Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C28H29N2O6.Na |
| Molecular Weight | 512.5294 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].CC[C@@H](OC1=CC=CC(CN(CCCOC2=CC=C(OC)C=C2)C3=NC4=CC=CC=C4O3)=C1)C([O-])=O
InChI
InChIKey=JSNXVHCVJMDNKW-VQIWEWKSSA-M
InChI=1S/C28H30N2O6.Na/c1-3-25(27(31)32)35-23-9-6-8-20(18-23)19-30(28-29-24-10-4-5-11-26(24)36-28)16-7-17-34-22-14-12-21(33-2)13-15-22;/h4-6,8-15,18,25H,3,7,16-17,19H2,1-2H3,(H,31,32);/q;+1/p-1/t25-;/m1./s1
Pemafibrate (Parmodia®) is a novel, highly selective peroxisome proliferator-activated receptor (PPAR)-α modulator (SPPARM). It acts by binding to PPAR-α and regulating the expression of target genes that modulate lipid metabolism, thereby decreasing plasma triglyceride levels and increasing high-density lipoprotein cholesterol levels. Developed by Kowa Company, Ltd., oral pemafibrate has been approved in Japan for the treatment of hyperlipidaemia (including familial hyperlipidaemia). Pemafibrate is undergoing phase III development in a
number of countries for the treatment of dyslipidaemias
and is also in phase III development for the treatment of
hypertriglyceridaemia.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pemafibrate, a novel selective peroxisome proliferator-activated receptor alpha modulator, improves the pathogenesis in a rodent model of nonalcoholic steatohepatitis. | 2017 Feb 14 |
|
| Phase 2 clinical trials with K-877 (pemafibrate): A promising selective PPAR-α modulator for treatment of combined dyslipidemia. | 2017 Jun |
|
| Pemafibrate: First Global Approval. | 2017 Oct |
Patents
Sample Use Guides
The recommended
dosage of oral pemafibrate is 0.1 mg twice daily
(administered in the morning and evening); this dosage can
be adjusted according to age and symptoms to a maximum
dosage of 0.2 mg twice daily.
Route of Administration:
Oral
In Vitro Use Guide
Curator's Comment: To test for a direct effect on apoB secretion by intestinal epithelial cells, polarized
Caco-2/TC7 cells grown and polarized on a porous filter to mimic the human
intestinal barrier, were treated with the different PPARα ligands added to the apical
side. After 24 hours, medium in the basolateral compartment was collected,
chylomicrons isolated by centrifugation and apoB quantified by ELISA.
Pemafibrate (K-877) (10uM) significantly decreased apoB
secretion.
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950644-31-2
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91826962
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321L8P020Q
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SUBSTANCE RECORD
