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
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
| 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 |
DescriptionCurator'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
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
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 1.7 nM [Ki] | |||
| 1.3 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | VIBERZI Approved UseVIBERZI is a mu-opioid receptor agonist, indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D) Launch Date1.43259835E12 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
19% |
unknown, oral |
ELUXADOLINE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse 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: |
healthy, adult Health Status: healthy Age Group: adult Sex: M Sources: |
Other AEs: Nausea, Abdominal pain... Other AEs: Nausea Sources: Abdominal pain Constipation |
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: |
healthy, adult n = 8 Health Status: healthy Age Group: adult Sex: F Population Size: 8 Sources: |
|
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: |
healthy, adult n = 5 Health Status: healthy Age Group: adult Sex: M Population Size: 5 Sources: |
|
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... Other AEs: Rash (3%) Sources: |
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%) Other AEs:Constipation (1.5%) Headache (0.1%) Dizziness (0.1%) Vomiting (0.2%) Somnolence (0.1%) Dizziness (2.6%) Sources: 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%) |
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... Other AEs: Rash (3%) 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: |
Disc. AE: Abdominal pain, Constipation... Other AEs: Dizziness, Fatigue... AEs leading to discontinuation/dose reduction: Abdominal pain (1.5%) Other AEs:Constipation (1.1%) Nausea (0.6%) Headache (0.4%) Dizziness (0.1%) Vomiting (0.1%) Pruritis (0.1%) Dizziness (2.6%) Sources: 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%) |
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%) Sources: Page: nda/2015/206940Orig1s000MedR.pdf - p.3Constipation (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%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| 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: |
healthy, adult Health Status: healthy Age Group: adult Sex: M Sources: |
|
| 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: |
healthy, adult Health Status: healthy Age Group: adult Sex: M Sources: |
|
| 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: |
healthy, adult Health Status: healthy Age Group: adult Sex: M Sources: |
|
| 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 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical 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
| Target | Modality | Activity | Metabolite | Clinical 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf#page=10 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf#page=10 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/206940Orig1s000ClinPharmR.pdf#page=10 Page: 10.0 |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Modulation of gastrointestinal function by MuDelta, a mixed µ opioid receptor agonist/ µ opioid receptor antagonist. | 2012 Nov |
|
| Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. | 2014 Dec 1 |
|
| Eluxadoline: First Global Approval. | 2015 Jul |
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
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A07DA06
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NDF-RT |
N0000191867
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9749
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Eluxadoline
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Eluxadoline
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N0000191866
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m11882
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5001
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> AGONIST |
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TRANSPORTER -> INHIBITOR |
WEAK
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TRANSPORTER -> SUBSTRATE |
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
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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).
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TRANSPORTER -> SUBSTRATE |
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
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BINDER->LIGAND |
BINDING
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> SUBSTRATE |
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
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TARGET -> INHIBITOR |
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TARGET -> AGONIST |
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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.
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TRANSPORTER -> SUBSTRATE |
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
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| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Biological Half-life | PHARMACOKINETIC |
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| Tmax | PHARMACOKINETIC |
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SINGLE DOSE ADMINISTRATION |
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