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roxadustat 🐶 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 | 5371 | 808118-40-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Roxadustat is a first-in-class orally administered inhibitor of hypoxia-inducible factor (HIF) prolylhydroxylase that corrects anemia by activating a response that occurs naturally when the body responds to reduced oxygen levels in the blood. The response activated by roxadustat involves the regulation of multiple, complementary processes to promote erythropoiesis and increase the blood’s oxygen-carrying capacity.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 43 | mg | O |
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,EGFR,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,MAP2K6,MAP3K21,MAPK7,MAPKAPK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKDC,STK33,TEK,TGFBR1,TTK,ZAP70 | 35 | |||
| kinase-selectivity-class | GRK2,PIK3CD | 2 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 17.989 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| rat-kpuu-brain | Rat brain Kpuu | 0.023 | % | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 18, 2021 | EMA | ASTELLAS PHARMA EUROPE B.V. | |
| Sept. 20, 2019 | PMDA | Astellas Pharma Inc. |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B03XA05 | BLOOD AND BLOOD FORMING ORGANS ANTIANEMIC PREPARATIONS OTHER ANTIANEMIC PREPARATIONS Other antianemic preparations |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:75835 | anti-anaemic agent |
| CHEBI has role | CHEBI:102248 | EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor |
| CHEBI has role | CHEBI:132365 | EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
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 |
|---|---|---|---|
| Refractory anemia (clinical) | indication | 109996008 | |
| Anemia in chronic kidney disease | indication | 707323002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.34 | acidic |
| pKa2 | 7.78 | acidic |
| pKa3 | 12.33 | acidic |
| pKa4 | 4.24 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
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 | 4.54 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Egl nine homolog 2 | Enzyme | INHIBITOR | IC50 | 5.24 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Egl nine homolog 3 | Enzyme | INHIBITOR | IC50 | 5.18 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Gamma-butyrobetaine dioxygenase | Enzyme | IC50 | 5.09 | CHEMBL | |||||
| Thyroid hormone receptor alpha | Nuclear hormone receptor | EC50 | 7.49 | CHEMBL | |||||
| Alpha-ketoglutarate-dependent dioxygenase FTO | Enzyme | IC50 | 5.01 | CHEMBL | |||||
| Thyroid hormone receptor beta | Nuclear hormone receptor | EC50 | 7.89 | CHEMBL | |||||
| Aspartyl/asparaginyl beta-hydroxylase | Enzyme | IC50 | 4.71 | CHEMBL | |||||
| Prolyl 4-hydroxylase | Enzyme | Ki | 5.97 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| CHEBI:132774 | CHEBI |
| CHEMBL2338329 | ChEMBL_ID |
| D10593 | KEGG_DRUG |
| C584543 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8454 | IUPHAR_LIGAND_ID |
| DB04847 | DRUGBANK_ID |
| 1287404005 | SNOMEDCT_US |
| 1287447005 | SNOMEDCT_US |
| C4310578 | UMLSCUI |
| 8HO | PDB_CHEM_ID |
| 9717 | INN_ID |
| 11256664 | PUBCHEM_CID |
| 018888 | NDDF |
| X3O30D9YMX | UNII |
| X3O30D9YMX | INXIGHT DRUGS |
Pharmaceutical products:
None