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

Stem definitionDrug idCAS RN
clofibrate derivatives, peroxisome proliferator activated receptor-alpha(PPAR-alpha) agonists 5248 848259-27-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pemafibrate
  • parmodia
  • K-877
  • (R)-K-13675
Pemafibrate is a selective PPAR-alpha modulator (SPPARM-alpha) that has antihyperlipidaemic activity.
  • Molecular weight: 490.56
  • Formula: C28H30N2O6
  • CLOGP: 6.23
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 1
  • TPSA: 94.26
  • ALOGS: -4.37
  • ROTB: 13

Drug dosage:

None

ADMET properties:

PropertyValueReference
CL (Clearance) 4.28 mL/min/kg Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
Vd (Volume of distribution) 0.91 L/kg Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
BA (Bioavailability) 0.62 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

DateAgencyCompanyOrphan
July 3, 2017 PMDA Kowa

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
Dyslipidemia indication 370992007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.58 acidic
pKa2 1.94 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
Peroxisome proliferator-activated receptor alpha Nuclear hormone receptor AGONIST EC50 9 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor AGONIST EC50 5.96 SCIENTIFIC LITERATURE
Peroxisome proliferator-activated receptor delta Nuclear hormone receptor AGONIST EC50 5.80 SCIENTIFIC LITERATURE

External reference:

IDSource
17VGG92R23 UNII
C4547051 UMLSCUI
CHEMBL247951 ChEMBL_ID
11526038 PUBCHEM_CID
DB15212 DRUGBANK_ID
D10711 KEGG_DRUG
CHEMBL3545412 ChEMBL_ID
9692 INN_ID
P7F PDB_CHEM_ID
C540740 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None