Details
Stereochemistry | ACHIRAL |
Molecular Formula | C18H15ClN2O2S |
Molecular Weight | 358.842 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=C(C=N1)C2=NC=C(Cl)C=C2C3=CC=C(C=C3)S(C)(=O)=O
InChI
InChIKey=MNJVRJDLRVPLFE-UHFFFAOYSA-N
InChI=1S/C18H15ClN2O2S/c1-12-3-4-14(10-20-12)18-17(9-15(19)11-21-18)13-5-7-16(8-6-13)24(2,22)23/h3-11H,1-2H3
Molecular Formula | C18H15ClN2O2S |
Molecular Weight | 358.842 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11160644
Curator's Comment: # Merck Research Laboratories
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P35354 Gene ID: 5743.0 Gene Symbol: PTGS2 Target Organism: Homo sapiens (Human) |
5.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | ARCOXIA Approved UseARCOXIA is indicated in the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and the pain and signs of inflammation associated with acute gouty arthritis. Launch Date2004 |
|||
Palliative | ARCOXIA Approved UseARCOXIA is indicated in the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and the pain and signs of inflammation associated with acute gouty arthritis. Launch Date2004 |
|||
Palliative | ARCOXIA Approved UseARCOXIA is indicated in the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and the pain and signs of inflammation associated with acute gouty arthritis. Launch Date2004 |
|||
Primary | ARCOXIA Approved UseARCOXIA is indicated in the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and the pain and signs of inflammation associated with acute gouty arthritis. Launch Date2004 |
|||
Palliative | ARCOXIA Approved UseARCOXIA is indicated in the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and the pain and signs of inflammation associated with acute gouty arthritis. Launch Date2008 |
|||
Primary | ARCOXIA Approved UseARCOXIA is indicated in the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and the pain and signs of inflammation associated with acute gouty arthritis. Launch Date2004 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
95 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
201 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
411 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
788 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2186 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2.43 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1.56 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT |
|
0.53 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1.27 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2.14 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
4.37 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2.05 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.59 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg 1 times / day steady-state, oral dose: 120 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1752 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1698 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1917 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2209 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1694 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1654 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1680 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / 2 days steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.55 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.47 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
6.7 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
13.29 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
40.56 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
41.35 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
40.16 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT |
|
9.08 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
18.57 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
35.84 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
76.1 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
18.43 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
37.83 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg 1 times / day steady-state, oral dose: 120 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.87 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
31.36 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
34.71 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
33.49 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
17.77 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
20.66 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
15.92 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / 2 days steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
22.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
21.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
21.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11583479/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
28.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
27.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT |
|
28.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
29.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
28.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
27.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
23.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
25.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12638395/ |
120 mg 1 times / day steady-state, oral dose: 120 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
19.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
24.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
21.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
20.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
21.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
24.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
30.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / 2 days steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
12.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
12.6% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
12.6% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8.1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14681341/ |
120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8.1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
10.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
10.1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/14517196/ |
60 mg 1 times / 2 days steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
ETORICOXIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
120 mg 1 times / day steady-state, oral Recommended Dose: 120 mg, 1 times / day Route: oral Route: steady-state Dose: 120 mg, 1 times / day Sources: |
healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Dyspepsia, Upper abdominal pain... AEs leading to discontinuation/dose reduction: Dyspepsia (1.4%) Sources: Upper abdominal pain (0.9%) Abdominal pain (0.7%) Hypertension (1.5%) Diarrhea (0.6%) Cerebral hemorrhage (grade 5, 0.03%) ALT increased AST increased |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Diarrhea | 0.6% Disc. AE |
90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Abdominal pain | 0.7% Disc. AE |
90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Upper abdominal pain | 0.9% Disc. AE |
90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Dyspepsia | 1.4% Disc. AE |
90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Hypertension | 1.5% Disc. AE |
90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
ALT increased | Disc. AE | 90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
AST increased | Disc. AE | 90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Cerebral hemorrhage | grade 5, 0.03% Disc. AE |
90 mg 1 times / day multiple, oral Recommended Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Preparation and novel reduction reactions of vinamidinium salts. | 2001 Jan 12 |
|
Dose proportionality of oral etoricoxib, a highly selective cyclooxygenase-2 inhibitor, in healthy volunteers. | 2001 Oct |
|
The biochemical selectivity of novel COX-2 inhibitors in whole blood assays of COX-isozyme activity. | 2002 |
|
Efficacy and tolerability profile of etoricoxib in patients with osteoarthritis: A randomized, double-blind, placebo and active-comparator controlled 12-week efficacy trial. | 2002 |
|
Cox-2 inhibitors: today and tomorrow. | 2002 Apr |
|
Simultaneous determination of unlabeled and carbon-13-labeled etoricoxib, a new cyclooxygenase-2 inhibitor, in human plasma using HPLC-MS/MS. | 2002 Feb |
|
Randomised double blind trial of etoricoxib and indometacin in treatment of acute gouty arthritis. | 2002 Jun 22 |
|
Analgesic efficacy of etoricoxib in primary dysmenorrhea: results of a randomized, controlled trial. | 2003 |
|
[Coxibs: highly selective cyclooxygenase-2 inhibitors. Part II. Side effects]. | 2003 Apr |
|
A literature review of the epidemiology and treatment of acute gout. | 2003 Jun |
|
Gateways to clinical trials. | 2003 Jun |
|
Single- and multiple-dose pharmacokinetics of etoricoxib, a selective inhibitor of cyclooxygenase-2, in man. | 2003 Mar |
|
Clinical pharmacology of selective COX-2 inhibitors. | 2003 May-Aug |
|
Economic evaluation of etoricoxib versus non-selective NSAIDs in the treatment of osteoarthritis and rheumatoid arthritis patients in the UK. | 2004 |
|
Selective cyclooxygenase-2 inhibitors: similarities and differences. | 2004 |
|
The second generation of COX-2 inhibitors: clinical pharmacological point of view. | 2004 Aug |
|
Novel insights and therapeutical applications in the field of inhibitors of COX-2. | 2004 Dec |
|
Efficacy and safety profile of treatment with etoricoxib 120 mg once daily compared with indomethacin 50 mg three times daily in acute gout: a randomized controlled trial. | 2004 Feb |
|
Gastrointestinal side-effects of traditional non-steroidal anti-inflammatory drugs and new formulations. | 2004 Jul |
|
Gateways to clinical trials. | 2004 Jul-Aug |
|
Etoricoxib. | 2004 May |
|
[Etoricoxib (Arcoxia)]. | 2004 May |
|
Gateways to clinical trials. | 2004 Oct |
|
Gateways to clinical trials. | 2004 Sep |
|
Gateways to clinical trials. | 2005 Apr |
|
The analgesic effect of etoricoxib relative to that of cetaminophen analgesics: a randomized, controlled single-dose study in acute dental impaction pain. | 2005 Jan |
|
Regulation of thrombomodulin expression in human vascular smooth muscle cells by COX-2-derived prostaglandins. | 2005 Jan 7 |
|
Gateways to clinical trials. | 2005 Jan-Feb |
|
Protective effects of etoricoxib, a selective inhibitor of cyclooxygenase-2, in experimental periodontitis in rats. | 2005 Jun |
|
Valdecoxib: assessment of cyclooxygenase-2 potency and selectivity. | 2005 Mar |
|
Association between health-related quality of life and clinical efficacy endpoints in rheumatoid arthritis patients after four weeks treatment with anti-inflammatory agents. | 2005 May |
|
Simultaneous quantitation of etoricoxib, salicylic acid, valdecoxib, ketoprofen, nimesulide and celecoxib in plasma by high-performance liquid chromatography with UV detection. | 2006 Jan |
Patents
Sample Use Guides
The recommended dose is 30 mg once a day (osteoarthritis) and 60 mg once a day (rheumatoid arthritis, ankylosing spondylitis); the dose may be increased to a maximum of 60 mg (osteoarthritis) or 90 mg (rheumatoid arthritis, ankylosing spondylitis) once a day if needed. In case of acute pain conditions etoricoxib should be used only for the acute painful period. In gout the recommended dose is 120 mg once a day which should only be used for the acute painful period, limited to a maximum of 8 days. For the treatment of postoperative dental surgery pain the recommended dose is 90 mg once daily, limited to a maximum of 3 days treatment.
Route of Administration:
Oral
Substance Class |
Chemical
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C1323
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
SELECTIVE
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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EXCRETED UNCHANGED |
URINE
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METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
FOLLOWING INTRAVENOUS ADMINISTRATION
URINE
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METABOLITE -> PARENT |
FOLLOWING INTRAVENOUS ADMINISTRATION
URINE
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METABOLITE -> PARENT |
FOLLOWING INTRAVENOUS ADMINISTRATION
MAJOR
URINE
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METABOLITE -> PARENT |
FOLLOWING INTRAVENOUS ADMINISTRATION
URINE
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METABOLITE -> PARENT |
FOLLOWING INTRAVENOUS ADMINISTRATION
URINE
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Related Record | Type | Details | ||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT | |||
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IMPURITY -> PARENT |
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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Tmax | PHARMACOKINETIC |
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ORAL SOLUTION DOSE |
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ORAL BIOAVAILABILITY | PHARMACOKINETIC |
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