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

Stem definitionDrug idCAS RN
hypoxia inducible factor (HIF) prolyl hydroxylase inhibitors 5486 1154028-82-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • molidustat
  • molidustat sodium
  • musredo
  • BAY 85-3934
Molidustat (BAY 85–3934) is a novel, orally bioavailable HIF-PH inhibitor that mimics hypoxia by stabilizing HIF-a subunits. Molidustat inhibits HIF-PH, allowing the accumulation of HIF, which then translocates to the nucleus where it activates the transcription of erythropoietin (EPO) and other hypoxia-inducible genes, thereby increasing endogenous EPO levels and formation of the red blood cell.
  • Molecular weight: 314.31
  • Formula: C13H14N8O2
  • CLOGP: -0.48
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 1
  • TPSA: 101.30
  • ALOGS: -1.74
  • ROTB: 3

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 2021 PMDA BAYER YAKUHIN, Ltd

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:

None

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

DiseaseRelationSNOMED_IDDOID
Renal anemia indication 234348004




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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 6.55 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Egl nine homolog 2 Enzyme INHIBITOR IC50 6.32 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Egl nine homolog 3 Enzyme INHIBITOR IC50 6.35 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Hypoxia-inducible factor 1-alpha inhibitor Enzyme IC50 4.51 CHEMBL
Prolyl 4-hydroxylase Unclassified Ki 4.79 CHEMBL

External reference:

IDSource
A1H PDB_CHEM_ID
QEQ PDB_CHEM_ID
CHEMBL3646118 ChEMBL_ID
C000603972 MESH_SUPPLEMENTAL_RECORD_UI
8456 IUPHAR_LIGAND_ID
1375799-59-9 SECONDARY_CAS_RN
DB15642 DRUGBANK_ID
D11273 KEGG_DRUG
C4078705 UMLSCUI
CHEMBL3931782 ChEMBL_ID
9655 INN_ID
59603622 PUBCHEM_CID
2637534 RXNORM
9JH486CZ13 UNII

Pharmaceutical products:

None