roxadustat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
hypoxia inducible factor (HIF) prolyl hydroxylase inhibitors 5371 808118-40-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • roxadustat
  • evrenzo
  • ASP 1517
  • AZD 9941
  • FG-4592
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.
  • Molecular weight: 352.35
  • Formula: C19H16N2O5
  • CLOGP: 4.73
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 108.75
  • ALOGS: -4.49
  • ROTB: 5

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
ATC B03XA05 BLOOD AND BLOOD FORMING ORGANS
ANTIANEMIC PREPARATIONS
OTHER ANTIANEMIC PREPARATIONS
Other antianemic preparations
CHEBI has role CHEBI:102248 EC 1.14.11.29 inhibitors
CHEBI has role CHEBI:132365 protocollagen hydroxylase inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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
Alpha-ketoglutarate-dependent dioxygenase FTO Unclassified IC50 5.01 CHEMBL
Prolyl 4-hydroxylase Unclassified Ki 5.97 CHEMBL

External reference:

IDSource
CHEBI:132774 CHEBI
CHEMBL2338329 ChEMBL_ID
D10593 KEGG_DRUG
C584543 MESH_SUPPLEMENTAL_RECORD_UI
8454 IUPHAR_LIGAND_ID
9717 INN_ID
DB04847 DRUGBANK_ID
X3O30D9YMX UNII
11256664 PUBCHEM_CID
C4310578 UMLSCUI
8HO PDB_CHEM_ID
018888 NDDF

Pharmaceutical products:

None