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Details

Stereochemistry ABSOLUTE
Molecular Formula C32H35N5O5
Molecular Weight 569.652
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ELUXADOLINE

SMILES

Cc1cc(cc(C)c1C[C@@]([H])(C(=O)N(Cc2ccc(c(c2)C(=O)O)OC)[C@@]([H])(C)c3ncc(-c4ccccc4)[nH]3)N)C(=O)N

InChI

InChIKey=QFNHIDANIVGXPE-FNZWTVRRSA-N
InChI=1S/C32H35N5O5/c1-18-12-23(29(34)38)13-19(2)24(18)15-26(33)31(39)37(17-21-10-11-28(42-4)25(14-21)32(40)41)20(3)30-35-16-27(36-30)22-8-6-5-7-9-22/h5-14,16,20,26H,15,17,33H2,1-4H3,(H2,34,38)(H,35,36)(H,40,41)/t20-,26-/m0/s1

HIDE SMILES / InChI

Molecular Formula C32H35N5O5
Molecular Weight 569.652
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800031329 | https://www.ncbi.nlm.nih.gov/pubmed/22695132 | https://www.ncbi.nlm.nih.gov/pubmed/25261794

Eluxadoline, an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist. Eluxadoline normalizes gastrointestinal (GI) transit and defecation under conditions of novel environment stress or post-inflammatory altered GI function. Allergan (previously Actavis) is developing eluxadoline for the treatment of diarrhoea-predominant irritable bowel syndrome. The agent was originated by Janssen Pharmaceutica. Eluxadoline has been launched in the US under trade name VIBERZI (eluxadoline) tablets, while is at the preregistration stage in the EU.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VIBERZI

Approved Use

VIBERZI is a mu-opioid receptor agonist, indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D)

Launch Date

1.43259835E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
29.9 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.1 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
58.8 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
27.6 ng/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
104.8 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
22.1 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
237.2 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
268.1 ng × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
21.8 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4.4 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
5.9 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
14.4 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELUXADOLINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
19%
unknown, oral
ELUXADOLINE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
2000 mg 1 times / day single, oral
Highest studied dose
healthy, adult
Other AEs: Nausea, Abdominal pain...
1000 mg 1 times / day single, oral
MTD
healthy, adult
n = 8
1500 mg 1 times / day single, oral
MTD
healthy, adult
n = 5
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Other AEs: Rash...
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Disc. AE: Abdominal pain, Constipation...
Other AEs: Dizziness, Fatigue...
AEs leading to
discontinuation/dose reduction:
Abdominal pain (1.4%)
Constipation (1.5%)
Headache (0.1%)
Dizziness (0.1%)
Vomiting (0.2%)
Somnolence (0.1%)
Other AEs:
Dizziness (2.6%)
Fatigue (1.9%)
Anxiety (1.9%)
Depression (1.2%)
Somnolence (1.1%)
Nausea (7.1%)
Constipation (8.1%)
Abdominal pain (4.6%)
Vomiting (4.2%)
Flatulence (3.2%)
Abdominal distension (2.7%)
Upper respiratory tract infection (5.1%)
Nasopharyngitis (3%)
Sinusitis (2.6%)
Bronchitis (2.9%)
Gastroenteritis viral (1.4%)
Urinary tract infection (1.7%)
Headache (4.3%)
Dizziness (3.2%)
Fatigue (1.9%)
ALT increased (2.5%)
Hypertension (1.4%)
Bilirubin elevated (1.3%)
Alkaline phosphatase (0.8%)
Sources:
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Other AEs: Rash...
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Disc. AE: Abdominal pain, Constipation...
Other AEs: Dizziness, Fatigue...
AEs leading to
discontinuation/dose reduction:
Abdominal pain (1.5%)
Constipation (1.1%)
Nausea (0.6%)
Headache (0.4%)
Dizziness (0.1%)
Vomiting (0.1%)
Pruritis (0.1%)
Other AEs:
Dizziness (2.6%)
Fatigue (2.6%)
Anxiety (1.2%)
Depression (1.1%)
Somnolence (0.1%)
Nausea (8.1%)
Constipation (7.4%)
Abdominal pain (4.1%)
Vomiting (4%)
Flatulence (2.6%)
Abdominal distension (2.6%)
Upper respiratory tract infection (3.3%)
Nasopharyngitis (4.1%)
Sinusitis (3.3%)
Bronchitis (3.2%)
Gastroenteritis viral (2.7%)
Urinary tract infection (2.1%)
Headache (4%)
Dizziness (2.6%)
Fatigue (2.6%)
ALT increased (2.1%)
Hypertension (2.5%)
Bilirubin elevated (1.9%)
Alkaline phosphatase (0.9%)
Sources:
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Disc. AE: Abdominal pain, Constipation...
AEs leading to
discontinuation/dose reduction:
Abdominal pain (7%)
Constipation (2.3%)
Nausea (2.3%)
Headache (1.8%)
Dizziness (1.8%)
Vomiting (1.2%)
Fatigue (1.2%)
Dry mouth (1.8%)
Somnolence (1.2%)
Pruritis (1.2%)
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
AEs

AEs

AESignificanceDosePopulation
Abdominal pain
2000 mg 1 times / day single, oral
Highest studied dose
healthy, adult
Constipation
2000 mg 1 times / day single, oral
Highest studied dose
healthy, adult
Nausea
2000 mg 1 times / day single, oral
Highest studied dose
healthy, adult
Rash 3%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Dizziness 0.1%
Disc. AE
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Headache 0.1%
Disc. AE
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Somnolence 0.1%
Disc. AE
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Vomiting 0.2%
Disc. AE
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Alkaline phosphatase 0.8%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Somnolence 1.1%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Depression 1.2%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Bilirubin elevated 1.3%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Gastroenteritis viral 1.4%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Hypertension 1.4%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Abdominal pain 1.4%
Disc. AE
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Constipation 1.5%
Disc. AE
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Urinary tract infection 1.7%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Anxiety 1.9%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Fatigue 1.9%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Fatigue 1.9%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
ALT increased 2.5%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Dizziness 2.6%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Sinusitis 2.6%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Abdominal distension 2.7%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Bronchitis 2.9%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Nasopharyngitis 3%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Dizziness 3.2%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Flatulence 3.2%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Vomiting 4.2%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Headache 4.3%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Abdominal pain 4.6%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Upper respiratory tract infection 5.1%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Nausea 7.1%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Constipation 8.1%
100 mg 2 times / day multiple, oral
Recommended
Dose: 100 mg, 2 times / day
Route: oral
Route: multiple
Dose: 100 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 1032
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 1032
Sources:
Rash 3%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Somnolence 0.1%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Dizziness 0.1%
Disc. AE
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Pruritis 0.1%
Disc. AE
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Vomiting 0.1%
Disc. AE
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Headache 0.4%
Disc. AE
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Nausea 0.6%
Disc. AE
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Alkaline phosphatase 0.9%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Depression 1.1%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Constipation 1.1%
Disc. AE
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Anxiety 1.2%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Abdominal pain 1.5%
Disc. AE
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Bilirubin elevated 1.9%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
ALT increased 2.1%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Urinary tract infection 2.1%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Hypertension 2.5%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Abdominal distension 2.6%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Dizziness 2.6%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Dizziness 2.6%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Fatigue 2.6%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Fatigue 2.6%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Flatulence 2.6%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Gastroenteritis viral 2.7%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Bronchitis 3.2%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Sinusitis 3.3%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Upper respiratory tract infection 3.3%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Headache 4%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Vomiting 4%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Abdominal pain 4.1%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Nasopharyngitis 4.1%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Constipation 7.4%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Nausea 8.1%
75 mg 2 times / day multiple, oral
Recommended
Dose: 75 mg, 2 times / day
Route: oral
Route: multiple
Dose: 75 mg, 2 times / day
Sources:
unhealthy, mean age 45.5 years
n = 807
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 45.5 years
Sex: M+F
Population Size: 807
Sources:
Fatigue 1.2%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Pruritis 1.2%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Somnolence 1.2%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Vomiting 1.2%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Dizziness 1.8%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Dry mouth 1.8%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Headache 1.8%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Constipation 2.3%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Nausea 2.3%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Abdominal pain 7%
Disc. AE
200 mg 2 times / day multiple, oral
Studied dose
Dose: 200 mg, 2 times / day
Route: oral
Route: multiple
Dose: 200 mg, 2 times / day
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
unhealthy, mean age 63.6 years
n = 171
Health Status: unhealthy
Condition: irritable bowel syndrome with diarrhea
Age Group: mean age 63.6 years
Sex: M+F
Population Size: 171
Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
weak
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
weak
weak
yes
yes
yes
yes (co-administration study)
Comment: Coadministration of single oral dose of 500 mg probenecid (an inhibitor of MRP2 and OAT3) with single oral dose of 100 mg eluxadoline increased both AUC and Cmax of eluxadoline by 30%, which is not considered to be clinically significant.
Page: 10.0
yes
yes (co-administration study)
Comment: Coadministration of single oral dose of 500 mg probenecid (an inhibitor of MRP2 and OAT3) with single oral dose of 100 mg eluxadoline increased both AUC and Cmax of eluxadoline by 30%, which is not considered to be clinically significant.
Page: 10.0
yes
yes (co-administration study)
Comment: Coadministration of single oral dose of 600 mg cyclosporine (an inhibitor of many transporters including OATP1B1 and MRP2) with single oral dose of 100 mg eluxadoline increased eluxadoline AUC by 4.4 fold and Cmax by 6.2 fold.
Page: 10.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist.
2012 Nov
Patents

Patents

Sample Use Guides

The recommended dosage in adults is 100 mg twice daily taken with food. • The recommended dosage is 75 mg twice daily taken with food in patients who: * do not have a gallbladder * are unable to tolerate the 100 mg dose * are receiving concomitant OATP1B1 inhibitors * have mild or moderate hepatic impairment • Discontinue VIBERZI in patients who develop severe constipation for more than 4 days • If a dose is missed, take the next dose at the regular time; do not take 2 doses at once
Route of Administration: Oral
In the guinea pig isolated ileum, MuDelta (eluxadoline) reduced electrical field stimulation-evoked contractions similar to DAMGO, with Kis of 1.0 and 1.3 nM, respectively. ) In guinea pig isolated proximal colon, MuDelta (eluxadoline) had weak k opioid receptor agonist activity compared with the k opioid receptor agonist ICI 204 448, with IC50 = 1.6 mM and 1.7 nM, respectively
Substance Class Chemical
Created
by admin
on Sat Jun 26 05:05:52 UTC 2021
Edited
by admin
on Sat Jun 26 05:05:52 UTC 2021
Record UNII
45TPJ4MBQ1
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ELUXADOLINE
DASH   INN   USAN   WHO-DD  
USAN   INN  
Official Name English
ELUXADOLINE [MI]
Common Name English
VIBERZI
Brand Name English
ELUXADOLINE [NFLIS-DRUG]
Common Name English
ELUXADOLINE [ORANGE BOOK]
Common Name English
JNJ-27018966
Code English
BENZOIC ACID, 5-((((2S)-2-AMINO-3-(4-(AMINOCARBONYL)-2,6-DIMETHYLPHENYL)-1-OXOPROPYL)((1S)-1-(5-PHENYL-1H-IMIDAZOL-2-YL)ETHYL)AMINO)METHYL)-2-METHOXY-
Common Name English
ELUXADOLINE [USAN]
Common Name English
5-((2-AMINO-3-(4-CARBAMOYL-2,6-DIMETHYLPHENYL)-N-(1-(5-PHENYL-1H-IMIDAZOL-2-YL)ETHYL)PROPANAMIDO)METHYL)-2-METHOXYBENZOIC ACID
Systematic Name English
5-((((2S)-2-AMINO-3-(4-CARBAMOYL-2,6-DIMETHYLPHENYL)PROPANOYL)((1S)-1-(4-PHENYL-1H-IMIDAZOL-2-YL)ETHYL)AMINO(METHYL)-2-METHOXYBENZOIC ACID
Systematic Name English
ELUXADOLINE [WHO-DD]
Common Name English
ELUXADOLINE [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC A07DA06
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
NDF-RT N0000191867
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
Code System Code Type Description
INN
9749
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
CAS
864821-90-9
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
WIKIPEDIA
Eluxadoline
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
PUBCHEM
11250029
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
LACTMED
Eluxadoline
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
IUPHAR
7691
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
DRUG BANK
DB09272
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
EVMPD
SUB175259
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
ChEMBL
CHEMBL2159122
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
NCI_THESAURUS
C166725
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
EPA CompTox
864821-90-9
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
FDA UNII
45TPJ4MBQ1
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
NDF-RT
N0000191866
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY Opioid mu-Receptor Agonists [MoA]
MERCK INDEX
M11882
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
RXCUI
1653781
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
5001
Created by admin on Sat Jun 26 05:05:52 UTC 2021 , Edited by admin on Sat Jun 26 05:05:52 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
WEAK
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
METABOLIC ENZYME -> INHIBITOR
In an in-vitro study, eluxadoline appears to show time-dependent inhibition of CYP3A4 at 50 ?M, a concentration that can be achieved in the gut (Igut is estimated to be 700 ?M).
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
BINDER->LIGAND
BINDING
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
EXCRETED UNCHANGED
On average, 0.12% of the administered dose was recovered from urine up to 192 hours post-dose and 82% was recovered from feces up to 336 hours post-dose. The percentage of radioactivity excreted as unchanged drug vs. metabolites in urine and feces was not assessed in this study.
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC SINGLE DOSE ADMINISTRATION