PEMAFIBRATE

Possibly Marketed Outside US

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

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	MOL RATIO 1 MOL RATIO (average)

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

Description

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	Agonist 2,678		1.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyperlipidemia 80	Primary		Approved 8,429	Parmodia

C_max

Value	Dose	Analyte	Population
1.82 ng/mL	0.1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
1.54 ng/mL	0.1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
4.504 ng/mL	0.3 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
6.007 ng/mL	0.5 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
14.325 ng/mL	1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
1.175 ng/mL	0.1 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.172 ng/mL	0.1 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.328 ng/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.524 ng/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
6.374 ng/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
6.775 ng/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.401 ng/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.593 ng/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.968 ng/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
3.572 ng/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
6.334 ng/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
7.229 ng/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
0.5 ng/mL	0.1 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
0.52 ng/mL	0.1 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
0.87 ng/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
0.86 ng/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.36 ng/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.38 ng/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
5.57 ng/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
5.96 ng/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
4.59 ng/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
4.27 ng/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
8.86 ng/mL	0.8 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
9.25 ng/mL	0.8 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
17.11 ng/mL	1.6 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
17.94 ng/mL	1.6 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.42 ng/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.264 ng/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.517 ng/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.478 ng/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
3.015 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
6.78 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
11.564 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
4.01 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.983 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
4.986 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
3.504 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
5.229 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
3.928 ng/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
5.75 ng × h/mL	0.1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
5.18 ng × h/mL	0.1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
15.936 ng × h/mL	0.3 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
24.031 ng × h/mL	0.5 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
54.538 ng × h/mL	1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
4.468 ng × h/mL	0.1 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
4.04 ng × h/mL	0.1 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
9.239 ng × h/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
9.024 ng × h/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
25.608 ng × h/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
23.305 ng × h/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
4.884 ng × h/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
5.404 ng × h/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
10.975 ng × h/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
12.207 ng × h/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
25.858 ng × h/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
29.768 ng × h/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.36 ng × h/mL	0.1 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.63 ng × h/mL	0.1 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.74 ng × h/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
3.46 ng × h/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
7.27 ng × h/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
9.17 ng × h/mL	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
17.07 ng × h/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
22.67 ng × h/mL	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
12.69 ng × h/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
13.85 ng × h/mL	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
30.71 ng × h/mL	0.8 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
35.16 ng × h/mL	0.8 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
53.52 ng × h/mL	1.6 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
59.98 ng × h/mL	1.6 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
10.232 ng × h/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
10.499 ng × h/mL	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
5.59 ng × h/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
6.301 ng × h/mL	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
9.311 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
20.32 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
40.445 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
12.112 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
9.953 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
16.5 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
12.041 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
11.032 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
16.788 ng × h/mL	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
1.88 h	0.1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
1.73 h	0.1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.061 h	0.3 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.06 h	0.5 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.435 h	1 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
1.494 h	0.1 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.562 h	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.806 h	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.528 h	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.708 h	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.088 h	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.26 h	0.1 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.51 h	0.1 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.43 h	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.78 h	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.91 h	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.09 h	0.4 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.05 h	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.44 h	0.8 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.42 h	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.68 h	0.4 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.2 h	0.8 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.29 h	0.8 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
3.99 h	1.6 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
3.04 h	1.6 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.295 h	0.2 mg 1 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
2.043 h	0.2 mg 2 times / day multiple, oral	PEMAFIBRATE plasma	Homo sapiens
1.637 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.035 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
3.515 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.031 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.371 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.873 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.498 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.961 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens
2.978 h	0.2 mg single, oral	PEMAFIBRATE plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.15%			PEMAFIBRATE plasma	Homo sapiens

Doses

Doses

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Dose	Population	Adverse events
0.8 mg 2 times / day multiple, oral Highest studied dose	healthy, ADULT
1.6 mg single, oral Highest studied dose	healthy, ADULT

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PubMed

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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

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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
Record UNII	17VGG92R23
Record Status	`Validated (UNII)`
Record Version

Show entries

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

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Classification Tree

Code System

Code

Designated

FDA ORPHAN DRUG

934223

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Code System

Code

Type

Description

NCI_THESAURUS

C166474

PRIMARY

DRUG CENTRAL

5248

PRIMARY

CAS

848259-27-8

PRIMARY

WIKIPEDIA

Pemafibrate

PRIMARY

INN

9692

PRIMARY

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Related Record

Type

Details


					2PDN1S3FVX

PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR ALPHA

TARGET -> AGONIST

Qualification:

EC50

Amount:

0.08 NANOMOLAR (average)

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Related Record

Type

Details


					17VGG92R23

PEMAFIBRATE

ACTIVE MOIETY

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SMILES

InChI

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Funbound

Doses

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound