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daprodustat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| hypoxia inducible factor (HIF) prolyl hydroxylase inhibitors | 5421 | 960539-70-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Daprodustat is a small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase (PHD) developed for the treatment of anaemia in patients with chronic kidney disease (CKD). Inhibition of PHD prevents degradation of hypoxia-inducible factor (HIF), leading to the production of erythropoietin and subsequent induction of erythropoiesis.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 39 | |||
| kinase-selectivity-class | AXL,GRK2,TTK | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 29, 2020 | PMDA | GlaxoSmithKline | |
| Feb. 1, 2023 | FDA | GLAXOSMITHKLINE |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Haemoglobin increased | 51.22 | 41.47 | 11 | 462 | 7470 | 90620504 |
| Renal impairment | 49.21 | 41.47 | 19 | 454 | 105402 | 90522572 |
| Cerebral infarction | 46.33 | 41.47 | 13 | 460 | 26583 | 90601391 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Haemoglobin increased | 75.35 | 39.26 | 17 | 894 | 9130 | 110579258 |
| Cerebral infarction | 65.41 | 39.26 | 22 | 889 | 51816 | 110536572 |
| Renal impairment | 57.87 | 39.26 | 29 | 882 | 188416 | 110399972 |
| Cardiac failure | 55.04 | 39.26 | 28 | 883 | 187598 | 110400790 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B03XA07 | BLOOD AND BLOOD FORMING ORGANS ANTIANEMIC PREPARATIONS OTHER ANTIANEMIC PREPARATIONS Other antianemic preparations |
| FDA MoA | N0000194079 | Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors |
| FDA EPC | N0000194080 | Hypoxia-inducible Factor Prolyl Hydroxylase Inhibitor |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:73336 | vulnerary |
| CHEBI has role | CHEBI:75835 | anti-anaemic agent |
| CHEBI has role | CHEBI:102248 | EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor |
Related Drugs by ATC class:
B03XA Other antianemic preparations 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Anemia of renal disease | indication | 234348004 | |
| Anemia in chronic kidney disease | indication | 707323002 | |
| Uncontrolled hypertension | contraindication | 38341003 | DOID:10763 |
| Concomitant administration of strong CYP2C8 inhibitors | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 1MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11643397 | June 22, 2027 | A METHOD OF TREATING ANEMIA |
| 1MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8557834 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 1MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8815884 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 2MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11643397 | June 22, 2027 | A METHOD OF TREATING ANEMIA |
| 2MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8557834 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 2MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8815884 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 4MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11643397 | June 22, 2027 | A METHOD OF TREATING ANEMIA |
| 4MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8557834 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 4MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8815884 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 6MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11643397 | June 22, 2027 | A METHOD OF TREATING ANEMIA |
| 6MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8557834 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 6MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8815884 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 8MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11643397 | June 22, 2027 | A METHOD OF TREATING ANEMIA |
| 8MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8557834 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 8MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 8815884 | June 22, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE |
| 1MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11117871 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 1MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11649217 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 2MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11117871 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 2MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11649217 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 4MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11117871 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 4MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11649217 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 6MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11117871 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 6MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11649217 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 8MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11117871 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
| 8MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | 11649217 | March 13, 2038 | A METHOD OF TREATING ANEMIA |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 1MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | Feb. 1, 2028 | NEW CHEMICAL ENTITY |
| 2MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | Feb. 1, 2028 | NEW CHEMICAL ENTITY |
| 4MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | Feb. 1, 2028 | NEW CHEMICAL ENTITY |
| 6MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | Feb. 1, 2028 | NEW CHEMICAL ENTITY |
| 8MG | JESDUVROQ | GLAXOSMITHKLINE | N216951 | Feb. 1, 2023 | DISCN | TABLET | ORAL | Feb. 1, 2028 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Egl nine homolog 1 | Enzyme | INHIBITOR | IC50 | 8.46 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Egl nine homolog 2 | Enzyme | INHIBITOR | IC50 | 8.14 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Egl nine homolog 3 | Enzyme | INHIBITOR | IC50 | 8.26 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Aspartyl/asparaginyl beta-hydroxylase | Enzyme | IC50 | 4.96 | CHEMBL | |||||
| Gamma-butyrobetaine dioxygenase | Enzyme | IC50 | 4.89 | CHEMBL | |||||
| Hypoxia-inducible factor 1-alpha inhibitor | Enzyme | IC50 | 4.68 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D10874 | KEGG_DRUG |
| JVR38ZM64B | UNII |
| C4519188 | UMLSCUI |
| CHEBI:229223 | CHEBI |
| CHEMBL3544988 | ChEMBL_ID |
| 91617630 | PUBCHEM_CID |
| DB11682 | DRUGBANK_ID |
| 10167 | INN_ID |
| C000599718 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8455 | IUPHAR_LIGAND_ID |
| 4042585 | VANDF |
| A0W | PDB_CHEM_ID |
| 364979 | MMSL |
| 41216 | MMSL |
| d09985 | MMSL |
| 019290 | NDDF |
| 2628210 | RXNORM |
| JVR38ZM64B | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Jesduvroq | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0897 | TABLET, FILM COATED | 1 mg | ORAL | NDA | 30 sections |
| Jesduvroq | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0903 | TABLET, FILM COATED | 2 mg | ORAL | NDA | 30 sections |
| Jesduvroq | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0906 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 30 sections |
| Jesduvroq | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0911 | TABLET, FILM COATED | 6 mg | ORAL | NDA | 30 sections |
| Jesduvroq | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0914 | TABLET, FILM COATED | 8 mg | ORAL | NDA | 30 sections |