Desidustat
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Also known as Zyan-1ZYAN1
Summary
Desidustat (CHEMBL4650314) is a phase-3 clinical-stage small molecule targeting EGLN2; indicated across 3 conditions including chronic kidney disease and severe acute respiratory syndrome.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (EGLN2)
- Indications: 3 conditions
- Clinical trials: 5
- Chemistry: 332.31 Da · C16H16N2O6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL4650314 |
| Name | Desidustat |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 75593290 |
| Molecular formula | C16H16N2O6 |
| Molecular weight | 332.31 |
| InChIKey | IKRKQQLJYBAPQT-UHFFFAOYSA-N |
SMILES: C1CC1CON2C3=CC=CC=C3C(=C(C2=O)C(=O)NCC(=O)O)O
IUPAC name: 2-[[1-(cyclopropylmethoxy)-4-hydroxy-2-oxoquinoline-3-carbonyl]amino]acetic acid
Also known as: Desidustat, Zyan-1, ZYAN1, DESIDUSTAT
Patent coverage: 110 distinct patent families (254 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 224 (88%) 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 |
|---|---|---|---|---|---|
| EGLN2 | egl-9 family hypoxia inducible factor 2 | Inhibition | 4.6% | Q96KS0 |
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 | 6.38 | IC50 | 420 | nM | CHEMBL_ACT_29204379 |
| EGLN1 | 5.89 | IC50 | 1300 | nM | CHEMBL_ACT_29204490 |
| ASPH | 5 | IC50 | 9900 | nM | CHEMBL_ACT_29204499 |
Target pathways
Aggregated over 1 target gene(s): EGLN2.
Top Reactome pathways
1 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Oxygen-dependent proline hydroxylation of Hypoxia-inducible Factor Alpha | 1 | EGLN2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| regulation of cell growth | 1 |
| response to hypoxia | 1 |
| peptidyl-proline hydroxylation to 4-hydroxy-L-proline | 1 |
| estrogen receptor signaling pathway | 1 |
| regulation of neuron apoptotic process | 1 |
| cell redox homeostasis | 1 |
| positive regulation of protein catabolic process | 1 |
| cellular response to hypoxia | 1 |
Indications & clinical
Indications
3 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 |
|---|---|---|---|
| chronic kidney disease | 3 | MONDO:0005300 | EFO:0009909 |
| severe acute respiratory syndrome | 2 | MONDO:0005091 | MONDO:0100096 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 5.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 2 |
| PHASE4 | 1 |
| PHASE2 | 1 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05515367 | PHASE4 | RECRUITING | A Post Marketing Surveillance to Evaluate the Safety of Desidustat for the Treatment of Anemia in Subjects With Chronic Kidney Disease (CKD).(Real World Evidence Study) |
| NCT04012957 | PHASE3 | COMPLETED | Desidustat in the Treatment of Anemia in CKD |
| NCT04215120 | PHASE3 | COMPLETED | Desidustat in the Treatment of Anemia in CKD on Dialysis Patients |
| NCT04463602 | PHASE2 | COMPLETED | Desidustat in the Management of COVID-19 Patients |
| NCT04667533 | PHASE1 | COMPLETED | Desidustat in the Treatment of Chemotherapy Induced Anemia |
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.
5 molecules share ≥1 primary target. Top 5 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| MOLIDUSTAT | ChEMBL + PubChem | Phase 2 (approved) | EGLN2 |
| anhydrous citric acid | PubChem | Approved | EGLN2 |
| ascorbic acid | PubChem | Approved | EGLN2 |
| Malic Acid | PubChem | Approved | EGLN2 |
| Oxygen | PubChem | Approved | EGLN2 |
Related Atlas pages
- Genes: EGLN2
- Diseases: chronic kidney disease
- Drugs: anhydrous citric acid, ascorbic acid, Oxygen