U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C32H35N5O5
Molecular Weight 569.6508
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ELUXADOLINE

SMILES

COC1=CC=C(CN([C@@H](C)C2=NC(=CN2)C3=CC=CC=C3)C(=O)[C@@H](N)CC4=C(C)C=C(C=C4C)C(N)=O)C=C1C(O)=O

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 569.6508
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.

CNS Activity

Originator

Approval Year

2015
471
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2678
 1.7 nM [Ki]
Antagonist
2778
 1.3 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
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

2015
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
29.9 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/28719721
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/206940s007lbl.pdf
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
Dose: 2000 mg, 1 times / day
Route: oral
Route: single
Dose: 2000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
Other AEs: Nausea, Abdominal pain...
Other AEs:
Nausea
Abdominal pain
Constipation
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
1000 mg 1 times / day single, oral
MTD
Dose: 1000 mg, 1 times / day
Route: oral
Route: single
Dose: 1000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
healthy, adult
n = 8
Health Status: healthy
Age Group: adult
Sex: F
Population Size: 8
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
1500 mg 1 times / day single, oral
MTD
Dose: 1500 mg, 1 times / day
Route: oral
Route: single
Dose: 1500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
healthy, adult
n = 5
Health Status: healthy
Age Group: adult
Sex: M
Population Size: 5
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
Other AEs: Rash...
Other AEs:
Rash (3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
Other AEs: Rash...
Other AEs:
Rash (3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
Page: nda/2015/206940Orig1s000MedR.pdf - p.3
AEs

AEs

AESignificanceDosePopulation
Abdominal pain
2000 mg 1 times / day single, oral
Highest studied dose
Dose: 2000 mg, 1 times / day
Route: oral
Route: single
Dose: 2000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
Constipation
2000 mg 1 times / day single, oral
Highest studied dose
Dose: 2000 mg, 1 times / day
Route: oral
Route: single
Dose: 2000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
Nausea
2000 mg 1 times / day single, oral
Highest studied dose
Dose: 2000 mg, 1 times / day
Route: oral
Route: single
Dose: 2000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf
https://www.ema.europa.eu/en/documents/assessment-report/truberzi-epar-public-assessment-report_en.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940Orig1s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000MedR.pdf
Page: nda/2015/206940Orig1s000MedR.pdf - p.3
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587
inhibitor
1767

inducer
389
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2C19
1478

OATP1B1
788

OAT1
599

OAT3
642

OCT1
512

OCT2
647

OATP1B3
706

P-gp
1461

BCRP
699

BSEP
402

MRP2
383

CYP2A6
707

CYP2B6
810

CYP2E1
882
OAT3
339

OATP1B1
406

BSEP
52

MRP2
205

OCT1
327

OCT2
355

OAT1
326

OATP1B3
350

P-gp
1537

BCRP
561

UGT1A1
418
CYP1A2
701

CYP2C19
293
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
773
 no
BSEP
403
 no
CYP1A2
1692
 no
CYP1A2
1692
 no
CYP2A6
739
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C19
1553
 no
CYP2C9
1819
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP3A4
1925
 no
MRP2
475
 no
OAT1
603
 no
OAT3
644
 no
OATP1B3
715
 no
OCT1
543
 no
OCT2
648
 no
P-gp
1650
 no
OATP1B1
803
 weak
CYP2E1
970
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
OAT1
326
 no
OATP1B3
350
 no
OCT1
327
 no
OCT2
355
 no
BCRP
561
 weak
P-gp
1537
 weak
BSEP
52
 yes
UGT1A1
418
 yes
MRP2
205
 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
OAT3
339
 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
OATP1B1
406
 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
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:85980
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:85980
ChemicalBook
CB12723517
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB12723517
MolPort
MolPort-044-183-657
https://www.molport.com/shop/molecule-link/MolPort-044-183-657
ZINC
ZINC000014210876
http://zinc15.docking.org/substances/ZINC000014210876
PubMed

PubMed

TitleDatePubMed
Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers.
2014 Dec 1
Patents

Patents

WO2016135756A1
2

Sample Use Guides

In Vivo Use Guide
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 Vitro Use Guide
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 Dec 16 04:50:34 GMT 2023
Edited
by admin
on Sat Dec 16 04:50:34 GMT 2023
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 [INN]
Common Name English
Eluxadoline [WHO-DD]
Common Name English
Classification Tree Code System Code
WHO-ATC A07DA06
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
NDF-RT N0000191867
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
Code System Code Type Description
INN
9749
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
USAN
ZZ-82
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
CAS
864821-90-9
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
SMS_ID
100000161317
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
WIKIPEDIA
Eluxadoline
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
PUBCHEM
11250029
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
LACTMED
Eluxadoline
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
IUPHAR
7691
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
DRUG BANK
DB09272
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
CHEBI
85980
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
EVMPD
SUB175259
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
ChEMBL
CHEMBL2159122
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
NCI_THESAURUS
C166725
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
DAILYMED
45TPJ4MBQ1
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
EPA CompTox
DTXSID70235589
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
FDA UNII
45TPJ4MBQ1
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
NDF-RT
N0000191866
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY Opioid mu-Receptor Agonists [MoA]
MERCK INDEX
m11882
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
RXCUI
1653781
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY RxNorm
DRUG CENTRAL
5001
Created by admin on Sat Dec 16 04:50:34 GMT 2023 , Edited by admin on Sat Dec 16 04:50:34 GMT 2023
PRIMARY
Related Record Type Details
MU-TYPE OPIOID RECEPTOR
TARGET -> AGONIST
OATP1B1
TRANSPORTER -> INHIBITOR
WEAK
BSEP
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INHIBITOR
In an in-vitro study, eluxadoline appears to show time-dependent inhibition of CYP3A4 at 50 μM, a concentration that can be achieved in the gut (Igut is estimated to be 700 μM).
OATP1B1
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of ELUXADOLINE DIHYDROCHLORIDE
SALT/SOLVATE -> PARENT
MRP-2
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
DELTA-TYPE OPIOID RECEPTOR
TARGET -> INHIBITOR
KAPPA-TYPE OPIOID RECEPTOR
TARGET -> AGONIST
Structure of ELUXADOLINE
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.
OAT-3
TRANSPORTER -> SUBSTRATE
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
Related Record Type Details
Structure of ELUXADOLINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC SINGLE DOSE ADMINISTRATION

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