Daprodustat
drugOn this page
Also known as GSK-1278863GSK1278863Jesduvroq
Summary
Daprodustat (CHEMBL3544988) is an approved small-molecule anti-anaemic agent (ATC B03XA07); indicated across 5 conditions including anemia and chronic kidney disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: B03XA07
- Indications: 5 conditions
- Clinical trials: 33
- Chemistry: 393.4 Da · C19H27N3O6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3544988 |
| Name | Daprodustat |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 91617630 |
| ChEBI | CHEBI:229223 |
| ATC | B03XA07 |
| Molecular formula | C19H27N3O6 |
| Molecular weight | 393.4 |
| InChIKey | RUEYEZADQJCKGV-UHFFFAOYSA-N |
SMILES: C1CCC(CC1)N2C(=O)C(C(=O)N(C2=O)C3CCCCC3)C(=O)NCC(=O)O
IUPAC name: 2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinane-5-carbonyl)amino]acetic acid
ChEBI definition: A member of the class of barbiturates that is barbituric acid substituted by cyclohexyl groups at positions 1 and 3, and by a (carboxymethyl)aminocarbonyl group at position 5. It is an inhibitor of hypoxia-inducible factor prolyl hydroxylase developed by GlaxoSmithKline for the treatment of anaemia in patients with chronic kidney disease.
Pharmacological roles (ChEBI): anti-anaemic agent, EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor, antiviral agent.
Also known as: Daprodustat, GSK-1278863, GSK1278863, Jesduvroq, DAPRODUSTAT
Patent coverage: 137 distinct patent families (308 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
Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Gamma-butyrobetaine dioxygenase, Bifunctional peptidase and arginyl-hydroxylase JMJD5, Aspartyl/asparaginyl beta-hydroxylase, Egl nine homolog 1, Hypoxia-inducible factor 1-alpha inhibitor.
Bioactivity
ChEMBL activities: 3 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| EGLN1 | 7.17 | IC50 | 67 | nM | CHEMBL_ACT_24960817 |
| EGLN1 | 6.75 | IC50 | 180 | nM | CHEMBL_ACT_29204492 |
| KDM8 | 5.07 | IC50 | 8500 | nM | CHEMBL_ACT_29204479 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
5 indications (3 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 |
|---|---|---|---|
| anemia | 4 | MONDO:0002280 | EFO:0004272 |
| chronic kidney disease | 4 | MONDO:0005300 | EFO:0003884 |
| peripheral vascular disease | 2 | MONDO:0005294 | EFO:0003875 |
| injury | 1 | MONDO:0021178 | EFO:0000546 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 33.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 12 |
| PHASE3 | 10 |
| PHASE1 | 9 |
| PHASE4 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05951192 | PHASE4 | COMPLETED | A Prospective Interventional Study Assessing the Clinical and Operational Effectiveness of Transitioning From Mircera to Daprodustat for the Treatment of Anemia in End Stage Kidney Disease |
| NCT07300111 | PHASE3 | NOT_YET_RECRUITING | A Study to Evaluate Efficacy and Safety of QLG1218(Daprodustat) in Chinese Hemodialysis (HD)-Dependent Subjects With Anemia Associated With Chronic Kidney Disease (CKD) |
| NCT02791763 | PHASE3 | COMPLETED | Phase III Study of GSK1278863 in Japanese Non-dialysis (ND) and Peritoneal Dialysis (PD) Subjects With Renal Anemia |
| NCT02829320 | PHASE3 | COMPLETED | Efficacy and Safety Study of GSK1278863 in Japanese Hemodialysis Subjects With Anemia Associated With Chronic Kidney Disease Who Are Not Taking Erythropoiesis Stimulating Agents |
| NCT02876835 | PHASE3 | COMPLETED | Anemia Studies in Chronic Kidney Disease: Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor Daprodustat-Non-Dialysis (ASCEND-ND) |
| NCT02879305 | PHASE3 | COMPLETED | Anemia Studies in Chronic Kidney Disease: Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor Daprodustat-Dialysis (ASCEND-D) |
| NCT02969655 | PHASE3 | COMPLETED | A Study to Evaluate Efficacy and Safety of Daprodustat Compared to Darbepoetin Alfa in Japanese Hemodialysis (HD)-Dependent Subjects With Anemia Associated With Chronic Kidney Disease (CKD) |
| NCT03029208 | PHASE3 | COMPLETED | Anemia Studies in Chronic Kidney Disease (CKD): Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat-in Incident Dialysis (ASCEND-ID) |
| NCT03400033 | PHASE3 | COMPLETED | Anemia Studies in Chronic Kidney Disease (CKD): Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat-Three-times Weekly Dosing in Dialysis (ASCEND-TD) |
| NCT03409107 | PHASE3 | COMPLETED | Anemia Studies in Chronic Kidney Disease (CKD): Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat in Non-Dialysis Subjects Evaluating Hemoglobin (Hgb) and Quality of Life (ASCEND-NHQ) |
| NCT05682326 | PHASE3 | COMPLETED | Anemia Studies in CKD: Erythropoiesis Via a Novel PHI Daprodustat - Pediatric (ASCEND-P) |
| NCT01587898 | PHASE2 | COMPLETED | 4 Week Correction Study in Subjects With Anemia Associated With Chronic Kidney Disease Who Are Not Undergoing Dialysis |
| NCT01587924 | PHASE2 | COMPLETED | 4 Week Switch Study in Hemodialysis-dependent Subjects With Anemia Associated With Chronic Kidney Disease |
| NCT01920594 | PHASE2 | COMPLETED | Study of GSK1278863 to Reduce Ischemic Events in Patients Undergoing Thoracic Aortic Aneurysm Repair |
| NCT01977482 | PHASE2 | COMPLETED | Evaluation of Dose Response Relationship, Safety and Efficacy of GSK1278863 in Hemodialysis-dependent Subjects With Chronic Kidney Disease Associated Anemia |
| NCT01977573 | PHASE2 | COMPLETED | A Study to Evaluate Safety and Efficacy of GSK1278863 in Non-Dialysis Dependent (NDD) Subjects With Anemia Associated With Chronic Kidney Diseases (CKD) |
| NCT02019719 | PHASE2 | COMPLETED | Study to Evaluate the Safety, Efficacy and Pharmacokinetics of GSK1278863 in Japanese Hemodialysis-Dependent Subjects With Anemia Associated With Chronic Kidney Disease |
| NCT02075463 | PHASE2 | TERMINATED | Study to Evaluate the Safety and Efficacy of GSK1278863 in Recombinant Human Erythropoietin (rhEPO) Hyporesponsive Hemodialysis-dependent Chronic Kidney Disease Subjects With Anemia |
| NCT02135848 | PHASE2 | COMPLETED | 3 Month PHI PAD PoM Study |
| NCT02689206 | PHASE2 | COMPLETED | Study to Evaluate the Efficacy, Safety and Pharmacokinetics of Three-times Weekly Dosing of GSK1278863 in Hemodialysis-dependent Subjects With Anemia Associated With Chronic Kidney Disease Who Are Switched From a Stable Dose of an Erythropoiesis-stimulating Agent |
| NCT03029247 | PHASE2 | COMPLETED | Anemia Study in Chronic Kidney Disease (CKD): Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat-Blood Pressure (ASCEND-BP) |
| NCT03446612 | PHASE2 | TERMINATED | Anemia Study in Chronic Kidney Disease (CKD) : Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat -Forearm Blood Flow (ASCEND-FBF) |
| NCT03457701 | PHASE2 | COMPLETED | Anemia Studies in CKD: Erythropoiesis Via a Novel Prolyl Hydroxylase Inhibitor (PHI) Daprodustat- Iron (ASCEND: Fe) |
| NCT01376232 | PHASE1 | COMPLETED | Study to Assess the Pharmacokinetics of GSK1278863A Coadministered With a High Fat Meal or an Inhibitor of CYP2C8 (Gemfibrozil) |
| NCT01406340 | PHASE1 | TERMINATED | Assessment of the Pharmacokinetics of GSK1278863 and Metabolites in Normal Subjects and Subjects With Renal Impairment |
| NCT01673555 | PHASE1 | COMPLETED | Effects of GSK1278863A on Pulmonary Artery Pressure in Healthy Volunteers |
| NCT01831804 | PHASE1 | COMPLETED | Safety, Tolerability, Pharmacokinetics and Pharmacodynamics Study of Single and Repeated Doses of Topical GSK1278863 |
| NCT02231190 | PHASE1 | COMPLETED | GSK1278863 Effects on Eccentric Exercise-Induced Muscle Damage |
| NCT02243306 | PHASE1 | COMPLETED | Study to Assess the Pharmacokinetics of GSK1278863 in Subjects With End Stage Renal Disease Undergoing Peritoneal Dialysis |
| NCT02293148 | PHASE1 | COMPLETED | Single Dose, Pharmacokinetic, Safety, Tolerability and QTc Study of GSK1278863 in Healthy Volunteers |
| NCT03223337 | PHASE1 | COMPLETED | Daprodustat Hepatic Impairment Study |
| NCT04640311 | PHASE1 | COMPLETED | Comparison of Daprodustat Formulations Produced by Two Methods of Manufacture for Bioequivalence and Dissolution in Healthy Participants |
| NCT07346547 | Not specified | NOT_YET_RECRUITING | REDCURE Registry for Chronic Kidney Disease (CKD) Anemia |
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.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: anemia, chronic kidney disease