ETORICOXIB

Possibly Marketed Outside US

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

Structure Search

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

HIDE SMILES / InChI

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

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Referrals_document/Arcoxia_6_12/WC500012804.pdf

Etoricoxib is a selective COX-2 inhibitor, which is approved in Europe for the treatment of inflammatory disorders such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute pain conditions, gout and postoperative dental surgery pain.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Prostaglandin G/H synthase 2 51 Target ID: P35354 Gene ID: 5743.0 Gene Symbol: PTGS2 Target Organism: Homo sapiens (Human) Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Referrals_document/Arcoxia_6_12/WC500012804.pdf	Inhibitor 8504		5.0 µM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Osteoarthritis 157 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Referrals_document/Arcoxia_6_12/WC500012804.pdf	Palliative	Approved 8583	ARCOXIA Approved Use ARCOXIA 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 Date 2004
Rheumatoid arthritis 320 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Referrals_document/Arcoxia_6_12/WC500012804.pdf	Palliative	Approved 8583	ARCOXIA Approved Use ARCOXIA 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 Date 2004
Acute gouty arthritis 2 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Referrals_document/Arcoxia_6_12/WC500012804.pdf	Palliative	Approved 8583	ARCOXIA Approved Use ARCOXIA 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 Date 2004
Pain 619 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Referrals_document/Arcoxia_6_12/WC500012804.pdf	Primary	Approved 8583	ARCOXIA Approved Use ARCOXIA 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 Date 2004
Ankylosing spondylitis 33 Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Referrals_document/Arcoxia_6_12/WC500012804.pdf	Palliative	Approved 8583	ARCOXIA Approved Use ARCOXIA 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 Date 2008
Postoperative dental surgery pain 2 Sources: https://www.medicines.org.uk/emc/PIL.29146.latest.pdf	Primary	Approved 8583	ARCOXIA Approved Use ARCOXIA 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 Date 2004

C_max

Value	Dose	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	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

T_1/2

Value	Dose	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

F_unbound

Value	Dose	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: https://pubmed.ncbi.nlm.nih.gov/12638395/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/12638395/	Sources: https://pubmed.ncbi.nlm.nih.gov/12638395/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/	Disc. AE: Dyspepsia, Upper abdominal pain... AEs leading to discontinuation/dose reduction: Dyspepsia (1.4%) 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 Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/

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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/
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: https://pubmed.ncbi.nlm.nih.gov/17304660/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/17304660/

PubMed

Title	Date	PubMed
Preparation and novel reduction reactions of vinamidinium salts.	2001 Jan 12	11429907
Dose proportionality of oral etoricoxib, a highly selective cyclooxygenase-2 inhibitor, in healthy volunteers.	2001 Oct	11583479
The biochemical selectivity of novel COX-2 inhibitors in whole blood assays of COX-isozyme activity.	2002	12564662
Efficacy and tolerability profile of etoricoxib in patients with osteoarthritis: A randomized, double-blind, placebo and active-comparator controlled 12-week efficacy trial.	2002	12017209
Cox-2 inhibitors: today and tomorrow.	2002 Apr	12003372
Simultaneous determination of unlabeled and carbon-13-labeled etoricoxib, a new cyclooxygenase-2 inhibitor, in human plasma using HPLC-MS/MS.	2002 Feb	11835200
Randomised double blind trial of etoricoxib and indometacin in treatment of acute gouty arthritis.	2002 Jun 22	12077033
Analgesic efficacy of etoricoxib in primary dysmenorrhea: results of a randomized, controlled trial.	2003	12900528
[Coxibs: highly selective cyclooxygenase-2 inhibitors. Part II. Side effects].	2003 Apr	12868201
A literature review of the epidemiology and treatment of acute gout.	2003 Jun	12860487
Gateways to clinical trials.	2003 Jun	12851663
Single- and multiple-dose pharmacokinetics of etoricoxib, a selective inhibitor of cyclooxygenase-2, in man.	2003 Mar	12638395
Clinical pharmacology of selective COX-2 inhibitors.	2003 May-Aug	14552704
Economic evaluation of etoricoxib versus non-selective NSAIDs in the treatment of osteoarthritis and rheumatoid arthritis patients in the UK.	2004	15244490
Selective cyclooxygenase-2 inhibitors: similarities and differences.	2004	15124935
The second generation of COX-2 inhibitors: clinical pharmacological point of view.	2004 Aug	15279595
Novel insights and therapeutical applications in the field of inhibitors of COX-2.	2004 Dec	15579005
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	14872504
Gastrointestinal side-effects of traditional non-steroidal anti-inflammatory drugs and new formulations.	2004 Jul	15335413
Gateways to clinical trials.	2004 Jul-Aug	15349141
Etoricoxib.	2004 May	15319795
[Etoricoxib (Arcoxia)].	2004 May	15270001
Gateways to clinical trials.	2004 Oct	15605126
Gateways to clinical trials.	2004 Sep	15538546
Gateways to clinical trials.	2005 Apr	15834452
The analgesic effect of etoricoxib relative to that of cetaminophen analgesics: a randomized, controlled single-dose study in acute dental impaction pain.	2005 Jan	15881486
Regulation of thrombomodulin expression in human vascular smooth muscle cells by COX-2-derived prostaglandins.	2005 Jan 7	15591227
Gateways to clinical trials.	2005 Jan-Feb	15834459
Protective effects of etoricoxib, a selective inhibitor of cyclooxygenase-2, in experimental periodontitis in rats.	2005 Jun	15853965
Valdecoxib: assessment of cyclooxygenase-2 potency and selectivity.	2005 Mar	15494548
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	15906586
Simultaneous quantitation of etoricoxib, salicylic acid, valdecoxib, ketoprofen, nimesulide and celecoxib in plasma by high-performance liquid chromatography with UV detection.	2006 Jan	16013036

Patents

Sample Use Guides

In Vivo Use Guide

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

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:09:13 GMT 2025` Edited by `admin` on `Mon Mar 31 18:09:13 GMT 2025`
Record UNII	WRX4NFY03R
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ARCOXIA

Preferred Name

English

ETORICOXIB

Official Name

English

MK-0663

Code

English

ETORICOXIB [MI]

Common Name

English

5-CHLORO-6'-METHYL-3-(4-(METHYLSULFONYL)PHENYL)-2,3'-BIPYRIDINE

Systematic Name

English

ETORICOXIB [USAN]

Common Name

English

L-791456

Code

English

Etoricoxib [WHO-DD]

Common Name

English

ETORICOXIB [MART.]

Common Name

English

2,3'-BIPYRIDINE, 5-CHLORO-6'-METHYL-3-(4-(METHYLSULFONYL)PHENYL)-

Systematic Name

English

etoricoxib [INN]

Common Name

English

Classification Tree Code System Code

WHO-ATC

M01AH05