation	4
cell surface receptor signaling pathway via JAK-STAT	4
cytokine-mediated signaling pathway	4
cell differentiation	4
intracellular signal transduction	4
growth hormone receptor signaling pathway via JAK-STAT	4
regulation of cell-cell adhesion	4
type II interferon-mediated signaling pathway	3
cellular response to virus	3
regulation of receptor signaling pathway via JAK-STAT	3
regulation of alpha-beta T cell activation	3
interleukin-15-mediated signaling pathway	2
interleukin-4-mediated signaling pathway	2
interleukin-2-mediated signaling pathway	2
interleukin-7-mediated signaling pathway	2

Indications & clinical

Indications

5 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).

Indication	Trial phase	MONDO	EFO
atopic eczema	2	MONDO:0004980	EFO:0000274
psoriasis	2	MONDO:0005083	EFO:0000676
alopecia areata	2	MONDO:0005340	EFO:0004192
discoid lupus erythematosus	2	MONDO:0019558	MONDO:0019558

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

Clinical trials

Total trials: 21.

Phase distribution

Phase	Trials
PHASE2	8
PHASE3	7
PHASE1	4
EARLY_PHASE1	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07335588	PHASE3	RECRUITING	A 52-Week Trial to Investigate the Efficacy and Safety of Delgocitinib Cream in Adult Participants With Lichen Sclerosus
NCT04871711	PHASE3	COMPLETED	Efficacy and Safety of Delgocitinib Cream in Adults With Moderate to Severe Chronic Hand Eczema
NCT04872101	PHASE3	COMPLETED	Efficacy and Safety of Delgocitinib Cream in Adults With Moderate to Severe Chronic Hand Eczema (DELTA 2)
NCT04949841	PHASE3	COMPLETED	Open-label Multi-site Extension Trial in Subjects Who Completed the DELTA 1 or DELTA 2 Trials
NCT05259722	PHASE3	COMPLETED	A 24 Week Trial to Compare the Efficacy and Safety of Delgocitinib Cream 20 mg/g Twice-daily With Alitretinoin Capsules Once-daily in Adult Participants With Severe Chronic Hand Eczema
NCT05355818	PHASE3	COMPLETED	Efficacy and Safety of Delgocitinib Cream in Adolescents 12-17 Years of Age With Moderate to Severe Chronic Hand Eczema
NCT06004050	PHASE3	COMPLETED	A Trial to Evaluate Efficacy, Safety, and Pharmacokinetics of Delgocitinib Cream in Chinese Adults and Adolescents With Moderate to Severe Chronic Hand Eczema
NCT07013201	PHASE2	RECRUITING	A 16-week Trial to Investigate the Efficacy and Safety of Delgocitinib Cream 20 mg/g in Adult Participants With Mild to Severe Palmoplantar Pustulosis
NCT07487948	PHASE2	RECRUITING	Safety and Biomarker Responses of Delgocitinib (JAK1,2,3/TYK2 Inhibitor) in Central Centrifugal Cicatricial Alopecia and Lichen Planopilaris
NCT02561585	PHASE2	COMPLETED	LEO 124249 Ointment in the Treatment of Alopecia Areata
NCT03325296	PHASE2	TERMINATED	Efficacy of Twice Daily Application of LEO 124249 Ointment 30 mg/g for 12 Weeks on Eyebrow Alopecia Areata.
NCT03683719	PHASE2	COMPLETED	Phase 2b Dose-ranging Trial to Evaluate Delgocitinib Cream 1, 3, 8, and 20 mg/g Compared to Delgocitinib Cream Vehicle Over a 16-week Treatment Period in Adult Subjects With Chronic Hand Eczema
NCT03725722	PHASE2	COMPLETED	Dose-ranging Trial to Evaluate Delgocitinib Cream 1, 3, 8, and 20 mg/g Compared to Delgocitinib Cream Vehicle Over an 8-week Treatment Period in Adult Subjects With Atopic Dermatitis.
NCT03958955	PHASE2	TERMINATED	Efficacy and Safety of Delgocitinib Cream in Discoid Lupus Erythematosus.
NCT05332366	PHASE2	COMPLETED	A Trial to Assess the Effect of Delgocitinib Cream 20 mg/g on the Molecular Signature, Safety, and Efficacy in Adults With Frontal Fibrosing Alopecia
NCT03826901	PHASE1	COMPLETED	Delgocitinib Cream for the Treatment of Moderate to Severe Atopic Dermatitis During 8 Weeks in Adults, Adolescents, and Children
NCT04361136	PHASE1	COMPLETED	Clinical Trial to Evaluate Light-induced Skin Reactions After Application of Delgocitinib Cream
NCT04807751	PHASE1	COMPLETED	Clinical Trial to Evaluate UV-light-induced Allergic Skin Reactions After Application of Delgocitinib Cream
NCT05486117	PHASE1	COMPLETED	Pharmacokinetics of Delgocitinib 20 mg/g Cream in Subjects With Chronic Hand Eczema
NCT05050279	EARLY_PHASE1	COMPLETED	A Trial to Evaluate the Effect of Delgocitinib on the Heart Rhythm of Healthy People
NCT07203274	Not specified	NOT_YET_RECRUITING	The Role of Janus Kinase (JAK) and Voltage-gated Sodium Channels (Nav) on Pain and Itch

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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 60 by shared-target count:

Molecule	Source	Status	Shared targets
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
DEUCRAVACITINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
Pazopanib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
RITLECITINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
ABROCITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
BARICITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
FEDRATINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
FILGOTINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
MOMELOTINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
NINTEDANIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
PACRITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
PEFICITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
RUXOLITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
SUNITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
TOFACITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
UPADACITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3, TYK2
BREPOCITINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, TYK2
DOVITINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, TYK2
ITACITINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, TYK2
LESTAURTINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3, TYK2
AT-9283	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
ATINVICITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
AZD-1480	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
BMS-911543	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
CC-401	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
CERDULATINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
DECERNOTINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
GANDOTINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
GOLIDOCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
GUSACITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
IFIDANCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
IZENCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
NEZULCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
NS-018	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
OCLACITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
R-406	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
ROPSACITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
SOLCITINIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
SU-014813	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
TOZASERTIB	ChEMBL	Phase 2	JAK1, JAK2, JAK3, TYK2
Afatinib	PubChem	Approved	JAK1, JAK2, JAK3, TYK2
Gefitinib	PubChem	Approved	JAK1, JAK2, JAK3, TYK2
Idelalisib	PubChem	Approved	JAK1, JAK2, JAK3, TYK2
Selumetinib	PubChem	Approved	JAK1, JAK2, JAK3, TYK2
dacomitinib	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK3, TYK2
IMATINIB	ChEMBL + PubChem	Phase 4 (approved)	JAK1, JAK2, TYK2
AXITINIB	ChEMBL	Phase 4 (approved)	JAK2, JAK3, TYK2
BOSUTINIB	ChEMBL	Phase 4 (approved)	JAK2, JAK3, TYK2
CERITINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3
DASATINIB	ChEMBL	Phase 4 (approved)	JAK2, JAK3, TYK2
ENTRECTINIB	ChEMBL	Phase 4 (approved)	JAK1, JAK2, JAK3
ERLOTINIB	ChEMBL	Phase 4 (approved)	JAK2, JAK3, TYK2
ABIVERTINIB	ChEMBL	Phase 3	JAK1, JAK2, JAK3
ALVOCIDIB	ChEMBL	Phase 3	JAK2, JAK3, TYK2
DEFACTINIB	ChEMBL	Phase 3	JAK2, JAK3, TYK2
BMS-919373	ChEMBL	Phase 2	JAK2, JAK3, TYK2
CENISERTIB	ChEMBL	Phase 2	JAK2, JAK3, TYK2
LONDAMOCITINIB	ChEMBL	Phase 2	JAK1, JAK2, TYK2
belumosudil	PubChem	Approved	JAK2, JAK3, TYK2