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Details

Stereochemistry ACHIRAL
Molecular Formula C26H32N4O4S
Molecular Weight 496.6238
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SELEXIPAG

SMILES

CC(C)N(CCCCOCC(=NS(=O)(=O)C)O)c1cnc(-c2ccccc2)c(-c3ccccc3)n1

InChI

InChIKey=QXWZQTURMXZVHJ-UHFFFAOYSA-N
InChI=1S/C26H32N4O4S/c1-20(2)30(16-10-11-17-34-19-24(31)29-35(3,32)33)23-18-27-25(21-12-6-4-7-13-21)26(28-23)22-14-8-5-9-15-22/h4-9,12-15,18,20H,10-11,16-17,19H2,1-3H3,(H,29,31)

HIDE SMILES / InChI

Molecular Formula C26H32N4O4S
Molecular Weight 496.6238
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: Description was created based on several sources, including https://www.drugbank.ca/drugs/DB11362

Selexipag was approved by the United States FDA on December 22, 2015 for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce risk of hospitalization. PAH is a relatively rare disease with usually a poor prognosis requiring more treatment options to prolong long-term outcomes. Marketed by Actelion Pharmaceuticals under brand name Uptravi, selexipag and its active metabolite, ACT-333679 (MRE-269), act as agonists of the prostacyclin receptor to increase vasodilation in the pulmonary circulation and decrease elevated pressure in the blood vessels supplying blood to the lungs. Selexipag is a selective prostacyclin (IP, also called PGI2) receptor agonist. The key features of pulmonary arterial hypertension include a decrease in prostacyclin and prostacyclin synthase (enzyme that helps produce prostacyclin) in the lung. Prostacyclin is a potent vasodilator with anti-proliferative, anti-inflammatory, and anti-thrombotic effects; therefore, there is strong rationale for treatment with IP receptor agonists. Selexipag is chemically distinct as it is not PGI2 or a PGI2 analogue and has high selectivity for the IP receptor. It is metabolized by carboxylesterase 1 to yield an active metabolite (ACT-333679) that is approximately 37 times more potent than selexipag. Both selexipag and its metabolite are selective for the IP receptor over other prostanoid receptors. Selexipag is marketed under the brand name UPTRAVI, indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH.

CNS Activity

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
UPTRAVI

Approved Use

UPTRAVI is a prostacyclin receptor agonist indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH.

Launch Date

1.45065601E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
5.29 ng/mL
600 μg 1 times / day steady-state, oral
dose: 600 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.85 ng/mL
200 μg 1 times / day steady-state, oral
dose: 200 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4.12 ng/mL
400 μg 1 times / day steady-state, oral
dose: 400 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
5.98 ng/mL
400 μg single, oral
dose: 400 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
11.19 ng/mL
600 μg single, oral
dose: 600 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
11.53 ng/mL
800 μg single, oral
dose: 800 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2.2 ng/mL
100 μg single, oral
dose: 100 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3.4 ng/mL
200 μg single, oral
dose: 200 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
13.78 ng × h/mL
600 μg 1 times / day steady-state, oral
dose: 600 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
5.38 ng × h/mL
200 μg 1 times / day steady-state, oral
dose: 200 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
9.7 ng × h/mL
400 μg 1 times / day steady-state, oral
dose: 400 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
12.35 ng × h/mL
400 μg single, oral
dose: 400 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
23.27 ng × h/mL
600 μg single, oral
dose: 600 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
24.97 ng × h/mL
800 μg single, oral
dose: 800 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4.61 ng × h/mL
100 μg single, oral
dose: 100 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6.77 ng × h/mL
200 μg single, oral
dose: 200 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1.24 h
600 μg 1 times / day steady-state, oral
dose: 600 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.14 h
200 μg 1 times / day steady-state, oral
dose: 200 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.41 h
400 μg 1 times / day steady-state, oral
dose: 400 μg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1 h
400 μg single, oral
dose: 400 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1.9 h
600 μg single, oral
dose: 600 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
2.3 h
800 μg single, oral
dose: 800 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.7 h
100 μg single, oral
dose: 100 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
0.8 h
200 μg single, oral
dose: 200 μg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELEXIPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
, oral
SELEXIPAG plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Disc. AE: Headache, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Headache
Diarrhea
Nausea
Myalgia
Abdominal pain
Pain in extremity
Dizziness
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 19 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 19 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Headache...
Other AEs:
Headache (65%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 20 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 20 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Diarrhoea...
Other AEs:
Diarrhoea (42%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 21 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 21 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Pain in jaw...
Other AEs:
Pain in jaw (26%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 22 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 22 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Nausea...
Other AEs:
Nausea (33%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 23 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 23 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Myalgia...
Other AEs:
Myalgia (16%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 24 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 24 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Vomiting...
Other AEs:
Vomiting (18%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 25 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 25 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Pain in extremity...
Other AEs:
Pain in extremity (17%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 26 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 26 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Flushing...
Other AEs:
Flushing (12%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 27 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 27 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Arthralgia...
Other AEs:
Arthralgia (11%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 28 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 28 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Anaemia...
Other AEs:
Anaemia (8%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 29 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 29 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Abdominal pain...
Other AEs:
Abdominal pain (8%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 30 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 30 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Decreased appetite...
Other AEs:
Decreased appetite (6%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 31 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 31 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Pain...
Other AEs:
Pain (3%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 32 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 32 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Other AEs: Nasopharyngitis...
Other AEs:
Nasopharyngitis (13%)
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
1800 ug 2 times / day multiple, oral
Highest studied dose
Dose: 1800 ug, 2 times / day
Route: oral
Route: multiple
Dose: 1800 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 8
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 8
Sources:
Disc. AE: Nausea, Nightmares...
AEs leading to
discontinuation/dose reduction:
Nausea (12.5%)
Nightmares (12.5%)
Sources:
1600 ug 2 times / day multiple, oral
MTD
Dose: 1600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 1600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 9
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 9
Sources:
1000 ug 2 times / day multiple, oral
Studied dose
Dose: 1000 ug, 2 times / day
Route: oral
Route: multiple
Dose: 1000 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 9
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 9
Sources:
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (11.1%)
Sources:
400 ug 2 times / day multiple, oral
Studied dose
Dose: 400 ug, 2 times / day
Route: oral
Route: multiple
Dose: 400 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 12
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 12
Sources:
Disc. AE: Myalgia...
AEs leading to
discontinuation/dose reduction:
Myalgia (8.3%)
Sources:
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Disc. AE: Feeling hot, Myalgia...
AEs leading to
discontinuation/dose reduction:
Feeling hot (9.1%)
Myalgia (9.1%)
Disturbance in attention (9.1%)
Dysaesthesia (9.1%)
Palpitations (9.1%)
Tinnitus (9.1%)
Dizziness (9.1%)
Dry mouth (9.1%)
Sources:
3200 ug 1 times / day single, oral
Studied dose
unhealthy
n = 1
Other AEs: Nausea...
AEs

AEs

AESignificanceDosePopulation
Abdominal pain Disc. AE
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Diarrhea Disc. AE
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Dizziness Disc. AE
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Headache Disc. AE
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Myalgia Disc. AE
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Nausea Disc. AE
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Pain in extremity Disc. AE
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
unhealthy, 18 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 18 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.98
Headache 65%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 19 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 19 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Diarrhoea 42%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 20 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 20 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Pain in jaw 26%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 21 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 21 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Nausea 33%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 22 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 22 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Myalgia 16%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 23 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 23 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Vomiting 18%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 24 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 24 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Pain in extremity 17%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 25 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 25 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Flushing 12%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 26 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 26 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Arthralgia 11%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 27 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 27 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Anaemia 8%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 28 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 28 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Abdominal pain 8%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 29 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 29 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Decreased appetite 6%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 30 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 30 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Pain 3%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 31 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 31 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Nasopharyngitis 13%
900 ug 2 times / day multiple, oral (mean)
Studied dose
Dose: 900 ug, 2 times / day
Route: oral
Route: multiple
Dose: 900 ug, 2 times / day
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
unhealthy, 32 to 75 years
n = 575
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 32 to 75 years
Sex: M+F
Population Size: 575
Sources: Page: nda/2015/207947Orig1s000MedR.pdf - p.102
Nausea 12.5%
Disc. AE
1800 ug 2 times / day multiple, oral
Highest studied dose
Dose: 1800 ug, 2 times / day
Route: oral
Route: multiple
Dose: 1800 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 8
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 8
Sources:
Nightmares 12.5%
Disc. AE
1800 ug 2 times / day multiple, oral
Highest studied dose
Dose: 1800 ug, 2 times / day
Route: oral
Route: multiple
Dose: 1800 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 8
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 8
Sources:
Headache 11.1%
Disc. AE
1000 ug 2 times / day multiple, oral
Studied dose
Dose: 1000 ug, 2 times / day
Route: oral
Route: multiple
Dose: 1000 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 9
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 9
Sources:
Myalgia 8.3%
Disc. AE
400 ug 2 times / day multiple, oral
Studied dose
Dose: 400 ug, 2 times / day
Route: oral
Route: multiple
Dose: 400 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 12
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 12
Sources:
Disturbance in attention 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Dizziness 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Dry mouth 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Dysaesthesia 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Feeling hot 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Myalgia 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Palpitations 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Tinnitus 9.1%
Disc. AE
600 ug 2 times / day multiple, oral
Studied dose
Dose: 600 ug, 2 times / day
Route: oral
Route: multiple
Dose: 600 ug, 2 times / day
Sources:
healthy, mean age of 36.4 years
n = 11
Health Status: healthy
Age Group: mean age of 36.4 years
Sex: M
Population Size: 11
Sources:
Nausea
3200 ug 1 times / day single, oral
Studied dose
unhealthy
n = 1
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 100 uM]
no [IC50 11 uM]
no [IC50 20 uM]
no [IC50 37 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >=50 uM]
no [IC50 >=50 uM]
no [IC50 >=50 uM]
no [IC50 >=50 uM]
no [IC50 >=50 uM]
no [IC50 >=50 uM]
no [IC50 >=50 uM]
no
no
no
no
weak
yes [IC50 1.4 uM]
yes [IC50 1.7 uM]
yes [IC50 1.7 uM]
yes [IC50 1.9 uM]
yes [IC50 15 uM]
yes [IC50 2.1 uM]
yes [IC50 2.4 uM]
yes [IC50 25 uM]
yes [IC50 3.5 uM]
yes [IC50 3.6 uM]
yes [IC50 32 uM]
yes [IC50 4.1 uM]
yes [IC50 5.6 uM]
yes [IC50 8.3 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
yes
yes
yes
yes
yes
yes
yes
yes
no (co-administration study)
Comment: Co-administration of Kaletra® [CYP3A, P-gp and OATP1B1/1B3 inhibitor] with selexipag resulted in approx. 2-fold increase in the exposure to selexipag, but not ACT-333679.
Page: 6.0
yes
no (co-administration study)
Comment: Co-administration of Kaletra® [CYP3A, P-gp and OATP1B1/1B3 inhibitor] with selexipag resulted in approx. 2-fold increase in the exposure to selexipag, but not ACT-333679.
Page: 6.0
yes
no (co-administration study)
Comment: Co-administration of Kaletra® [CYP3A, P-gp and OATP1B1/1B3 inhibitor] with selexipag resulted in approx. 2-fold increase in the exposure to selexipag, but not ACT-333679.
Page: 6.0
yes
no (co-administration study)
Comment: Co-administration of Kaletra® [CYP3A, P-gp and OATP1B1/1B3 inhibitor] with selexipag resulted in approx. 2-fold increase in the exposure to selexipag, but not ACT-333679.
Page: 6.0
yes
no (co-administration study)
Comment: Co-administration of Kaletra® [CYP3A, P-gp and OATP1B1/1B3 inhibitor] with selexipag resulted in approx. 2-fold increase in the exposure to selexipag, but not ACT-333679.
Page: 6.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation.
1976 Oct 21
Prostanoid receptors and their biological actions.
1993
Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist.
2007 Dec 15
Structure-activity studies on diphenylpyrazine derivatives: a novel class of prostacyclin receptor agonists.
2007 Nov 1
Selexipag: a selective prostacyclin receptor agonist that does not affect rat gastric function.
2010 Oct
Pathways in pulmonary arterial hypertension: the future is here.
2012 Dec 1
Pharmacokinetics and Tolerability of the Novel Oral Prostacyclin IP Receptor Agonist Selexipag.
2015 Jun
Selexipag for the treatment of pulmonary arterial hypertension.
2016
Patents

Sample Use Guides

Starting dose: 200 mcg twice daily. Increase the dose by 200 mcg twice daily at weekly intervals to the highest tolerated dose up to 1600 mcg twice daily. Maintenance dose is determined by tolerability. Moderate hepatic impairment: Starting dose 200 mcg once daily, increase the dose by 200 mcg once daily at weekly intervals to the highest tolerated dose up to 1600 mcg.
Route of Administration: Oral
Both selexipag and its active metabolite caused concentration-dependent inhibition of platelet aggregation in vitro with an IC50 of 5.5 uM and 0.21 uM, respectively.
Substance Class Chemical
Created
by admin
on Sat Jun 26 04:32:30 UTC 2021
Edited
by admin
on Sat Jun 26 04:32:30 UTC 2021
Record UNII
5EXC0E384L
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SELEXIPAG
DASH   INN   USAN   WHO-DD  
INN   USAN  
Official Name English
SELEXIPAG [USAN]
Common Name English
SELEXIPAG [WHO-DD]
Common Name English
SELEXIPAG [INN]
Common Name English
2-(4-((5,6-DIPHENYLPYRAZIN-2-YL)(PROPAN-2-YL)AMINO)BUTOXY)-N-(METHANESULFONYL)ACETAMIDE
Systematic Name English
SELEXIPAG [JAN]
Common Name English
SELEXIPAG [ORANGE BOOK]
Common Name English
UPTRAVI
Brand Name English
ACT-293987
Code English
SELEXIPAG [MI]
Common Name English
NS-304
Code English
Classification Tree Code System Code
NDF-RT N0000192339
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
FDA ORPHAN DRUG 652018
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
WHO-ATC B01AC27
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
NCI_THESAURUS C78568
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
EMA ASSESSMENT REPORTS UPTRAVI (AUTHORIZED: HYPERTENSION, PULMONARY)
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
FDA ORPHAN DRUG 304810
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
Code System Code Type Description
RXCUI
1729002
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
ChEMBL
CHEMBL238804
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
PUBCHEM
9913767
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
FDA UNII
5EXC0E384L
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
MERCK INDEX
M11914
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
NCI_THESAURUS
C152321
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
DRUG BANK
DB11362
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
DRUG CENTRAL
5077
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
CAS
475086-01-2
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
INN
9231
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
EVMPD
SUB130805
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY
EU-Orphan Drug
EU/3/05/316(WITHDRAWN)
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY Please note that this product was withdrawn from the Community Register of designated Orphan Medicinal Products in February 2016 on request of the Sponsor, at the time of the granting of a marketing authorisation. On 26 August 2005, orphan designation (EU/3/05/316) was granted by the European Commission to Nippon Shinyaku Co. Ltd, Germany, for 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide for the treatment of pulmonary arterial hypertension and chronic thromoembolic pulmonary hypertension. The sponsorship was transferred to Actelion Registration Limited, United Kingdom, in February 2009. Update: 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide has been authorised in the EU as Uptravi since 12 May 2016. More information on Uptravi can be found in the European public assessment report (EPAR) on the Agency’s website.
NDF-RT
N0000020068
Created by admin on Sat Jun 26 04:32:31 UTC 2021 , Edited by admin on Sat Jun 26 04:32:31 UTC 2021
PRIMARY Prostacyclin Receptor Agonists [MoA]
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> SUBSTRATE
TRANSPORTER -> INHIBITOR
IC50
BINDER->LIGAND
BINDING
TRANSPORTER -> INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
IC50
EXCRETED UNCHANGED
No unchanged selexipag is excreted in the urine and feces.
FECAL; URINE
TRANSPORTER -> INHIBITOR
IC50
METABOLIC ENZYME -> SUBSTRATE
MAJOR
METABOLIC ENZYME -> INHIBITOR
IC50
TARGET -> AGONIST
EC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION