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

Stem definitionDrug idCAS RN
calcium-sensing receptors (CaSR) agonists 5307 870964-67-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • evocalcet
  • orkedia
  • KHK-7580
  • KHK7580
  • MT-4580
Evocalcet is a new type of oral calcimimetics agent. The drug suppresses parathyroid hormone secretion by acting on the calcium receptors on parathyroid gland cells.
  • Molecular weight: 374.48
  • Formula: C24H26N2O2
  • CLOGP: 2.14
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 52.57
  • ALOGS: -5.22
  • ROTB: 6

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 0.63 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

DateAgencyCompanyOrphan
March 23, 2018 PMDA Kyowa Hakko Kirin Co., Ltd.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Shunt stenosis 94.84 60.19 12 67 770 34956082

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Shunt stenosis 162.19 56.62 20 117 1371 79742880
Shunt occlusion 98.44 56.62 13 124 1491 79742760

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

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

DiseaseRelationSNOMED_IDDOID
Hypercalcemia in primary hyperparathyroidism indication 2243000
Hypercalcemia in parathyroid carcinoma indication 47709007
Secondary hyperparathyroidism indication 91478007 DOID:12466




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.32 acidic
pKa2 8.08 Basic
pKa3 4.84 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
Extracellular calcium-sensing receptor GPCR AGONIST EC50 7.03 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
E58MLH082P UNII
C4519114 UMLSCUI
H43 PDB_CHEM_ID
CHEMBL4297621 ChEMBL_ID
71242808 PUBCHEM_CID
DB12388 DRUGBANK_ID
D11063 KEGG_DRUG
10098 INN_ID
9042 IUPHAR_LIGAND_ID
C000631688 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None