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

Details

Stereochemistry ACHIRAL
Molecular Formula C18H26ClN3O3.C4H6O4
Molecular Weight 485.958
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PRUCALOPRIDE SUCCINATE

SMILES

OC(=O)CCC(O)=O.COCCCN1CCC(CC1)NC(=O)C2=C3OCCC3=C(N)C(Cl)=C2

InChI

InChIKey=QZRSNVSQLGRAID-UHFFFAOYSA-N
InChI=1S/C18H26ClN3O3.C4H6O4/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14;5-3(6)1-2-4(7)8/h11-12H,2-10,20H2,1H3,(H,21,23);1-2H2,(H,5,6)(H,7,8)

HIDE SMILES / InChI
Molecular Formula C18H26ClN3O3
Molecular Weight 367.87
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C4H6O4
Molecular Weight 118.088
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Prucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. Prucalopride is a potent, selective and specific serotonin 5-HT4 receptor (5-HT4-R) agonist. Prucalopride (Resolor®), a highly selective serotonin 5-HT4 receptor agonist, is indicated in the European Economic Area for the treatment of adults with chronic idiopathic constipation (CIC) in whom laxatives have failed to provide adequate relief.

CNS Activity

Originator

Approval Year

2018
436
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2678
 8.6 null [pKi]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
RESOLOR

Approved Use

Resolor is indicated for symptomatic treatment of chronic constipation in adults in whom laxatives fail to provide adequate relief

Launch Date

2008
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
2 mg 1 times / day steady-state, oral
dose: 2 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PRUCALOPRIDE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
109 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
2 mg 1 times / day steady-state, oral
dose: 2 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PRUCALOPRIDE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
1 day
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
2 mg 1 times / day steady-state, oral
dose: 2 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PRUCALOPRIDE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
70%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
2 mg 1 times / day steady-state, oral
dose: 2 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PRUCALOPRIDE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Disc. AE: Nausea, Headache...
Other AEs: Headache, Abdominal pain...
AEs leading to
discontinuation/dose reduction:
Nausea (2%)
Headache (1%)
Diarrhea (1%)
Abdominal pain (1%)
Other AEs:
Headache (19%)
Abdominal pain (16%)
Upper abdominal pain (16%)
Lower abdominal pain (16%)
Abdominal tenderness (16%)
Abdominal discomfort (16%)
Epigastric discomfort (16%)
Nausea (14%)
Diarrhea (13%)
Abdominal distension (5%)
Dizziness (4%)
Vomiting (3%)
Flatulence (3%)
Fatigue (2%)
Nausea (2%)
Headache (1%)
Diarrhea (1%)
Abdominal pain (1%)
Headache (19%)
Abdominal pain (16%)
Upper abdominal pain (16%)
Lower abdominal pain (16%)
Abdominal tenderness (16%)
Abdominal discomfort (16%)
Epigastric discomfort (16%)
Nausea (14%)
Diarrhea (13%)
Abdominal distension (5%)
Dizziness (4%)
Vomiting (3%)
Flatulence (3%)
Fatigue (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
10 mg 1 times / day multiple, oral
Highest studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf
healthy
n = 60
Health Status: healthy
Population Size: 60
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210166Orig1s000MultidisciplineR.pdf
AEs

AEs

AESignificanceDosePopulation
Abdominal pain 1%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Diarrhea 1%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Headache 1%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal pain 1%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Diarrhea 1%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Headache 1%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Diarrhea 13%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Diarrhea 13%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Nausea 14%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Nausea 14%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal discomfort 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal discomfort 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal pain 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal pain 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal tenderness 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal tenderness 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Epigastric discomfort 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Epigastric discomfort 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Lower abdominal pain 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Lower abdominal pain 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Upper abdominal pain 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Upper abdominal pain 16%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Headache 19%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Headache 19%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Fatigue 2%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Fatigue 2%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Nausea 2%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Nausea 2%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Flatulence 3%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Flatulence 3%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Vomiting 3%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Vomiting 3%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Dizziness 4%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Dizziness 4%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal distension 5%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Abdominal distension 5%
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
unhealthy, 47 years (range: 17-95 years)
n = 1251
Health Status: unhealthy
Condition: chronic idiopathic constipation
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Population Size: 1251
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587

inducer
781
substrate
1037

inhibitor
1767
substrate
1217

inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP2E1
882

OATP1B1
788

OATP1B3
706

OAT1
599

OAT3
642

BSEP
402

MRP2
383

OCT1
512

OCT2
647

MATE1
306

MATE2
263

P-gp
1461

BCRP
699
CYP1A1
349

CYP1A2
1054

CYP2A6
543

CYP2B6
664

CYP2C8
693

CYP2C19
991

CYP2E1
667

CYP3A5
395

P-gp
1537

BCRP
561

OATP1B1
406

OATP1B3
350

OAT1
326

OAT3
339

OCT1
327

OCT2
355

MATE1
135

MATE2
96

BSEP
52

MRP2
205
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no [IC50 >100 uM]
CYP2A6
739
 no [IC50 >100 uM]
CYP2B6
1001
 no [IC50 >100 uM]
CYP2C19
1553
 no [IC50 >100 uM]
CYP2C8
965
 no [IC50 >100 uM]
CYP2C9
1819
 no [IC50 >100 uM]
CYP2E1
970
 no [IC50 >100 uM]
CYP3A4
1925
 no [IC50 >100 uM]
BCRP
773
 no [IC50 >=300 uM]
P-gp
1650
 no [IC50 >=300 uM]
BSEP
403
 no
CYP1A2
1692
 no
CYP3A4
1925
 no
MRP2
475
 no
OAT1
603
 no
OAT3
644
 no
OATP1B1
803
 no
OATP1B3
715
 no
CYP2B6
1001
 weak
CYP2D6
1891
 yes [IC50 38 uM]
weak (co-administration study)
Comment: administered with dextromethorphan; in vivo DDI potential via inhibition of CYP2D6 appears low at the proposed dose
Page: 188.0
MATE1
308
 yes [IC50 4 uM]
MATE2
263
 yes [IC50 69 uM]
OCT2
648
 yes [IC50 7.8 uM]
OCT1
543
 yes [IC50 9.4 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BSEP
52
 no
CYP1A1
349
 no
CYP1A2
1054
 no
CYP2A6
543
 no
CYP2B6
664
 no
CYP2C19
991
 no
CYP2C8
693
 no
CYP2C9
1037
 no
CYP2D6
1217
 no
CYP2E1
667
 no
CYP3A5
395
 no
MATE1
135
 no
MATE2
96
 no
MRP2
205
 no
OAT1
326
 no
OAT3
339
 no
OATP1B1
406
 no
OATP1B3
350
 no
OCT1
327
 no
OCT2
355
 no
P-gp
1537
 yes [Km 116 uM]
BCRP
561
 yes [Km 15 uM]
CYP3A4
1737
 yes
weak (co-administration study)
Comment: co-administration of ketoconazole increased the Cmax and AUCtau of prucalopride at steady state by 38% and 37%, respectively; Administration of erythromycin, probenecid, cimetidine, and paroxetine did not have a significant effect on the PK of prucalopride (<10% change in Cmax and AUC)
Page: 100;187
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA0026Y3
http://www.aablocks.com/goods/Goods/detail?id=AA0026Y3
AK Scientific, Inc. (AKSCI)
Y0251
http://www.aksci.com/item_detail.php?cat=Y0251
Aaron Chemicals
AR0027PV
http://www.aaronchem.com/179474-81-8
AbMole Bioscience
M2146
http://www.abmole.com/products/prucalopride.html
Achemtek
0104-024538
http://www.achemtek.com/179474-81-8
Adooq BioScience
A11771
https://www.adooq.com/prucalopride.html
Alfa Chemistry
AP179474818
https://reagents.alfa-chemistry.com/product/prucalopride-cas-179474-81-8-6688.html
Alsachim
2960
http://www.alsachim.com/product-C4032-glo.bal-view.html
Ambinter
Amb20241338
http://www.ambinter.com/reference/20241338
Angel Pharmatech
AG151228
http://www.angelpharmatech.com/179474-81-8.html
ApexBio Technology
B2253
http://www.apexbt.com/prucalopride.html
Ark Pharm
AK170477
http://www.arkpharminc.com/products/179474-81-8.html
Aurora Fine Chemicals LLC
A24.082.365
http://online.aurorafinechemicals.com/info?ID=A24.082.365
Aurora Fine Chemicals LLC
K16.609.755
http://online.aurorafinechemicals.com/info?ID=K16.609.755
Aurum Pharmatech LLC
Q-3828
http://www.Aurumpharmatech.com/Product/ProductDetails/Q_3828
Axon MedChem
1479
https://www.axonmedchem.com/product/1479
BLD Pharm
BD149417
http://www.bldpharm.com/products/179474-81-8.html
BioChemPartner
BCP02177
http://www.biochempartner.com/179474-81-8-BCP02177
BioCrick
BCC5055
http://www.biocrick.com/Prucalopride-BCC5055.html
CSNpharm
CSN11795
https://www.csnpharm.com/products/prucalopride.html
Capot Chemical
22481
http://www.capotchem.com/en/22481.htm
Capot Chemical
PubChem22481
http://www.capotchem.com/en/22481.htm
Chem Scene
CS-2574
http://www.chemscene.com/179474-81-8.html
ChemMol
49400298
http://www.chemmol.com/chemmol/49400298.html
ChemMol
97900178
http://www.chemmol.com/chemmol/97900178.html
Chemenu
CM107382
http://www.chemenu.com/products/CM107382
Chemspace
CSSB00016993940
https://chem-space.com/CSSB00016993940
Clearsynth
CS-O-30738
https://www.clearsynth.com/en/CSO30738.html
DC Chemicals
DC4147
http://www.dcchemicals.com/product_show-Prucalopride.html
Excenen
EX-A1333
http://www.excenen.com/searchresultlist.php?id=179474-81-8
Finetech
FT-0674128
http://www.finetechnology-ind.com/prod/detail/pub/179474-81-8.html
Glentham Life Sciences
GP6979
http://www.glentham.com/products/product/GP6979/
Hairui
HR103880
http://www.hairuichem.com/en/product/179474-81-8.html
Lab Network
LN01343283
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343283
MedChem Express
HY-14151
https://www.medchemexpress.com/Prucalopride.html
MuseChem
A000859
https://www.musechem.com/product/A000859.html
OChem
25269
http://www.ocheminc.com/index.php?act=psearch&pid=474P818
Renno Tech
RL02293
http://www.rennotech.com/product_show.asp?id=2542
Smolecule
S540468
http://www.smolecule.com/products/s540468
Synblock Inc
PB31402
http://www.synblock.com/product/179474-81-8.html
THE BioTek
bt-280940
https://www.thebiotek.com/product/inhibitors/bt-280940
THE BioTek
bt-331990
https://www.thebiotek.com/product/others/bt-331990
VladaChem
VL261712-1G
https://www.vladachem.com/product.php?products=179474-81-8
abcr GmbH
AB454709
http://www.abcr.com/shop/en/AB454709
eNovation Chemicals
D381138
http://www.enovationchem.com/productDetails.asp?productID=D381138
eNovation Chemicals
Y1012706
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1012706
iChemical
EBD25754
http://www.ichemical.com/chemicals/cas-179474-81-8
PubMed

PubMed

TitleDatePubMed
Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
2000 Feb
Serotonin: a mediator of the brain-gut connection.
2000 Oct
Prucalopride accelerates gastrointestinal and colonic transit in patients with constipation without a rectal evacuation disorder.
2001 Feb
Pharmacological treatment of irritable bowel syndrome--from concept to sales.
2002
Irritable bowel syndrome: update on pathogenesis and management.
2002 Jan-Mar
The effects of the specific 5HT(4) receptor agonist, prucalopride, on colonic motility in healthy volunteers.
2002 Mar
Review article: the complexity of drug development for irritable bowel syndrome.
2002 Mar
New and emerging treatments for irritable bowel syndrome and functional dyspepsia.
2002 May
5-HT4 receptors exert a frequency-related facilitatory control on dorsal raphé nucleus 5-HT neuronal activity.
2002 Sep
Prucalopride is effective in patients with severe chronic constipation in whom laxatives fail to provide adequate relief. Results of a double-blind, placebo-controlled clinical trial.
2003
[Visceral hypersensitivity: a concept within our reach].
2003 Jan
Irritable bowel syndrome: an overview of diagnosis and pharmacologic treatment.
2003 Jun
Electrophysiological effects of prucalopride, a novel enterokinetic agent, on isolated atrial myocytes from patients treated with beta-adrenoceptor antagonists.
2005 Apr
Rationale for using serotonergic agents to treat irritable bowel syndrome.
2005 Apr 1
5-HT4 receptor agonists enhance both cholinergic and nitrergic activities in human isolated colon circular muscle.
2006 Sep
The serotonin signaling system: from basic understanding to drug development for functional GI disorders.
2007 Jan
Electrophysiological and arrhythmogenic effects of 5-hydroxytryptamine on human atrial cells are reduced in atrial fibrillation.
2007 Jan
Gastric and enteric involvement in progressive systemic sclerosis.
2008 Jan
Prucalopride: the evidence for its use in the treatment of chronic constipation.
2008 Jun
Management of constipation in the elderly: emerging therapeutic strategies.
2008 Sep 7
Prucalopride: a new drug for the treatment of chronic constipation.
2009 Aug
Prucalopride for chronic constipation.
2009 Dec
Gateways to clinical trials.
2009 Mar
Prucalopride (Resolor) in the treatment of severe chronic constipation in patients dissatisfied with laxatives.
2009 Mar
Comments on tegaserod trial on irritable bowel syndrome.
2010 Apr
Effect of ICU interventions on gastrointestinal motility.
2010 Apr
Update on the management of constipation in the elderly: new treatment options.
2010 Aug 9
Prucalopride for constipation.
2010 Feb
Hyperfunction of muscarinic receptor maintains long-term memory in 5-HT4 receptor knock-out mice.
2010 Mar 4
Emerging pharmacologic therapies for irritable bowel syndrome.
2010 Oct
Efficacy and safety of prucalopride in patients with chronic noncancer pain suffering from opioid-induced constipation.
2010 Oct
Fixed combination of oxycodone with naloxone: a new way to prevent and treat opioid-induced constipation.
2010 Sep
A double-blind, placebo-controlled study of prucalopride in elderly patients with chronic constipation.
2010 Sep
Patents

Patents

JP2002542287A
27

Sample Use Guides

In Vivo Use Guide
Adults: 2 mg once daily with or without food, at any time of the day.
Route of Administration: Oral
In Vitro Use Guide
Cell shortening and real-time Ca(2+) measurements were processed on field-stimulated intact cardiomyocytes with the selective 5-HT4R agonist, prucalopride (1 uM).
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:32:35 GMT 2023
Edited
by admin
on Fri Dec 15 15:32:35 GMT 2023
Record UNII
4V2G75E1CK
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PRUCALOPRIDE SUCCINATE
MART.   USAN   WHO-DD  
USAN  
Official Name English
PRUCALOPRIDE SUCCINATE [USAN]
Common Name English
PRUCALOPRIDE SUCCINATE [MART.]
Common Name English
MOTEGRITY
Brand Name English
Prucalopride succinate [WHO-DD]
Common Name English
PRUCALOPRIDE (AS SUCCINATE)
Common Name English
BUTANEDIOIC ACID, COMPD. WITH 4-AMINO-5-CHLORO-2,3-DIHYDRO-N-(1-(3-METHOXYPROPYL)-4-PIPERIDINYL)-7-BENZOFURANCARBOXAMIDE (1:1)
Common Name English
RESOLOR
Brand Name English
PRUCALOPRIDE SUCCINATE [ORANGE BOOK]
Common Name English
R-108512
Code English
Classification Tree Code System Code
NCI_THESAURUS C47794
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
EMA ASSESSMENT REPORTS RESOLOR (AUTHORIZED: CONSTIPATION)
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
Code System Code Type Description
USAN
YY-101
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
EPA CompTox
DTXSID701027749
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
FDA UNII
4V2G75E1CK
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
PUBCHEM
9870009
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
EVMPD
SUB28850
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
RXCUI
2107309
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
NCI_THESAURUS
C152112
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
CAS
179474-85-2
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
SMS_ID
100000092989
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
ChEMBL
CHEMBL117287
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
DRUG BANK
DBSALT002626
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
DAILYMED
4V2G75E1CK
Created by admin on Fri Dec 15 15:32:35 GMT 2023 , Edited by admin on Fri Dec 15 15:32:35 GMT 2023
PRIMARY
Related Record Type Details
Structure of PRUCALOPRIDE
PARENT -> SALT/SOLVATE
Structure of SUCCINIC ACID
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of PRUCALOPRIDE
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