PEMAFIBRATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C28H30N2O6
Molecular Weight	490.5476
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC[C@@H](OC1=CC=CC(CN(CCCOC2=CC=C(OC)C=C2)C3=NC4=CC=CC=C4O3)=C1)C(O)=O

InChI

InChIKey=ZHKNLJLMDFQVHJ-RUZDIDTESA-N

InChI=1S/C28H30N2O6/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)/t25-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C28H30N2O6
Molecular Weight	490.5476
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28929345 | http://adisinsight.springer.com/drugs/800032781

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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Peroxisome proliferator-activated receptor alpha 62 Target ID: CHEMBL239 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17553678	Agonist 2678		1.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyperlipidemia 80 Sources: http://adisinsight.springer.com/drugs/800032781 https://www.ncbi.nlm.nih.gov/pubmed/28929345	Primary		Approved 8429	Parmodia Approved Use Indicated for the treatment of hyperlipidaemia. Launch Date 2017

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	28195199
Phase 2 clinical trials with K-877 (pemafibrate): A promising selective PPAR-α modulator for treatment of combined dyslipidemia.	2017 Jun	28434555
Pemafibrate: First Global Approval.	2017 Oct	28929345
A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice.	2018 Feb 1	28781340

Patents

Sample Use Guides

In Vivo Use Guide

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

Pemafibrate (K-877) (10uM) significantly decreased apoB secretion.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 21:32:10 GMT 2023` Edited by `admin` on `Fri Dec 15 21:32:10 GMT 2023`
Record UNII	17VGG92R23
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PEMAFIBRATE

Official Name

English

K-13675, (R)-

Common Name

English

(R)-K-13675

Code

English

pemafibrate [INN]

Common Name

English

Pemafibrate [WHO-DD]

Common Name

English

(R)-2-(3-((N-(BENZOXAZOL-2-YL)-N-(3-(4-METHOXYPHENOXY)PROPYL)AMINO)METHYL)PHENOXY)BUTANOIC ACID

Systematic Name

English

PEMAFIBRATE [MI]

Common Name

English

PEMAFIBRATE [JAN]

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

934223