Enarodustat

Summary

Enarodustat (CHEMBL4297619) is a phase-3 clinical-stage small molecule targeting EGLN1; indicated across 1 condition including chronic kidney disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (EGLN1)
• Indications: 1 condition
• Clinical trials: 9
• Chemistry: 340.33 Da · C17H16N4O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL4297619
Name	Enarodustat
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	50899324
Molecular formula	C17H16N4O4
Molecular weight	340.33
InChIKey	FJYRBJKWDXVHHO-UHFFFAOYSA-N

SMILES: C1=CC=C(C=C1)CCC2=CC(=O)C(=C3N2NC=N3)C(=O)NCC(=O)O

IUPAC name: 2-[[7-oxo-5-(2-phenylethyl)-3H-[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl]amino]acetic acid

Also known as: Enarodustat, Jtz-951, JTZ-951, ENARODUSTAT

Parent form; salt/anhydrous children: CHEMBL4166742

Patent coverage: 54 distinct patent families (109 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).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
EGLN1	egl-9 family hypoxia inducible factor 1	Inhibition	6.66	16.6%	Q9GZT9

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Gamma-butyrobetaine dioxygenase, Bifunctional peptidase and arginyl-hydroxylase JMJD5, Aspartyl/asparaginyl beta-hydroxylase, Egl nine homolog 1.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
BBOX1	7	IC50	100	nM	CHEMBL_ACT_29204380
EGLN1	6.42	IC50	380	nM	CHEMBL_ACT_29204491
ASPH	5.02	IC50	9600	nM	CHEMBL_ACT_29204500

Target pathways

Aggregated over 1 target gene(s): EGLN1.

Top Reactome pathways

1 total, by targets touching each:

Pathway	Targets	Genes
Oxygen-dependent proline hydroxylation of Hypoxia-inducible Factor Alpha	1	EGLN1

Dominant GO biological processes

GO term	Targets
response to hypoxia	1
intracellular iron ion homeostasis	1
intracellular oxygen homeostasis	1
regulation of neuron apoptotic process	1
regulation of angiogenesis	1
positive regulation of transcription by RNA polymerase II	1
cardiac muscle tissue morphogenesis	1
heart trabecula formation	1
ventricular septum morphogenesis	1
labyrinthine layer development	1
cellular response to hypoxia	1
response to nitric oxide	1
regulation of modification of postsynaptic structure	1
regulation protein catabolic process at postsynapse	1
negative regulation of hypoxia-inducible factor-1alpha signaling pathway	1

Indications & clinical

Indications

1 indication (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
chronic kidney disease	3	MONDO:0005300	EFO:0003884

Clinical trials

Total trials: 9.

Phase distribution

Phase	Trials
PHASE1	4
PHASE3	3
PHASE4	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06725810	PHASE4	RECRUITING	Correction of Anemia With Enarodustat in Non-dialysis Dependent Chronic Kidney Disease
NCT07079579	PHASE4	NOT_YET_RECRUITING	Enarodustat Tablets at Different Initial Doses for Anemia in Non-dialysis CKD Patients
NCT07522996	PHASE3	NOT_YET_RECRUITING	Enarodustat+CsA vs CsA in the Treatment of Newly-diagnosed TD-NSAA
NCT07548671	PHASE3	NOT_YET_RECRUITING	Enarodustat + CsA vs CsA in Newly Diagnosed TD-NSAA
NCT04027517	PHASE3	COMPLETED	A Study to Evaluate Efficacy and Safety of JTZ-951 Compared to Darbepoetin Alfa in Korean Renal Anemia Patients Receiving Hemodialysis.
NCT01971164	PHASE1	COMPLETED	Safety, Tolerability, PK & PD Study of JTZ-951 in Anemic Subjects With End-stage Renal Disease
NCT01978587	PHASE1	COMPLETED	Effect of Hemodialysis on the PK of JTZ-951 in Subjects With End-stage Renal Disease
NCT02581124	PHASE1	COMPLETED	Study to Evaluate Effect of Lapatinib on Pharmacokinetics of JTZ-951 in Subjects With End-stage Renal Disease
NCT02805244	PHASE1	COMPLETED	Mass Balance Study of JTZ-951 in Subjects With End-stage Renal Disease on Hemodialysis

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.

9 molecules share ≥1 primary target. Top 9 by shared-target count:

Molecule	Source	Status	Shared targets
VADADUSTAT	ChEMBL + PubChem	Phase 4 (approved)	EGLN1
DAPRODUSTAT	ChEMBL	Phase 4 (approved)	EGLN1
ROXADUSTAT	ChEMBL	Phase 4 (approved)	EGLN1
DESIDUSTAT	ChEMBL	Phase 3	EGLN1
FUMARIC ACID	ChEMBL	Phase 3	EGLN1
SUCCINIC ACID	ChEMBL	Phase 3	EGLN1
IZILENDUSTAT	ChEMBL	Phase 2	EGLN1
MOLIDUSTAT	ChEMBL	Phase 2	EGLN1
anhydrous citric acid	PubChem	Approved	EGLN1