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(CN(CCCOC2=CC=C(OC)C=C2)C3=NC4=C(O3)C=CC=C4)=CC=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
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.82 ng/mL |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.54 ng/mL |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.504 ng/mL |
0.3 mg single, oral dose: 0.3 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.007 ng/mL |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
14.325 ng/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.175 ng/mL |
0.1 mg 1 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.172 ng/mL |
0.1 mg 1 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2.328 ng/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2.524 ng/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
6.374 ng/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
6.775 ng/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.401 ng/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.593 ng/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2.968 ng/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
3.572 ng/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
6.334 ng/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
7.229 ng/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
0.5 ng/mL |
0.1 mg 2 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
0.52 ng/mL |
0.1 mg 2 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
0.87 ng/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
0.86 ng/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.36 ng/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.38 ng/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
5.57 ng/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
5.96 ng/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
4.59 ng/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
4.27 ng/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
8.86 ng/mL |
0.8 mg 1 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
9.25 ng/mL |
0.8 mg 1 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
17.11 ng/mL |
1.6 mg 1 times / day multiple, oral dose: 1.6 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
17.94 ng/mL |
1.6 mg 1 times / day multiple, oral dose: 1.6 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.42 ng/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
2.264 ng/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
1.517 ng/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
1.478 ng/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
3.015 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.78 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.564 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.01 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.983 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.986 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.504 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
5.229 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.928 ng/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.75 ng × h/mL |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5.18 ng × h/mL |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
15.936 ng × h/mL |
0.3 mg single, oral dose: 0.3 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
24.031 ng × h/mL |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
54.538 ng × h/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.468 ng × h/mL |
0.1 mg 1 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.04 ng × h/mL |
0.1 mg 1 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
9.239 ng × h/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
9.024 ng × h/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
25.608 ng × h/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
23.305 ng × h/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
4.884 ng × h/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
5.404 ng × h/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
10.975 ng × h/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
12.207 ng × h/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
25.858 ng × h/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
29.768 ng × h/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.36 ng × h/mL |
0.1 mg 2 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1.63 ng × h/mL |
0.1 mg 2 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.74 ng × h/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
3.46 ng × h/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
7.27 ng × h/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
9.17 ng × h/mL |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
17.07 ng × h/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
22.67 ng × h/mL |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
12.69 ng × h/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
13.85 ng × h/mL |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
30.71 ng × h/mL |
0.8 mg 1 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
35.16 ng × h/mL |
0.8 mg 1 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
53.52 ng × h/mL |
1.6 mg 1 times / day multiple, oral dose: 1.6 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
59.98 ng × h/mL |
1.6 mg 1 times / day multiple, oral dose: 1.6 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
10.232 ng × h/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
10.499 ng × h/mL |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
5.59 ng × h/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
6.301 ng × h/mL |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
9.311 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.32 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
40.445 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
12.112 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
9.953 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
16.5 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
12.041 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
11.032 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
16.788 ng × h/mL |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.88 h |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.73 h |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2.061 h |
0.3 mg single, oral dose: 0.3 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.06 h |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.435 h |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1.494 h |
0.1 mg 1 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.562 h |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.806 h |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.528 h |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.708 h |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2.088 h |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
1.26 h |
0.1 mg 2 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1.51 h |
0.1 mg 2 times / day multiple, oral dose: 0.1 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1.43 h |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1.78 h |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1.91 h |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.09 h |
0.4 mg 2 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.05 h |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.44 h |
0.8 mg 2 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1.42 h |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1.68 h |
0.4 mg 1 times / day multiple, oral dose: 0.4 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.2 h |
0.8 mg 1 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.29 h |
0.8 mg 1 times / day multiple, oral dose: 0.8 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
3.99 h |
1.6 mg 1 times / day multiple, oral dose: 1.6 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
3.04 h |
1.6 mg 1 times / day multiple, oral dose: 1.6 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2.295 h |
0.2 mg 1 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
2.043 h |
0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FED |
|
1.637 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.035 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
3.515 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.031 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.371 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.873 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.498 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.961 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.978 h |
0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered: |
PEMAFIBRATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.15% |
PEMAFIBRATE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
0.8 mg 2 times / day multiple, oral Highest studied dose Dose: 0.8 mg, 2 times / day Route: oral Route: multiple Dose: 0.8 mg, 2 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FED Sources: |
|
1.6 mg single, oral Highest studied dose Dose: 1.6 mg Route: oral Route: single Dose: 1.6 mg Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FED Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| A Novel Selective PPARα Modulator (SPPARMα), K-877 (Pemafibrate), Attenuates Postprandial Hypertriglyceridemia in Mice. | 2018-02-01 |
|
| Pemafibrate: First Global Approval. | 2017-10 |
|
| Phase 2 clinical trials with K-877 (pemafibrate): A promising selective PPAR-α modulator for treatment of combined dyslipidemia. | 2017-06 |
|
| Pemafibrate, a novel selective peroxisome proliferator-activated receptor alpha modulator, improves the pathogenesis in a rodent model of nonalcoholic steatohepatitis. | 2017-02-14 |
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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91826962
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321L8P020Q
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SUBSTANCE RECORD
