Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H16F2N8O2 |
Molecular Weight | 426.3795 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC(=O)NC1=C(N)N=C(N=C1N)C2=NN(CC3=CC=CC=C3F)C4=NC=C(F)C=C24
InChI
InChIKey=QZFHIXARHDBPBY-UHFFFAOYSA-N
InChI=1S/C19H16F2N8O2/c1-31-19(30)25-14-15(22)26-17(27-16(14)23)13-11-6-10(20)7-24-18(11)29(28-13)8-9-4-2-3-5-12(9)21/h2-7H,8H2,1H3,(H,25,30)(H4,22,23,26,27)
Molecular Formula | C19H16F2N8O2 |
Molecular Weight | 426.3795 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2111348 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28557445 |
1005.0 nM [EC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
350 μg/L |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
41 μg/L |
1.25 mg single, oral dose: 1.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
106 μg/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
176 μg/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
115 μg/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
72 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
129 μg/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
279 μg/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
202 μg/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
274 μg/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
195 μg/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
61.8 μg/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
236 μg/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
324 μg/L |
7.5 mg 1 times / day multiple, oral dose: 7.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
365 μg/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
46.4 μg/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
161 μg/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
242 μg/L |
7.5 mg 1 times / day multiple, oral dose: 7.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
285 μg/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
89.2 μg/L |
1.25 mg 1 times / day steady-state, oral dose: 1.25 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
289 μg/L |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
407 μg/L |
7.5 mg 1 times / day steady-state, oral dose: 7.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
472 μg/L |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.2 μg/L |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
39.3 μg/L |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
82.7 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
158 μg/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
194 μg/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
259 μg/L |
7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
285 μg/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
430 μg/L |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
38.5 μg/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
114 μg/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
200 μg/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
136 μg/L |
5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
51.4 μg/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
185 μg/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
310 μg/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
312 μg/L |
5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
83.1 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
76.2 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
92.7 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
91.4 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
66.6 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
69.5 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
68.7 μg/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6680 μg × h/mL |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
754 μg × h/L |
1.25 mg single, oral dose: 1.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2300 μg × h/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3260 μg × h/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2730 μg × h/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
1360 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2520 μg × h/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
5480 μg × h/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
3890 μg × h/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
5600 μg × h/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
3890 μg × h/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
703 μg × h/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2540 μg × h/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3230 μg × h/L |
7.5 mg 1 times / day multiple, oral dose: 7.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4410 μg × h/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
666 μg × h/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
2370 μg × h/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
3300 μg × h/L |
7.5 mg 1 times / day multiple, oral dose: 7.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
4340 μg × h/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
1170 μg × h/L |
1.25 mg 1 times / day steady-state, oral dose: 1.25 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3670 μg × h/L |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4810 μg × h/L |
7.5 mg 1 times / day steady-state, oral dose: 7.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6170 μg × h/L |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
273 μg × h/L |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
618 μg × h/L |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1450 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2900 μg × h/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2500 μg × h/L |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4460 μg × h/L |
7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4940 μg × h/L |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
7900 μg × h/L |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
423 μg × h/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1370 μg × h/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2240 μg × h/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
951 μg × h/L |
5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
656 μg × h/L |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2230 μg × h/L |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
3840 μg × h/L |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2600 μg × h/L |
5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
1330 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1390 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2200 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
2940 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1550 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1780 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
1250 μg × h/L |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20 h |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
18.8 h |
1.25 mg single, oral dose: 1.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.4 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
21.4 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
18.9 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT |
|
18.5 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
18.1 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
17.6 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
18.2 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
18 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
18.9 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
22.3 h |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
21.1 h |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.9 h |
7.5 mg 1 times / day multiple, oral dose: 7.5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
18.3 h |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
27 h |
1.25 mg 1 times / day steady-state, oral dose: 1.25 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
23.5 h |
5 mg 1 times / day steady-state, oral dose: 5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
22.1 h |
7.5 mg 1 times / day steady-state, oral dose: 7.5 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.7 h |
10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.2 h |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
19.4 h |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
19.4 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
19.8 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
14.5 h |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
19.8 h |
7.5 mg single, oral dose: 7.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.7 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
17.2 h |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
25.7 h |
1.25 mg 1 times / day multiple, oral dose: 1.25 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
24.7 h |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
19.9 h |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.7 h |
5 mg 2 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
20.7 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
17.1 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
32.1 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
36.9 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
19.8 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
23.7 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
20.2 h |
2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
VERICIGUAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2% |
VERICIGUAT plasma | Homo sapiens |
Doses
Dose | Population | Adverse events |
---|---|---|
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Disc. AE: Embryo-fetal toxicity... AEs leading to discontinuation/dose reduction: Embryo-fetal toxicity Sources: |
10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Hypotension, Syncope... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Embryo-fetal toxicity | Disc. AE | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Hypotension | 15.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Syncope | 4.4% | 10 mg 1 times / day multiple, oral Recommended Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02861534
Starting dose of 2.5 mg taken orally once daily with food, on a background of standard of care. Dose will be uptitrated to 5 mg and to 10 mg.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28557445
Studies on the in
vitro effects of Vericiguat on highly purified sGC (soluble guanylate cyclase) revealed that Vericiguat (0.01
uM to 100 uM) stimulates recombinant sGC concentration
dependently, by 1.7-fold to 57.6-fold.
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:44:51 GMT 2025
by
admin
on
Mon Mar 31 21:44:51 GMT 2025
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Record UNII |
LV66ADM269
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Record Status |
Validated (UNII)
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Record Version |
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Common Name | English | ||
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Code | English | ||
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Common Name | English |
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NCI_THESAURUS |
C29707
Created by
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LV66ADM269
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Vericiguat
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142432
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9805
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DB15456
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LV66ADM269
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DTXSID001318361
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100000175190
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C152862
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1350653-20-1
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54674461
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2475830
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GH-146
Created by
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> SUBSTRATE |
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BINDER->LIGAND |
Protein binding (primarily to serum albumin) of vericiguat is about 98%.
BINDING
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TRANSPORTER -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE |
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TARGET -> ACTIVATOR |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Volume of Distribution | PHARMACOKINETIC |
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IN HEALTHY SUBJECTS PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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FASTED STATE PHARMACOKINETIC |
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ABSOLUTE BIOAVAILABILITY | PHARMACOKINETIC |
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FED CONDITION PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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IN PATIENTS WITH HEART FAILURE NUCLEIC ACID FEATURE |
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Tmax | PHARMACOKINETIC |
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HIGH-FAT, HIGH-CALORIE MEAL PHARMACOKINETIC |
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