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

Details

Stereochemistry ACHIRAL
Molecular Formula C18H26ClN3O3
Molecular Weight 367.87
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Prucalopride

SMILES

COCCCN1CCC(CC1)NC(=O)C2=CC(Cl)=C(N)C3=C2OCC3

InChI

InChIKey=ZPMNHBXQOOVQJL-UHFFFAOYSA-N
InChI=1S/C18H26ClN3O3/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/h11-12H,2-10,20H2,1H3,(H,21,23)

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

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
425
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2752
 8.6 null [pKi]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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
Health Status: healthy
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 47 years (range: 17-95 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210166s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252

inducer
1087
substrate
1193

inhibitor
2438
substrate
1388

inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2A6
879

CYP2B6
926

CYP2C8
1057

CYP2C19
2057

CYP2E1
1060

OATP1B1
1079

OATP1B3
961

OAT1
725

OAT3
747

BSEP
550

MRP2
499

OCT1
620

OCT2
779

MATE1
415

MATE2
267

P-gp
1741

BCRP
910
CYP1A1
389

CYP1A2
1197

CYP2A6
626

CYP2B6
776

CYP2C8
810

CYP2C19
1119

CYP2E1
729

CYP3A5
446

P-gp
2052

BCRP
697

OATP1B1
503

OATP1B3
435

OAT1
395

OAT3
391

OCT1
393

OCT2
434

MATE1
182

MATE2
98

BSEP
63

MRP2
252
CYP1A2
832

CYP2B6
669
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
2333
 no [IC50 >100 uM]
CYP2A6
911
 no [IC50 >100 uM]
CYP2B6
1160
 no [IC50 >100 uM]
CYP2C19
2141
 no [IC50 >100 uM]
CYP2C8
1117
 no [IC50 >100 uM]
CYP2C9
2497
 no [IC50 >100 uM]
CYP2E1
1146
 no [IC50 >100 uM]
CYP3A4
2633
 no [IC50 >100 uM]
BCRP
985
 no [IC50 >=300 uM]
P-gp
1932
 no [IC50 >=300 uM]
BSEP
554
 no
CYP1A2
2333
 no
CYP3A4
2633
 no
MRP2
625
 no
OAT1
730
 no
OAT3
749
 no
OATP1B1
1095
 no
OATP1B3
970
 no
CYP2B6
1160
 weak
CYP2D6
2546
 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
416
 yes [IC50 4 uM]
MATE2
267
 yes [IC50 69 uM]
OCT2
782
 yes [IC50 7.8 uM]
OCT1
656
 yes [IC50 9.4 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BSEP
63
 no
CYP1A1
389
 no
CYP1A2
1197
 no
CYP2A6
626
 no
CYP2B6
776
 no
CYP2C19
1119
 no
CYP2C8
810
 no
CYP2C9
1193
 no
CYP2D6
1388
 no
CYP2E1
729
 no
CYP3A5
446
 no
MATE1
182
 no
MATE2
98
 no
MRP2
252
 no
OAT1
395
 no
OAT3
391
 no
OATP1B1
503
 no
OATP1B3
435
 no
OCT1
393
 no
OCT2
434
 no
P-gp
2052
 yes [Km 116 uM]
BCRP
697
 yes [Km 15 uM]
CYP3A4
1946
 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
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA0026Y3
http://www.aablocks.com/goods/Goods/detail?id=AA0026Y3
Aaron Chemicals
AR0027PV
http://www.aaronchem.com/179474-81-8
abcr GmbH
AB454709
http://www.abcr.com/shop/en/AB454709
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
AK Scientific, Inc. (AKSCI)
Y0251
http://www.aksci.com/item_detail.php?cat=Y0251
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
BioChemPartner
BCP02177
http://www.biochempartner.com/179474-81-8-BCP02177
BioCrick
BCC5055
http://www.biocrick.com/Prucalopride-BCC5055.html
BLD Pharm
BD149417
http://www.bldpharm.com/products/179474-81-8.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
Chemenu
CM107382
http://www.chemenu.com/products/CM107382
ChemMol
49400298
http://www.chemmol.com/chemmol/49400298.html
ChemMol
97900178
http://www.chemmol.com/chemmol/97900178.html
Chemspace
CSSB00016993940
https://chem-space.com/CSSB00016993940
Clearsynth
CS-O-30738
https://www.clearsynth.com/en/CSO30738.html
CSNpharm
CSN11795
https://www.csnpharm.com/products/prucalopride.html
DC Chemicals
DC4147
http://www.dcchemicals.com/product_show-Prucalopride.html
eNovation Chemicals
D381138
http://www.enovationchem.com/productDetails.asp?productID=D381138
eNovation Chemicals
Y1012706
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1012706
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
iChemical
EBD25754
http://www.ichemical.com/chemicals/cas-179474-81-8
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
PubMed

PubMed

TitleDatePubMed
Emerging pharmacologic therapies for irritable bowel syndrome.
2010-10
Efficacy and safety of prucalopride in patients with chronic noncancer pain suffering from opioid-induced constipation.
2010-10
Fixed combination of oxycodone with naloxone: a new way to prevent and treat opioid-induced constipation.
2010-09
A double-blind, placebo-controlled study of prucalopride in elderly patients with chronic constipation.
2010-09
Update on the management of constipation in the elderly: new treatment options.
2010-08-09
[New drugs for the treatment of constipation].
2010-07
Psychometric evaluation of a visual analog scale for the assessment of anxiety.
2010-06-08
New-generation 5-HT4 receptor agonists: potential for treatment of gastrointestinal motility disorders.
2010-06
Influence of 5-HT4 receptor activation on acetylcholine release in human large intestine with endometriosis.
2010-05
Comments on tegaserod trial on irritable bowel syndrome.
2010-04
Effect of ICU interventions on gastrointestinal motility.
2010-04
Hyperfunction of muscarinic receptor maintains long-term memory in 5-HT4 receptor knock-out mice.
2010-03-04
Selective serotonin reuptake inhibitors potentiate the rapid antidepressant-like effects of serotonin4 receptor agonists in the rat.
2010-02-16
Prucalopride for constipation.
2010-02
Psychometric performance and clinical meaningfulness of the Patient Assessment of Constipation-Quality of Life questionnaire in prucalopride (RESOLOR) trials for chronic constipation.
2010-02
Investigations into the binding affinities of different human 5-HT4 receptor splice variants.
2010
Gateways to clinical trials.
2009-12
Prucalopride for chronic constipation.
2009-12
Translating 5-HT receptor pharmacology.
2009-12
Safety assessment of prucalopride in elderly patients with constipation: a double-blind, placebo-controlled study.
2009-12
Prucalopride: a new drug for the treatment of chronic constipation.
2009-08
Motility: prucalopride for chronic constipation.
2009-06
The use of novel promotility and prosecretory agents for the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation.
2009-05
Gateways to clinical trials.
2009-04
Gateways to clinical trials.
2009-03
Prucalopride (Resolor) in the treatment of severe chronic constipation in patients dissatisfied with laxatives.
2009-03
Clinical trial: the efficacy, impact on quality of life, and safety and tolerability of prucalopride in severe chronic constipation--a 12-week, randomized, double-blind, placebo-controlled study.
2009-02-01
Selective desensitization of the 5-HT4 receptor-mediated response in pig atrium but not in stomach.
2009-01
Prucalopride.
2009
New treatments for irritable bowel syndrome in women.
2008-11
Gateways to clinical trials. July-August 2008.
2008-10-14
[Functional and motor gastrointestinal disorders].
2008-10
Gateways to clinical trials.
2008-10
Management of constipation in the elderly: emerging therapeutic strategies.
2008-09-07
Gateways to clinical trials.
2008-09
Alternative splicing and exon duplication generates 10 unique porcine 5-HT 4 receptor splice variants including a functional homofusion variant.
2008-06-12
Prucalopride: the evidence for its use in the treatment of chronic constipation.
2008-06
The long and short of a constipation-reducing medication.
2008-05-29
A placebo-controlled trial of prucalopride for severe chronic constipation.
2008-05-29
Synergy between 5-HT4 receptor activation and acetylcholinesterase inhibition in human colon and rat forestomach.
2008-05
Prucalopride and donepezil act synergistically to reverse scopolamine-induced memory deficit in C57Bl/6j mice.
2008-03-05
5-HT4 receptor agonists: similar but not the same.
2008-02
Gastric and enteric involvement in progressive systemic sclerosis.
2008-01
Recent advances in understanding the role of serotonin in gastrointestinal motility in functional bowel disorders: alterations in 5-HT signalling and metabolism in human disease.
2007-08
5-HT4 receptor agonists increase sAPPalpha levels in the cortex and hippocampus of male C57BL/6j mice.
2007-04
The action of the novel gastrointestinal prokinetic prucalopride on the HERG K+ channel and the common T897 polymorph.
2007-01-12
The serotonin signaling system: from basic understanding to drug development for functional GI disorders.
2007-01
Little or no ability of obestatin to interact with ghrelin or modify motility in the rat gastrointestinal tract.
2007-01
Electrophysiological and arrhythmogenic effects of 5-hydroxytryptamine on human atrial cells are reduced in atrial fibrillation.
2007-01
5-HT4 receptor agonists enhance both cholinergic and nitrergic activities in human isolated colon circular muscle.
2006-09
Patents

Patents

JP2002542287A
30

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 Mon Mar 31 18:33:30 GMT 2025
Edited
by admin
on Mon Mar 31 18:33:30 GMT 2025
Record UNII
0A09IUW5TP
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
R-093877
Preferred Name English
Prucalopride
EMA EPAR   INN   MART.   MI   USAN   WHO-DD  
INN   USAN  
Official Name English
4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidyl]-7-benzofurancarboxamide
Systematic Name English
PRUCALOPRIDE [EMA EPAR]
Common Name English
PRUCALOPRIDE [MI]
Common Name English
R093877
Common Name English
PRUCALOPRIDE [USAN]
Common Name English
7-Benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-
Systematic Name English
4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide
Systematic Name English
Prucalopride [WHO-DD]
Common Name English
PRUCALOPRIDE [MART.]
Common Name English
prucalopride [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC A03AE04
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
NCI_THESAURUS C47794
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
WHO-ATC A06AX05
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
WHO-VATC QA06AX05
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
Code System Code Type Description
FDA UNII
0A09IUW5TP
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
INN
7702
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
RXCUI
2107310
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
SMS_ID
100000080862
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
DAILYMED
0A09IUW5TP
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
EVMPD
SUB10155MIG
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
NCI_THESAURUS
C74386
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
MESH
C406662
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
DRUG CENTRAL
3502
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
EPA CompTox
DTXSID5057670
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
LACTMED
Prucalopride
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
ChEMBL
CHEMBL117287
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
IUPHAR
243
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
DRUG BANK
DB06480
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
WIKIPEDIA
PRUCALOPRIDE
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
USAN
YY-100
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
MERCK INDEX
m9285
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY Merck Index
CAS
179474-81-8
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
PUBCHEM
3052762
Created by admin on Mon Mar 31 18:33:30 GMT 2025 , Edited by admin on Mon Mar 31 18:33:30 GMT 2025
PRIMARY
Related Record Type Details
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> SUBSTRATE
Structure of Prucalopride
EXCRETED UNCHANGED
URINE
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of Prucalopride
CUMULATIVE EXCRETION
FECAL
Structure of Prucalopride
EXCRETED UNCHANGED
URINE
Structure of Prucalopride succinate
SALT/SOLVATE -> PARENT
5-HYDROXYTRYPTAMINE RECEPTOR 4
TARGET -> AGONIST
Interaction with the 5-HT4 receptor leads to the elevation of cyclic adenosine monophosphate (cAMP) levels in HEK293 cells
EC50
Structure of Prucalopride
CUMULATIVE EXCRETION
URINE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
In human plasma, the binding of R093877 increased at higher pH values. In the pH-range 7.1 to 7.7, the percentage bound increased from 23.3% to 35.5%
BINDING
Structure of PRUCALOPRIDE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of O-DESMETHYL PRUCALOPRIDE ACID
METABOLITE -> PARENT
Seven metabolites were recovered in urine and feces, with the most abundant metabolite R107504 (O-desmethyl prucalopride acid) accounting for 3.2% and 3.1% of the dose in urine and feces, respectively.
FECAL; URINE
Related Record Type Details
Structure of Prucalopride
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC ROUTE OF ADMINISTRATION
PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC DOSE
PHARMACOKINETIC
ROUTE OF ADMINISTRATION
PHARMACOKINETIC
BREAST MILK/PLASMA RATIO PHARMACOKINETIC COMMENTS
PHARMACOKINETIC
NIH
NCATS
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