Page last updated: 2024-11-10

prucalopride

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Description

prucalopride: a 5-HT4 agonist enterokinetic compound [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3052762
CHEMBL ID117287
CHEBI ID135552
SCHEMBL ID16952
MeSH IDM0360790

Synonyms (70)

Synonym
gtpl243
r-93877
r-093877
prucalopride
CHEBI:135552
4-amino-5-chloro-2,3-dihydro-benzofuran-7-carboxylic acid [1-(3-methoxy-propyl)-piperidin-4-yl]-amide
bdbm50122872
L000891
CHEMBL117287 ,
r093877
179474-81-8
D09205
prucalopride (usan/inn)
4-amino-5-chloro-n-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide
A25458
motegrity
4-amino-5-chloro-n-(1-(3-methoxypropyl)-4-piperidinyl)-2,3-dihydro-1-benzofuran-7-carboxamide
resotrans
4-amino-5-chloro-2,3-dihydro-n-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide
AKOS015951096
4-amino-5-chloro-2,3-dihydro-n-(1-(3-methoxypropyl)-4-piperidyl)-7-benzofurancarboxamide
prucalopride [usan:inn:ban]
unii-0a09iuw5tp
0a09iuw5tp ,
FT-0674128
BCPP000099
NCGC00253867-01
PB31402
AM84628
4-amino-5-chloro-2,3-dihydro-n-[1-(3-methoxypropyl)-4-piperidyl]-7-benzofurancarboxamide
prucalopride [usan]
prucalopride [mart.]
prucalopride [inn]
prucalopride [mi]
prucalopride [who-dd]
prucalopride [ema epar]
S2875
HY-14151
SCHEMBL16952
cas-179474-81-8
dtxsid5057670 ,
dtxcid2031459
tox21_113885
NCGC00253867-02
4-amino-5-chloro-n-[1-(3-methoxypropyl)-4-piperidyl]-2,3-dihydrobenzofuran-7-carboxamide
4-amino-5+k445-chloro-2,3-dihydro-benzofuran-7-carboxylic acid [1-(3-methoxy-propyl)-piperidin-4-yl]-amide
4-amino-5-chloro-n-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide
AC-23945
DB06480
EX-A1333
SR-01000945275-1
sr-01000945275
HMS3651F04
mfcd09837787
SW219198-2
179474-81-8 (free base)
AS-19549
BCP02177
Q68484
7-benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-n-[1-(3-methoxypropyl)-4-piperidinyl]-
HMS3884P20
HMS3748M09
CCG-268257
SY097702
a06ax05
prucalopridum
prucaloprida
prucalopride (mart.)
P2467
EN300-7393093

Research Excerpts

Overview

Prucalopride is a prokinetic drug, that has been commercially available in recent years for the treatment of chronically constipated adults. It is a serotonin receptor agonist that stimulates gastrointestinal motility and provides propulsive force for defecation.

ExcerptReferenceRelevance
"Prucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. "( The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Bosmans, JP; Briejer, MR; Heylen, L; Jurzak, M; Leysen, JE; Prins, NH; Schuurkes, JA; Van Daele, P, 2001
)
2.02
"Prucalopride is a dihydrobenzofurancarboxamide derivative with gastrointestinal prokinetic activities and is recommended as an appropriate choice in patients unresponsive to laxatives."( Safety/Efficacy of Prucalopride in Korean Patients with Chronic Constipation: Post-marketing Surveillance.
Choi, CH; Choi, MG; Chung, WC; Jeon, SW; Kim, SY; Park, SJ; Yeon, SE, 2021
)
1.67
"Prucalopride is a selective serotonin-4-receptor agonist that may improve gut motility."( Effect of prucalopride to improve time to gut function recovery following elective colorectal surgery: randomized clinical trial.
Bissett, I; Liu, C; Milne, T; O'Grady, G; Woodfield, J, 2022
)
1.85
"Prucalopride is a novel, well-tolerated enterokinetic with high 5-hydroxytryptamine 4 receptor selectivity."( Efficacy and safety analysis of prucalopride in refractory chronic constipation cases in a tertiary care hospital in Eastern India: A randomized, single-blind, placebo-controlled study.
Das, HS; Dehury, S; Goutam, S; Kaushik, C; Mohapatra, S,
)
1.14
"Prucalopride is a selective, high-affinity serotonin type 4 receptor agonist approved for the treatment of chronic idiopathic constipation (CIC) in adults. "( Effects of treatment cessation and re-treatment in randomized controlled trials of prucalopride in patients with chronic idiopathic constipation.
Achenbach, H; Boules, M; Hinson, J; Terreri, B, 2023
)
2.58
"Prucalopride is a pan-gut prokinetic with selective agonist effects on serotonin 5-HT4 receptors in the gut."( Prucalopride in diabetic and connective tissue disease-related gastroparesis: Randomized placebo-controlled crossover pilot trial.
Andrews, CN; Buresi, M; Curley, M; Gupta, M; Nasser, Y; Tack, J; Wilsack, L; Woo, M, 2021
)
2.79
"Prucalopride is a serotonin receptor agonist that stimulates gastrointestinal motility and provides propulsive force for defecation."( A randomized controlled trial comparing the efficacy of 1-L polyethylene glycol solution with ascorbic acid plus prucalopride versus 2-L polyethylene glycol solution with ascorbic acid for bowel preparation.
Choi, BK; Choi, HS; Choi, SJ; Chun, HJ; Jeen, YT; Keum, B; Kim, CD; Kim, ES; Kim, SH; Kim, W; Lee, HS; Lee, JM; Min, G, 2018
)
1.41
"Prucalopride is a prokinetic drug, that has been commercially available in recent years for the treatment of chronically constipated patients. "( Prucalopride for the treatment of constipation: a view from 2015 and beyond.
Bassotti, G; Bellini, M; Usai Satta, P, 2019
)
3.4
"Prucalopride is a selective, high-affinity 5-HT4 receptor agonist with gastrointestinal prokinetic activities. "( Oral prucalopride in children with functional constipation.
Ausma, J; Benninga, MA; Di Lorenzo, C; Gilger, MA; Hoppenbrouwers, M; Hyman, PE; Kearns, GL; Vandeplassche, L; Winter, HS, 2013
)
2.35
"Prucalopride is a selective, high-affinity, 5-hydroxytryptamine 4 (5-HT4) receptor agonist, which is approved for the symptomatic treatment of chronic constipation in women in whom laxatives fail to provide adequate relief. "( Effect of prucalopride on the pharmacokinetics of oral contraceptives in healthy women.
Ausma, J; Boterman, M; Hoppenbrouwers, M; Van de Velde, V; Vandeplassche, L, 2013
)
2.23
"Prucalopride is a selective serotonin receptor agonist with prokinetic activity, indicated for women with chronic constipation in whom laxatives have failed to provide adequate relief. "( The association between prucalopride efficacy and constipation type.
Brown, SR; Chapple, K; Jadav, AM; McMullin, CM; Smith, J, 2013
)
2.14
"Prucalopride is a 5-HT4 receptor agonist with gastrointestinal prokinetic activities. "( Effect of prucalopride on symptoms of chronic constipation.
Dubois, D; Joseph, A; Kerstens, R; Stanghellini, V; Tack, J; Vandeplassche, L, 2014
)
2.25
"Prucalopride is a selective 5-hydroxytryptamine receptor agonist."( Novel therapies for constipation.
Ali, H; Thayalasekeran, S; Tsai, HH, 2013
)
1.11
"Prucalopride is a novel enterokinetic drug, that has been demonstrated to improve bowel functions and relieve a broad spectrum of digestive symptoms in patients with severe chronic constipation who had failed to respond to various traditional laxatives."( [Some practical questions on chronic stipsis treatment with prucalopride].
Barbara, G; Bellacosa, L; Cogliandro, R; Cremon, C; De Giorgio, R; Stanghellini, V, 2014
)
1.37
"Prucalopride is a selective, high-affinity agonist of the 5-hydroxytryptamine (serotonin) receptor 4 that enhances motility in the gastrointestinal tract. "( Prucalopride is no more effective than placebo for children with functional constipation.
Ausma, J; Benninga, MA; Bodi, P; Green, A; Kerstens, R; Korczowski, B; Levine, A; Mugie, SM; Ruth, M, 2014
)
3.29
"Prucalopride is a first-in-class selective, high affinity serotonin 5-hydroxytryptamine type 4 (5-HT4) receptor agonist promoting gastro-intestinal prokinetic activity and has been evaluated for the treatment of CC."( Efficacy and safety of prucalopride in adults and children with chronic constipation.
Benninga, MA; Diederen, K; Mugie, SM, 2015
)
1.45
"Prucalopride is a high-affinity 5-HT4 receptor agonist for the treatment of chronic constipation. "( Association between health-related quality of life and symptoms in patients with chronic constipation: an integrated analysis of three phase 3 trials of prucalopride.
Camilleri, M; Dubois, D; Joseph, A; Kerstens, R; Tack, J; Vandeplassche, L, 2015
)
2.06
"Prucalopride is a highly selective 5-hydroxytryptamine receptor-4 agonist with colonic pro-motility effects."( Randomised clinical trial: prucalopride, a colonic pro-motility agent, reduces the duration of post-operative ileus after elective gastrointestinal surgery.
Gong, J; Gu, L; Guo, Z; Li, J; Li, N; Li, Y; Lu, N; Xie, Z; Yao, W; Zhang, T; Zhu, W, 2016
)
1.45
"Prucalopride is a safe and effective treatment to reduce post-operative ileus and systemic inflammation without affecting post-operative complications in patients undergoing elective gastrointestinal surgery. "( Randomised clinical trial: prucalopride, a colonic pro-motility agent, reduces the duration of post-operative ileus after elective gastrointestinal surgery.
Gong, J; Gu, L; Guo, Z; Li, J; Li, N; Li, Y; Lu, N; Xie, Z; Yao, W; Zhang, T; Zhu, W, 2016
)
2.17
"Prucalopride is a new prokinetic agent, recently available in Europe for the treatment of functional constipation in adults in whom treatment with laxatives failed to provide adequate relief. "( Prucalopride: For functional constipation only?
Bassotti, G; Bellini, M; Gambaccini, D, 2016
)
3.32
"Prucalopride is an efficacious and generally safe, new therapeutic option in the management of chronic constipation."( Prucalopride for constipation.
Camilleri, M; Deiteren, A, 2010
)
3.25
"Prucalopride is a new, selective 5-HT(4) agonist and enterokinetic with strong clinical data in chronic constipation."( Efficacy and safety of prucalopride in patients with chronic noncancer pain suffering from opioid-induced constipation.
Cools, M; De Pauw, M; Kerstens, R; Rykx, A; Sloots, CE, 2010
)
1.39
"Prucalopride is an important addition to the therapeutic abilities for treating chronic constipation, especially in females poorly responding to laxatives. "( Prucalopride: evaluation of the pharmacokinetics, pharmacodynamics, efficacy and safety in the treatment of chronic constipation.
Corsetti, M; Tack, J, 2012
)
3.26
"Prucalopride is a novel, selective serotonin(4) receptor agonist with enterokinetic properties."( 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.
Coremans, G; De Pauw, M; Kerstens, R; Stevens, M, 2003
)
2.48
"Prucalopride is a selective 5-hydroxytryptamine type 4 (5-HT4) receptor agonist developed for the treatment of gastrointestinal disorders. "( Electrophysiological effects of prucalopride, a novel enterokinetic agent, on isolated atrial myocytes from patients treated with beta-adrenoceptor antagonists.
Kane, KA; Pau, D; Rankin, AC; Workman, AJ, 2005
)
2.05
"Prucalopride is a gastrointestinal prokinetic drug that acts through 5-HT4 receptors, but its potential effects on cardiac atrial function are unknown. "( Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants.
Brattelid, T; Kaumann, AJ; Krobert, KA; Levy, FO, 2005
)
3.21
"Prucalopride (R093877) is a selective and specific 5HT4 agonist, the first of a new chemical class of benzofurans, with gastrointestinal prokinetic activities in vitro."( Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans.
Bouras, EP; Burton, DD; Camilleri, M; McKinzie, S, 1999
)
1.98
"Prucalopride (PR) is a novel 5-HT4 agonist enterokinetic compound."( Effect of prucalopride, a new enterokinetic agent, on gastrointestinal transit and anorectal function in healthy volunteers.
Felt-Bersma, RJ; Meuwissen, SG; Poen, AC; Van Dongen, PA, 1999
)
2.15
"Prucalopride (PRU) is a selective benzofuran 5-hydroxytryptamine(4)-receptor agonist with gastrointestinal and colonic prokinetic activities. "( Prucalopride accelerates gastrointestinal and colonic transit in patients with constipation without a rectal evacuation disorder.
Bouras, EP; Burton, DD; Camilleri, M; McKinzie, S; Thomforde, G; Zinsmeister, AR, 2001
)
3.2
"Prucalopride is a selective and specific 5-hydroxytryptamine(4) receptor agonist that is known to increase stool frequency and to accelerate colonic transit."( The effects of the specific 5HT(4) receptor agonist, prucalopride, on colonic motility in healthy volunteers.
Akkermans, LM; Andriesse, GI; De Schryver, AM; Gooszen, HG; Samsom, M; Smout, AJ, 2002
)
2.01
"Prucalopride is a highly selective, specific, serotonin4 receptor agonist with enterokinetic properties."( Effects of prucalopride on colonic transit, anorectal function and bowel habits in patients with chronic constipation.
De Pauw, M; Felt-Bersma, RJ; Kerstens, R; Meuwissen, SG; Poen, AC; Sloots, CE; Stevens, M; Van Oene, JC, 2002
)
1.43
"Prucalopride is a novel, highly selective, specific serotonin4 receptor agonist with enterokinetic properties."( Efficacy and tolerability of prucalopride in patients with constipation due to spinal cord injury.
De Pauw, M; Gandrup, P; Jensen, MB; Kerstens, R; Krogh, K; Laurberg, S; Nilsson, J, 2002
)
1.33

Effects

Prucalopride is effective, has a good safety profile, and is well tolerated for the treatment of men with chronic constipation. It has a stimulatory effect on gastrointestinal motility and transit, as established by in vivo and in vitro studies.

Prucalopride has been used in adults with gastroparesis, accelerating gastric emptying. It has no major effect on the number of propagating contractions but increases HAPCs amplitude (p = 0.01).

ExcerptReferenceRelevance
"Prucalopride is effective, has a good safety profile, and is well tolerated for the treatment of men with chronic constipation."( A randomized, double-blind, placebo-controlled, phase 3 trial to evaluate the efficacy, safety, and tolerability of prucalopride in men with chronic constipation.
Bouchoucha, M; Dina, I; Etherson, K; Filip, R; Gabalec, L; Kerstens, R; Levine, A; Piessevaux, H; Schiefke, I; Stephenson, D; Yiannakou, Y, 2015
)
2.07
"Prucalopride has a stimulatory effect on gastrointestinal motility and transit, as established by in vivo and in vitro studies in animals and humans."( Prucalopride: a new drug for the treatment of chronic constipation.
Tack, J, 2009
)
2.52
"Prucalopride has been used in adults with gastroparesis, accelerating gastric emptying. "( A case report of prucalopride treatment in pediatric gastroparesis: a novel therapy.
Escobar-Serna, DP; Peralta-Palmezano, FJ; Peralta-Palmezano, JJ, 2022
)
2.5
"Prucalopride has no major effect on the number of propagating contractions but increases HAPCs amplitude (p = 0.01)."( High-resolution manometry reveals different effect of polyethylene glycol, bisacodyl, and prucalopride on colonic motility in healthy subjects: An acute, open label, randomized, crossover, reader-blinded study with potential clinical implications.
Corsetti, M; Deloose, E; Demedts, I; Harris, A; Pagliaro, G; Tack, J; Thys, A, 2021
)
1.56
"Prucalopride is effective, has a good safety profile, and is well tolerated for the treatment of men with chronic constipation."( A randomized, double-blind, placebo-controlled, phase 3 trial to evaluate the efficacy, safety, and tolerability of prucalopride in men with chronic constipation.
Bouchoucha, M; Dina, I; Etherson, K; Filip, R; Gabalec, L; Kerstens, R; Levine, A; Piessevaux, H; Schiefke, I; Stephenson, D; Yiannakou, Y, 2015
)
2.07
"Prucalopride has a stimulatory effect on gastrointestinal motility and transit, as established by in vivo and in vitro studies in animals and humans."( Prucalopride: a new drug for the treatment of chronic constipation.
Tack, J, 2009
)
2.52

Actions

Prucalopride promotes secondary peristalsis by stimulating 5-hydroxytrypatamine 4 receptors in the esophagus. It also promotes a significant neuroprotection against oxidative-mediated proapoptotic mechanisms.

ExcerptReferenceRelevance
"Prucalopride did not cause relevant inhibition of 5-HT(2A), 5-HT(2B), or 5-HT(3), motilin or cholecystokinin (CCK(1)) receptor-mediated contractions, nor nicotinic or muscarinic acetylcholine receptor-mediated contractions, up to 10 microM."( The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
Bosmans, JP; Briejer, MR; Heylen, L; Jurzak, M; Leysen, JE; Prins, NH; Schuurkes, JA; Van Daele, P, 2001
)
1.3
"Prucalopride promotes secondary peristalsis by stimulating 5-hydroxytrypatamine 4 receptors in the esophagus."( Influence of prucalopride on esophageal secondary peristalsis in reflux patients with ineffective motility.
Chen, CL; Hung, JS; Lei, WY; Liu, TT; Yi, CH, 2018
)
1.57
"Prucalopride promotes a significant neuroprotection against oxidative-mediated proapoptotic mechanisms."( Prucalopride exerts neuroprotection in human enteric neurons.
Bazzoli, F; Bianco, F; Bonora, E; Boschetti, E; Clavenzani, P; De Giorgio, R; Giancola, F; Mazzoni, M; Natarajan, D; Seri, M; Stanghellini, V; Sternini, C; Thapar, N; Torresan, F; Vargiolu, M; Volta, U, 2016
)
2.6
"Prucalopride seems to increase prolactin levels."( Prucalopride. In chronic constipation: poorly documented risks.
, 2011
)
2.53

Treatment

Prucalopride treatment resulted in a mean bowel movement frequency of 6.8/week, normal stool consistency, and reduced frequency of fecal incontinence. Treatment was significantly as-sociated with diarrhea, headache, and nausea (p<0.001), but not with abdominal pain.

ExcerptReferenceRelevance
"Prucalopride treatment also ameliorated intestinal barrier impairment and increased IL-6 release in PD model mice."( Protective effects of prucalopride in MPTP-induced Parkinson's disease mice: Neurochemistry, motor function and gut barrier.
Cui, C; Hong, H; Huang, SB; Jia, XB; Qiao, CM; Shen, YQ; Shi, Y; Wu, J; Yao, L; Zhao, WJ; Zhou, Y, 2021
)
1.66
"Prucalopride treatment resulted in a mean bowel movement frequency of 6.8/week, normal stool consistency, and reduced frequency of fecal incontinence."( Oral prucalopride in children with functional constipation.
Ausma, J; Benninga, MA; Di Lorenzo, C; Gilger, MA; Hoppenbrouwers, M; Hyman, PE; Kearns, GL; Vandeplassche, L; Winter, HS, 2013
)
1.63
"Prucalopride treatment for 8 weeks demonstrated an apparent favorable efficacy and tolerability profile in children with functional constipation."( Oral prucalopride in children with functional constipation.
Ausma, J; Benninga, MA; Di Lorenzo, C; Gilger, MA; Hoppenbrouwers, M; Hyman, PE; Kearns, GL; Vandeplassche, L; Winter, HS, 2013
)
1.63
"Prucalopride treatment was significantly as-sociated with diarrhea, headache, and nausea (p<0.001), but not with abdominal pain, compared with placebo."( Factors predictive of treatment-emergent adverse events of prucalopride: an integrated analysis of four randomized, double-blind, placebo-controlled trials.
Choi, SC; Ke, M; Kim, JY; Leelakusolvong, S; Liu, A; Quigley, EM; Tack, J; Zou, D, 2015
)
1.38
"Prucalopride-treated patients also achieved significantly greater satisfaction with treatment and bowel function, and improved perception of constipation severity and constipation-related QoL, compared with placebo."( 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.
Ausma, J; Kerstens, R; Quigley, EM; Vandeplassche, L, 2009
)
1.3
"Treatment with prucalopride accelerated CTT in these individuals."( Prucalopride improves bowel function and colonic transit time in patients with chronic constipation: an integrated analysis.
Cools, M; Emmanuel, A; Kerstens, R; Vandeplassche, L, 2014
)
2.18

Toxicity

Among 1,750 patients with CIC who received prucalopride (2-4 mg) in 5 phase 3 studies, no trends in CV adverse events, electrocardiogram parameters, or blood pressure were documented.

ExcerptReferenceRelevance
" Most frequent treatment-related adverse events were headache, abdominal pain, nausea and diarrhoea (mainly during day 1)."( 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.
Ausma, J; Kerstens, R; Quigley, EM; Vandeplassche, L, 2009
)
0.58
" Adverse events, vital signs, ECG, Holter monitor and pharmacokinetics were assessed (Clinicaltrials."( Safety assessment of prucalopride in elderly patients with constipation: a double-blind, placebo-controlled study.
Beyens, G; Camilleri, M; Kerstens, R; Robinson, P; Vandeplassche, L, 2009
)
0.67
" Secondary endpoints [proportion of patients with ≥ 3 SCBM/week, weekly frequency of (SC)BM, severity of constipation, and efficacy of treatment], adverse events (AEs), and safety parameters were also monitored."( Efficacy and safety of prucalopride in patients with chronic noncancer pain suffering from opioid-induced constipation.
Cools, M; De Pauw, M; Kerstens, R; Rykx, A; Sloots, CE, 2010
)
0.67
"In this population with OIC, prucalopride improved bowel function and was safe and well tolerated."( Efficacy and safety of prucalopride in patients with chronic noncancer pain suffering from opioid-induced constipation.
Cools, M; De Pauw, M; Kerstens, R; Rykx, A; Sloots, CE, 2010
)
0.96
" We present the case of a 61-year-old woman, who developed such adverse effects when given prucalopride for the treatment for chronic constipation."( Neurological and psychiatric adverse events with prucalopride: case report and possible mechanisms.
Antoniazzi, S; Carnovale, C; Clementi, E; Nisic, A; Pellegrino, P; Perrone, V; Pozzi, M; Radice, S, 2013
)
0.86
" The absence of other similar reports suggests that prucalopride rarely causes these adverse effects."( Neurological and psychiatric adverse events with prucalopride: case report and possible mechanisms.
Antoniazzi, S; Carnovale, C; Clementi, E; Nisic, A; Pellegrino, P; Perrone, V; Pozzi, M; Radice, S, 2013
)
0.89
"This integrated analysis aimed to identify the factors associated with the most frequently re-ported treatment-emergent adverse events (TEAEs) in Asian and non-Asian patients with chronic constipation (CC) who receive prucalopride or placebo over 12 weeks."( Factors predictive of treatment-emergent adverse events of prucalopride: an integrated analysis of four randomized, double-blind, placebo-controlled trials.
Choi, SC; Ke, M; Kim, JY; Leelakusolvong, S; Liu, A; Quigley, EM; Tack, J; Zou, D, 2015
)
0.85
"This observational population-based cohort study (EUPAS9200) conducted in five data sources (three in the UK, one in Sweden, and one in Germany [which was subsequently excluded from the pooled analyses]) aimed to estimate the pooled adjusted incidence rate ratio for major adverse cardiovascular events (defined as hospitalization for non-fatal acute myocardial infarction or stroke, and in-hospital cardiovascular death) in adult initiators of prucalopride compared with initiators of polyethylene glycol 3350 (PEG) following a common protocol."( Cardiovascular Safety of Prucalopride in Patients with Chronic Constipation: A Multinational Population-Based Cohort Study.
Andrews, EB; Cainzos-Achirica, M; Cantero, OF; Flynn, RWV; Fortuny, J; Garcia-Rodriguez, L; Gilsenan, A; Harding, A; Karlsson, P; Kollhorst, B; Linnér, L; MacDonald, TM; Odsbu, I; Plana, E; Ruigómez, A; Schink, T; Ziemiecki, R, 2019
)
0.98
"00 for major adverse cardiovascular events in patients with chronic constipation using prucalopride as compared with PEG."( Cardiovascular Safety of Prucalopride in Patients with Chronic Constipation: A Multinational Population-Based Cohort Study.
Andrews, EB; Cainzos-Achirica, M; Cantero, OF; Flynn, RWV; Fortuny, J; Garcia-Rodriguez, L; Gilsenan, A; Harding, A; Karlsson, P; Kollhorst, B; Linnér, L; MacDonald, TM; Odsbu, I; Plana, E; Ruigómez, A; Schink, T; Ziemiecki, R, 2019
)
1.04
" During administration of the medication, there were 18 adverse events in 6 subjects in the test formulation group and 19 cases of adverse events in 6 subjects in the reference formulation group (P > ."( Pharmacokinetics, Bioequivalence, and Safety Studies of Prucalopride in Healthy Chinese Subjects.
Chen, H; Huang, X; Wang, C; Xia, Y; Yu, C; Yu, X; Zhang, D; Zhang, X; Zheng, X; Zhou, Z, 2020
)
0.8
" The primary safety outcome was major adverse cardiovascular events (MACE), a composite of hospitalization for acute myocardial infarction, stroke, or in-hospital cardiovascular death."( Identification and Validation of Major Cardiovascular Events in the United Kingdom Data Sources Included in a Multi-database Post-authorization Safety Study of Prucalopride.
Andrews, EB; Cainzos-Achirica, M; Flynn, RWV; Fortuny, J; Garcia-Rodriguez, L; Gilsenan, A; MacDonald, TM; Plana, E; Ruigómez, A; Ziemiecki, R, 2021
)
0.82
" The baseline characteristics, adverse events (AEs), and seven-point scale of Clinical Global Impression-Improvement were collected."( Safety/Efficacy of Prucalopride in Korean Patients with Chronic Constipation: Post-marketing Surveillance.
Choi, CH; Choi, MG; Chung, WC; Jeon, SW; Kim, SY; Park, SJ; Yeon, SE, 2021
)
0.95
" Among 1,750 patients with CIC who received prucalopride (2-4 mg) in 5 phase 3 studies, no trends in CV adverse events, electrocardiogram parameters, or blood pressure were documented; ≤1."( A Review of the Cardiovascular Safety of Prucalopride in Patients With Chronic Idiopathic Constipation.
Boules, M; Derakhchan, K; Gabriel, A; Kowey, PR; Kreidieh, B; Spalding, W; Tack, J; Terreri, B; Youssef, A, 2023
)
1.44
" Adverse events, electrocardiogram, and other laboratory parameters were monitored at different time intervals."( Efficacy and safety analysis of prucalopride in refractory chronic constipation cases in a tertiary care hospital in Eastern India: A randomized, single-blind, placebo-controlled study.
Das, HS; Dehury, S; Goutam, S; Kaushik, C; Mohapatra, S,
)
0.41
" The most common adverse events reported from both the groups were headache, nausea, bloating, and diarrhea."( Efficacy and safety analysis of prucalopride in refractory chronic constipation cases in a tertiary care hospital in Eastern India: A randomized, single-blind, placebo-controlled study.
Das, HS; Dehury, S; Goutam, S; Kaushik, C; Mohapatra, S,
)
0.41

Pharmacokinetics

Co-administration of prucalopride with an oral contraceptive did not result in any clinically meaningful pharmacokinetic interactions and was well tolerated. Compared to females, males exhibited a slightly lower exposure of the drug but similar changes of bowel habits were observed in both genders.

ExcerptReferenceRelevance
"78 ng/ml with a median time to Cmax (tmax) of 2 hours and resulted in an area under concentration-time curve (AUC0-∞) of 89."( Pharmacokinetics of single and repeated oral doses prucalopride in healthy Chinese volunteers.
Chen, X; Hu, P; Jiang, J; Liu, H; Liu, T; Zhong, W, 2012
)
0.63
" Compared to females, males exhibited a slightly lower exposure of prucalopride but similar changes of bowel habits were observed in both genders suggesting the inter-gender pharmacokinetic differences are not clinically relevant."( Pharmacokinetics of single and repeated oral doses prucalopride in healthy Chinese volunteers.
Chen, X; Hu, P; Jiang, J; Liu, H; Liu, T; Zhong, W, 2012
)
0.87
"Co-administration of prucalopride with an oral contraceptive did not result in any clinically meaningful pharmacokinetic interactions and was well tolerated."( Effect of prucalopride on the pharmacokinetics of oral contraceptives in healthy women.
Ausma, J; Boterman, M; Hoppenbrouwers, M; Van de Velde, V; Vandeplassche, L, 2013
)
1.11
" The aim of this study was to investigate the pharmacokinetic properties and excretion of prucalopride in healthy individuals, using a microtracer approach with (14)C radioactivity detection using liquid scintillation counting and accelerator mass spectrometry."( A Phase I Study to Investigate the Absorption, Pharmacokinetics, and Excretion of [(14)C]Prucalopride After a Single Oral Dose in Healthy Volunteers.
Ding, J; Dragone, J; Flach, S; Getsy, J; Pankratz, T; Pennick, M; Scarfe, G; Seymour, M; Troy, S, 2016
)
0.88
"The objectives of the present study were to evaluate the bioequivalence of 2 tablet formulations of prucalopride, generic and branded, and to investigate relevant pharmacokinetic and safety profiles."( Pharmacokinetics, Bioequivalence, and Safety Studies of Prucalopride in Healthy Chinese Subjects.
Chen, H; Huang, X; Wang, C; Xia, Y; Yu, C; Yu, X; Zhang, D; Zhang, X; Zheng, X; Zhou, Z, 2020
)
1.02

Bioavailability

ExcerptReferenceRelevance
"Prucalopride was well absorbed and excreted mainly by the kidneys, including both passive and active transporter mechanisms."( A Phase I Study to Investigate the Absorption, Pharmacokinetics, and Excretion of [(14)C]Prucalopride After a Single Oral Dose in Healthy Volunteers.
Ding, J; Dragone, J; Flach, S; Getsy, J; Pankratz, T; Pennick, M; Scarfe, G; Seymour, M; Troy, S, 2016
)
2.1
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

There was no additional benefit with the 4 mg/day over the 2mg/day dosage of prucalopride. Colonic pressures were recorded in 10 healthy subjects.

ExcerptRelevanceReference
"After 1 week of dosing (prucalopride or placebo in a double-blind, randomized, crossover fashion), colonic pressures were recorded in 10 healthy subjects using a solid-state pressure catheter with six sensors spaced 10 cm apart."( The effects of the specific 5HT(4) receptor agonist, prucalopride, on colonic motility in healthy volunteers.
Akkermans, LM; Andriesse, GI; De Schryver, AM; Gooszen, HG; Samsom, M; Smout, AJ, 2002
)
0.87
" There was no additional benefit with the 4 mg/day over the 2 mg/day dosage of prucalopride."( Prucalopride.
Frampton, JE, 2009
)
2.02
" Dosing information is however needed to establish its actual clinical efficacy and its proper effects on the large bowel in these animals."( Effects of Single-Dose Prucalopride on Intestinal Hypomotility in Horses: Preliminary Observations.
Bassotti, G; Faillace, V; Fettucciari, K; Fratini, M; Laus, F; Paggi, E; Spaterna, A; Tesei, B, 2017
)
0.77
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzamides
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency24.64280.002541.796015,848.9004AID1347395; AID1347397; AID1347398
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
GLI family zinc finger 3Homo sapiens (human)Potency0.74980.000714.592883.7951AID1259369
EWS/FLI fusion proteinHomo sapiens (human)Potency36.20920.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
farnesoid X nuclear receptorHomo sapiens (human)Potency13.33220.375827.485161.6524AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency33.49150.005428.02631,258.9301AID1346982
GVesicular stomatitis virusPotency2.45450.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency3.46710.00108.379861.1304AID1645840
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency2.45450.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.45450.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.45450.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.45450.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki3.98110.00000.887110.0000AID416399
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki3.98110.00000.74119.9000AID416399
5-hydroxytryptamine receptor 4Homo sapiens (human)Ki0.28000.00000.443910.0000AID416400; AID6272; AID6273
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 3A4Homo sapiens (human)EC50 (µMol)0.00520.00010.23283.2000AID1264125
5-hydroxytryptamine receptor 4Homo sapiens (human)EC50 (µMol)0.01210.00060.08791.1220AID1264125; AID1375752; AID1375782
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)EC50 (µMol)0.02600.00870.04570.1023AID1264225
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (79)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
maintenance of gastrointestinal epithelium5-hydroxytryptamine receptor 4Homo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 4Homo sapiens (human)
mucus secretion5-hydroxytryptamine receptor 4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
large intestinal transit5-hydroxytryptamine receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 4Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 4Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 4Homo sapiens (human)
serotonin receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 4Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 4Homo sapiens (human)
endosome5-hydroxytryptamine receptor 4Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
membrane5-hydroxytryptamine receptor 4Homo sapiens (human)
synapse5-hydroxytryptamine receptor 4Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 4Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (83)

Assay IDTitleYearJournalArticle
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID624236Agonists at Human 5-Hydroxytryptamine receptor 5-HT42001European journal of pharmacology, Jun-29, Volume: 423, Issue:1
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
AID1346953Human 5-HT4 receptor (5-Hydroxytryptamine receptors)2001European journal of pharmacology, Jun-29, Volume: 423, Issue:1
The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.
AID624236Agonists at Human 5-Hydroxytryptamine receptor 5-HT42000Journal of neurochemistry, Feb, Volume: 74, Issue:2
Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
AID1346953Human 5-HT4 receptor (5-Hydroxytryptamine receptors)2000Journal of neurochemistry, Feb, Volume: 74, Issue:2
Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1375783Agonist activity at 5-HT4E receptor (unknown origin) relative to 5-HT2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1264125Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID706218Agonist activity at 5HT4 receptor in rat oesophagus assessed as reversal of carbamylcholine-induced contraction at 10 uM incubated at 7 mins post carbamylcholine-challenge measured after 30 mins relative to 5HT2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
AID1375753Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay relative to 5-HT2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID706215Agonist activity at rat 5HT4E receptor expressed in HEK293 cells relative to 5HT2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
AID6273Tested for selectivity for 5-hydroxytryptamine 4 receptor2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
5-HT4 receptor ligands: applications and new prospects.
AID1375760Ratio of drug level in Wistar rat brain to plasma at 10 mg/kg, po measured at 1 hr by LC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID416400Binding affinity at 5HT4 receptor2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1375752Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1264126Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay relative to 5-HT2015European journal of medicinal chemistry, Oct-20, Volume: 103Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.
AID1375758AUC in Wistar rat at 3 mg/kg, po or 1 mg/kg, iv by LC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID706211Receptor occupancy of 5HT4 receptor in Sprague-Dawley rat brain at 10 mg/kg, sc at 1 hr2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
AID1375774In vivo partial agonist activity at 5-HT4 receptor in C57BL/6J mouse assessed as increase in cortical sAPPalpha levels at 10 mg/kg, sc after 60 to 90 mins by ELISA relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1375757Cmax in Wistar rat at 3 mg/kg, po or 1 mg/kg, iv by LC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1375755Drug metabolism in human liver microsomes after 30 mins by LC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID706217Agonist activity at rat 5HT4L receptor expressed in HEK293 cells relative to 5HT2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
AID706212Procognitive activity in Sprague-Dawley rat assessed as increase in acetylcholine level in prefrontal cortex at 10 mg/kg, sc after 3 hrs by brain microdialysis relative to control2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1375782Agonist activity at 5-HT4E receptor (unknown origin)2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1375754Drug metabolism in rat liver microsomes after 30 mins by LC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID706216Agonist activity at rat 5HT4S receptor expressed in HEK293 cells relative to 5HT2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
AID1375756Oral bioavailability in Wistar rat at 3 mg/kg by LC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID416399Binding affinity at 5HT3 receptor2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.
AID6272Tested for agonist activity against 5-hydroxytryptamine 4 receptor2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
5-HT4 receptor ligands: applications and new prospects.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1264225Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay2015European journal of medicinal chemistry, Oct-20, Volume: 103Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.
AID1375759Clearance in Wistar rat at 1 mg/kg, iv by LC-MS/MS method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HT
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1264226Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay relative to 5-HT2015European journal of medicinal chemistry, Oct-20, Volume: 103Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (231)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (0.87)18.2507
2000's51 (22.08)29.6817
2010's137 (59.31)24.3611
2020's41 (17.75)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 94.11

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index94.11 (24.57)
Research Supply Index5.69 (2.92)
Research Growth Index5.68 (4.65)
Search Engine Demand Index167.04 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (94.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials57 (23.95%)5.53%
Reviews46 (19.33%)6.00%
Case Studies10 (4.20%)4.05%
Observational1 (0.42%)0.25%
Other124 (52.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (63)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Prucalopride (Resolor) Tablets in Participants With Chronic Constipation [NCT01116206]Phase 3507 participants (Actual)Interventional2010-05-31Completed
The Effect of a Single Dose of Prucalopride on Emotional Processing in Healthy Volunteers [NCT03863366]41 participants (Actual)Interventional2017-02-07Completed
A Study to Evaluate the Long-Term Tolerability and Safety of Oral Prucalopride Administered to Patients With Chronic Constipation [NCT01070615]Phase 3693 participants (Actual)Interventional1998-06-30Completed
Optimization of the Bowel Preparation Regimen for Colon Capsule Endoscopy Procedure [NCT05726097]Phase 3147 participants (Anticipated)Interventional2023-02-01Recruiting
Double-dummy, Double-blind, Randomised, Parallel Group, Controlled Comparative Study of Polyethylene Glycol (PEG)Plus Electrolytes Versus Prucalopride in Females With Chronic Constipation Who Failed Adequate Relief With Laxatives [NCT01251822]Phase 3240 participants (Actual)Interventional2010-11-30Completed
The Effect of 2mg Sub-acute Prucalopride on Cognition and Emotional Processing in Participants Recovered From Depression [NCT05220228]Early Phase 150 participants (Anticipated)Interventional2022-01-04Recruiting
A Placebo-controlled Trial With Prucalopride for the Treatment of Typical Reflux Symptoms in Patients With Gastro-esophageal Reflux Disease With Incomplete Proton Pump Inhibitor Response [NCT03676374]Phase 460 participants (Anticipated)Interventional2019-02-18Recruiting
Prucalopride Versus Placebo in Gastroparesis: Randomized Placebo-controlled Crossover Trial [NCT02031081]Phase 2/Phase 315 participants (Actual)Interventional2014-03-31Completed
A Multicenter, Single-Arm, Interventional, Phase 4 Study to Evaluate the Efficacy and Safety of Prucalopride in Combination With PEG or Lactulose in Women With Chronic Constipation (CC) [NCT02228616]Phase 4280 participants (Actual)Interventional2014-10-14Completed
Evaluation of Pharmacokinetics, Safety and Tolerability of a Single Dose of Prucalopride, in Subjects With Moderate and Severe Hepatic Impairment, in Comparison With Healthy Subjects [NCT01134185]Phase 124 participants (Actual)Interventional2010-05-31Completed
A Double-Blind, Placebo-Controlled, Two-Way Cross-Over in Healthy Volunteers, to Evaluate the Pharmacokinetics, Tolerability and Cardiac Safety of Prucalopride at Steady-State [NCT00793429]Phase 10 participants InterventionalCompleted
The Effect of Prucalopride on Small Bowel Transit Time in Patients Undergoing Capsule Endoscopy: A Randomized Controlled Trial [NCT02806206]Phase 4122 participants (Anticipated)Interventional2016-07-31Not yet recruiting
The Effect of Prucalopride (Resolor®) on Gastric Motor Function and Gastric Sensitivity [NCT04429802]17 participants (Actual)Interventional2013-09-26Completed
A Randomized, Double-blind/Open-label, Placebo/Active-controlled, Single/Multiple Dose, Parallel, Phase 1/2a Trial to Evaluate the Safety, Tolerability, PK , PD of YH12852 in Healthy Subjects and Patients With Functional Constipation [NCT02538367]Phase 1/Phase 2120 participants (Actual)Interventional2015-08-31Completed
Phase 3, Multicenter, Randomized Study With 2 Different Doses of Prucalopride Administered to Male and Female Pediatric Subjects Aged 6 Months to 17 Years With Functional Constipation, Consisting of a 12-week Double-blind, Placebo-controlled Part (Part A) [NCT04759833]Phase 3175 participants (Actual)Interventional2021-08-02Terminated(stopped due to Data Monitoring Committe (DMC) decision; terminated due to futility, with no safety concerns; FDA agreement to terminate the study.)
The Effect of Prucalopride on the Plasma Levels of Oral Contraceptives (Ethinylestradiol and Norethisterone) in Healthy Subjects [NCT01036893]Phase 116 participants (Anticipated)Interventional2009-12-31Completed
A Double-Blind Placebo-Controlled Dose-Finding Trial to Evaluate the Efficacy and Safety of R093877 in Patients With Chronic Idiopathic Constipation [NCT00617513]Phase 2174 participants (Actual)Interventional1995-03-31Completed
A 12-week, Randomised, Double-blind, Placebo-controlled Trial to Evaluate the Efficacy, Quality of Life, Safety and Tolerability of Prucalopride in Male Subjects With Chronic Constipation [NCT01147926]Phase 3374 participants (Actual)Interventional2010-09-23Completed
A Double-Blind, Placebo-Controlled, Dose-Finding Trial to Evaluate the Efficacy and Safety of Prucalopride (R093877) in Subjects With Chronic Idiopathic Constipation [NCT00596596]Phase 2313 participants (Actual)Interventional1996-09-30Completed
A Phase I Thorough QT/QTc Study To Evaluate The Effect of Therapeutic and Supratherapeutic Multiple Doses of Prucalopride on Cardiac Repolarisation in Healthy Male and Female Volunteers [NCT00903747]Phase 1120 participants (Actual)Interventional2009-01-31Completed
A Study to Evaluate the Long-Term Tolerability, Safety, Patient Satisfaction, Pharmacokinetics, and Use Patterns of Oral Prucalopride Tablets in Patients With Chronic Constipation [NCT00987844]Phase 31,775 participants (Actual)Interventional1998-07-31Completed
A Double-Blind, Placebo-Controlled Trial to Evaluate the Safety and Tolerability of Oral Once-Daily Prucalopride (R108512) Solution in Constipated Elderly Subjects Living in a Nursing Facility [NCT00627692]Phase 2100 participants (Actual)Interventional1999-02-28Completed
Prucalopride + Prucalopride Booster vs. Prucalopride + Picosalax Booster for the Colon Capsule [NCT01864915]Phase 360 participants (Actual)Interventional2013-06-30Completed
The Colonic Transit Time: a Modifiable Determinant of Intestinal Production and Uptake of Microbial Metabolites? [NCT01869751]0 participants (Actual)Observational2013-05-31Withdrawn(stopped due to failure to recruit patients)
A Randomized, Double-blind, Placebo/Active-controlled, Single/Multiple Dose Phase 1 Clinical Study to Investigate the Safety/Tolerability and PK/PD of YH12852 After Oral Administration in Healthy Subjects [NCT01870674]Phase 1127 participants (Actual)Interventional2013-08-31Completed
Health Related Quality of Life in Female Patients With Chronic Constipation [NCT01902537]150 participants (Actual)Observational2012-08-31Completed
A Randomized, Controlled, Double-blind Efficacy and Tolerability Study Of Prucalopride For The Treatment Of Postoperative Ileus In Patients Undergoing Gastrointestinal Surgery [NCT02004652]Phase 2110 participants (Actual)Interventional2013-11-30Completed
A 12-week, Randomised, Double-blind, Placebo-controlled Trial to Evaluate the Efficacy and Safety of Prucalopride in Subjects With Chronic Non-cancer Pain Suffering From Opioid Induced Constipation [NCT01117051]Phase 3174 participants (Actual)Interventional2010-05-19Terminated(stopped due to The study was stopped by the sponsor based on a non-safety related business priority decision)
A Two-Period, Double-Blind, Placebo-Controlled Trial to Evaluate the Effects of re-Treatment of Prucalopride on Efficacy and Safety in Subjects With Chronic Constipation. [NCT00598338]Phase 3516 participants (Actual)Interventional1999-04-30Completed
[NCT02781493]Phase 4600 participants (Anticipated)Interventional2016-06-30Not yet recruiting
A Phase 1 Study to Investigate the Absorption, Metabolism, and Excretion of [14C] Prucalopride Succinate Following a Single Oral Dose in Healthy Male Subjects [NCT01807000]Phase 16 participants (Actual)Interventional2013-03-18Completed
Study to Evaluate the Effect of a 1 mg o.d. Dose of Prucalopride in Patients With Chronic Idiopathic Constipation [NCT00575614]Phase 287 participants (Actual)Interventional1997-04-30Completed
A Double-Blind, Placebo-Controlled Trial to Evaluate the Efficacy and Safety of R093877 in Patients With Severe Chronic Constipation [NCT00576511]Phase 253 participants (Actual)Interventional1994-12-31Completed
A Double-Blind, Placebo-Controlled Trial to Evaluate the Effect of Dose-Titration on the Safety and Efficacy and R108512 Tablets in Subjects With Chronic Constipation [NCT00577018]Phase 3755 participants (Actual)Interventional1998-08-31Completed
An Open-label, Randomised, Crossover, Reader Blinded, Study to Compare the Effect of Polyethylene Glycol 3350, Bisacodyl and Prucalopride on Colonic Motility Assessed With Intraluminal Colonic Manometry in Healthy Subjects [NCT03279341]Phase 410 participants (Actual)Interventional2012-12-03Completed
A Double-Blind, Placebo-Controlled Trial to Evaluate the Efficacy, Safety and Quality-of-Life of R108512 Tablets in Elderly Subjects With Chronic Constipation [NCT00487422]Phase 3303 participants (Actual)Interventional1998-10-31Completed
A Randomized Double-blind Placebo Controlled Trial of Prucalopride to Reduce the Duration of Postoperative Ileus in Patients Undergoing Elective Colorectal Surgery [NCT02947269]Phase 3150 participants (Actual)Interventional2017-10-25Completed
An Open-label Follow-up Study of 0.01 mg/kg/Day to 0.03 mg/kg/Day Prucalopride (R108512) Oral Solution in Paediatric Subjects, Aged >= 4 to <= 12 Years With Functional Faecal Retention (FFR), Who Participated in the PRU-USA-12. [NCT01670669]Phase 137 participants (Actual)Interventional1998-11-30Completed
The Effect of Prucalopride Succinate on Gastrointestinal Motility After Laparoscopic Gastrectomy : Prospective Double Blind Case-control Study [NCT05966246]106 participants (Actual)Interventional2022-01-25Completed
A Double-blind, Placebo-controlled Trial to Evaluate the Efficacy and Safety of Prucalopride (R108512) Tablets in Subjects With Chronic Constipation. [NCT00483886]Phase 3620 participants (Actual)Interventional1998-04-30Completed
A Double-blind, Placebo-controlled Trial to Evaluate the Efficacy and Safety of Prucalopride (R108512) Tablets in Subjects With Chronic Constipation [NCT00488137]Phase 3716 participants (Actual)Interventional1998-03-31Completed
A Double-Blind, Placebo-Controlled, 2-Way Cross-Over Trial in Healthy Volunteers, to Evaluate the Pharmacokinetics, Tolerability and Cardiac Safety of Oral Prucalopride at Steady State, After up-Titration to a Maximum of 20 mg. [NCT00488215]Phase 132 participants (Actual)Interventional2000-01-31Completed
The Effect of Seven Day Prucalopride Administration on Emotional Processing in Healthy Volunteers [NCT03572790]50 participants (Actual)Interventional2018-06-11Completed
A Double-Blind Placebo-Controlled Dose-Finding Trial to Evaluate the Efficacy and Safety of R093877 in Patients With Chronic Idiopathic Constipation [NCT00631813]Phase 2253 participants (Actual)Interventional1995-11-30Completed
A Double-blind, Placebo-controlled Trial to Evaluate the Efficacy and Safety of R108512 Tablets in Subjects With Chronic Constipation [NCT00485940]Phase 3641 participants (Actual)Interventional1998-03-31Completed
A Randomised, Double-blind, Placebo-controlled Trial to Evaluate the Efficacy, Quality of Life, Safety and Tolerability of Long-term Treatment (24 Weeks) With Prucalopride in Subjects Aged ≥18 Years With Chronic Constipation [NCT01424228]Phase 4364 participants (Actual)Interventional2011-04-06Completed
Trial Consisting of an 8-week Double-blind Placebo-controlled Part to Evaluate Efficacy, Safety, Tolerability and Pharmacokinetics of Prucalopride in Paediatric Subjects With Functional Constipation, Aged ≥6 Months to <18 Years, Followed by a 16-week Open [NCT01330381]Phase 3215 participants (Actual)Interventional2011-04-28Completed
Improving Bowel Preparation for the Colon Capsule: Picosalax and Prucalopride vs. PEG and Prucalopride [NCT01655095]Phase 320 participants (Actual)Interventional2012-07-31Completed
A Study on the Safety and Effectiveness of Prucalopride in the Treatment of Chronic Constipation [NCT01692132]0 participants (Actual)Observational2013-02-28Withdrawn(stopped due to The company decided to cancel this study in conformity with PH FDA Circular 2013-004)
Single Dose Pharmacokinetic Trial of Oral Prucalopride (R093877) in Subjects With Mild, Moderate and Severe Renal Impairment [NCT01674192]Phase 134 participants (Actual)Interventional1997-07-31Completed
The Impact of Upper Gastrointestinal Dysmotility on Aspiration-associated Symptoms [NCT05455359]Phase 4120 participants (Anticipated)Interventional2022-07-18Not yet recruiting
The Effect of Prucalopride on Gastric Emptying in Intensive Care Unit Patients [NCT05496179]Phase 1/Phase 270 participants (Actual)Interventional2022-03-07Completed
Anti-inflammatory Effect of Pre-operative Stimulation of the Cholinergic Anti-Inflammatory Pathway: A Potential New Therapeutical Intervention for Postoperative Ileus [NCT02425774]Phase 430 participants (Anticipated)Interventional2014-07-31Recruiting
Treatment of Dysphagia and Ineffective Esophageal Motility With Prucalopride: A Pilot Study [NCT03244553]Phase 228 participants (Actual)Interventional2017-10-20Completed
Gastric Glitch: a New Functional Disease Treated With Prucalopride and Buspirone in a N-of-1 Double-blind Clinical Trial [NCT05377619]Phase 1/Phase 21 participants (Actual)Interventional2022-01-06Completed
Study of Comparative Effectiveness of Prucalopride and Lubiprostone in Constipation Predominant Irritable Bowel Syndrome [NCT04985669]Phase 4140 participants (Anticipated)Interventional2021-08-15Recruiting
A Single-dose Pharmacokinetic Trial of 0.03 mg/kg R108512 Solution in Paediatric Subjects, Aged >= 4 to <= 12 Years With Functional Faecal Retention (FFR). [NCT01674166]Phase 138 participants (Actual)Interventional1998-11-30Completed
An Open-label, Randomized, Crossover, Reader-blinded Study to Investigate the Effect of Prucalopride and Polyethylene Glycol 3350 on Colon Motility With Intramural Manometry in Subjects With Chronic Constipation [NCT01707667]Phase 413 participants (Actual)Interventional2013-02-27Completed
A Randomized Controlled Clinical Trial of Prucaloprude Succinate in Promoting the Recovery of Intestinal Function After Robot-assisted Laparoscopic Radical Cystectomy and Urinary Diversion [NCT05001763]Phase 2160 participants (Anticipated)Interventional2021-09-01Not yet recruiting
Prucalopride Versus Placebo in Functional Dyspepsia With Delayed Gastric Emptying [NCT02510976]Phase 430 participants (Anticipated)Interventional2011-11-30Recruiting
The Effects of Prucalopride in Patients With Constipation Predominant Irritable Bowel Syndrome: A Double Blind Placebo Controlled Trial [NCT04757493]Phase 2/Phase 3160 participants (Anticipated)Interventional2021-03-10Recruiting
Efficacy of Prucalopride in Critically Ill Patients With Paralytic Ileus; a Pilot Randomized Double-blind Controlled Trial [NCT04190173]Phase 362 participants (Anticipated)Interventional2017-07-01Recruiting
Effect Comparison of Electro-acupuncture and Prucalopride for Severe Chronic Constipation: a Multi-center Noninferiority Randomized Controlled Trial [NCT02047045]560 participants (Actual)Interventional2014-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01117051 (3) [back to overview]Percent of Subjects With an Average Frequency of >=3 Spontaneous Bowel Movements Per Week
NCT01117051 (3) [back to overview]Plasma Concentration of Prucalopride at Week 2
NCT01117051 (3) [back to overview]Plasma Concentration of Prucalopride at Week 8
NCT01147926 (14) [back to overview]Bisacodyl Tablets Taken Per Week
NCT01147926 (14) [back to overview]Days With Rescue Medication Taken Per Week
NCT01147926 (14) [back to overview]Percent of Subjects on the Subject Global Evaluation on Efficacy of Treatment Score Rating Treatment as Quite a Bit to Extremely Effective at Final On-Treatment Assessment
NCT01147926 (14) [back to overview]Percent of Subjects on the Subject Global Evaluation on Severity of Constipation Score Rating Constipation as Severe to Very Severe at Final On-Treatment Assessment
NCT01147926 (14) [back to overview]Percent of Subjects With an Improvement of ≥ 1 Point on the Patient Assessment of Constipation - Quality of Life (PAC-QOL) Total Score at Final On Treatment Assessment
NCT01147926 (14) [back to overview]Percent of Subjects With an Improvement of ≥ 1 Point on the Patient Assessment of Constipation - Symptom (PAC-SYM) Questionnaire Total Score at Final On Treatment Assessment
NCT01147926 (14) [back to overview]Percent SBM With Sensation of Complete Evacuation
NCT01147926 (14) [back to overview]Percentage of Subjects With an Average Weekly Frequency of at Least 3 SCBM Per Week and an Increase of ≥ 1 SCBM Per Week for ≥ 75% of the 12-week Treatment Period and ≥ 75% of the Last Third of the 12-week Treatment Period
NCT01147926 (14) [back to overview]Percentage of Subjects With an Increase of at Least 1 SCBM Per Week
NCT01147926 (14) [back to overview]SCBM Per Week
NCT01147926 (14) [back to overview]The Percentage of Subjects With an Average of ≥3 Spontaneous Complete Bowel Movements (SCBM) Per Week
NCT01147926 (14) [back to overview]Time to First SCBM After Investigational Product Intake on Day 1
NCT01147926 (14) [back to overview]Percent SBM With a Consistency of Normal and Hard/Very Hard
NCT01147926 (14) [back to overview]Percent SCBM With No Straining and Severe/Very Severe Straining
NCT01330381 (19) [back to overview]Efficacy of Treatment for Final On Treatment Assessment in Open-Label Treatment Period
NCT01330381 (19) [back to overview]Efficacy of Treatment for Final On Treatment Assessment in Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Convenience of Treatment for Final On Treatment Assessment in Open-Label Treatment Period
NCT01330381 (19) [back to overview]Time to First SBM in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Stool Consistency Per SBM Score in Children Without Diapers in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Stool Consistency Per SBM Score in Children With Diapers in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Percent of Subjects With Fecal Incontinence Episodes of 1 or Less Per 2 Weeks in the Last Four Weeks of the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Percent of Subjects With Bowel Frequency of 3 or More Spontaneous Bowel Movements (SBM) Per Week in the Last Four Weeks of the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Percent of Responders in the Last Four Weeks of the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Painful Bowel Movements Score in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Number of Retentive Posturing or Excessive Volitional Stool Retention in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Number of Rescue Medications Taken in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Large Diameter Stools in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Frequency of Toilet Training in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Change From Baseline in the Number of SBM Per Week Over the 8 Week Double Blind Treatment Period
NCT01330381 (19) [back to overview]Abdominal Pain Score in Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Number of SBM Per Week in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Severity of Constipation Over the Past 2 Weeks for the Final On Treatment Assessment in the Double-Blind Treatment Period
NCT01330381 (19) [back to overview]Severity of Constipation Over the Past 2 Weeks for the Final On Treatment Assessment in the Open-Label Treatment Period
NCT01424228 (17) [back to overview]Change From Baseline in Spontaneous Complete Bowel Movements Per Week at Up to 24 Weeks
NCT01424228 (17) [back to overview]Change From Baseline in Straining Per SCBM at Up to 24 Weeks
NCT01424228 (17) [back to overview]Change From Baseline in the Number of Bisacodyl Tablets Taken Per Week at Up to 24 Weeks
NCT01424228 (17) [back to overview]Change From Baseline in the Number of Days With Rescue Medication Taken Per Week at Up to 24 Weeks
NCT01424228 (17) [back to overview]Change From Baseline in the Patient Assessment of Constipation - Quality of Life (PAC-QOL) Score at Up to the Final On Treatment Assessment Value
NCT01424228 (17) [back to overview]Change From Baseline in the Patient Assessment of Constipation - Symptom (PAC-SYM) Questionnaire Score at Up to the Final On Treatment Assessment Value
NCT01424228 (17) [back to overview]Percentage of Subjects With an Increase of ≥1 Spontaneous Complete Bowel Movement (SCBM) Per Week Up to 24 Weeks
NCT01424228 (17) [back to overview]The Percentage of Subjects With an Average of ≥3 Spontaneous Complete Bowel Movements (SCBM) Per Week Over the 24 Week Treatment Period
NCT01424228 (17) [back to overview]Change From Baseline in Percent SCBM With a Consistency of Normal and Hard/Very Hard at Up to 24 Weeks
NCT01424228 (17) [back to overview]Change From Baseline in Average Consistency Per SCBM at Up to 24 Weeks
NCT01424228 (17) [back to overview]Change From Baseline in the Short Form-36 Health Survey (SF-36) Score at Up to the Final On Treatment Assessment Value
NCT01424228 (17) [back to overview]Percent of Subjects With an Average Weekly Frequency of at Least 3 SCBM by 4-Week Treatment Period
NCT01424228 (17) [back to overview]Percent of Subjects With an Average Weekly Frequency of at Least 3 SCBM by Week
NCT01424228 (17) [back to overview]Time to First SCBM After Investigational Product Intake on Day 1 and Day 28
NCT01424228 (17) [back to overview]Change From Baseline in Percent SCBM With No Straining and Severe/Very Severe Straining at Up to 24 Weeks
NCT01424228 (17) [back to overview]Average Number of Spontaneous Complete Bowel Movements (SCBM) Per Week Up to 24 Weeks
NCT01424228 (17) [back to overview]Change From Baseline in Percent SBM With Sensation of Complete Evacuation at Up to 24 Weeks
NCT01707667 (7) [back to overview]Propagation Velocity of HAPC
NCT01707667 (7) [back to overview]Duration of HAPC
NCT01707667 (7) [back to overview]Area Under the Concentration Curve (AUC) of All HAPCs
NCT01707667 (7) [back to overview]The Mean Amplitude of HAPC
NCT01707667 (7) [back to overview]The Number of High-Amplitude Propagating Contractions (HAPC)
NCT01707667 (7) [back to overview]Time to First HAPC
NCT01707667 (7) [back to overview]Motility Index
NCT01807000 (16) [back to overview]Percent Total Radioactivity Excreted in Stool of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Maximum Plasma Concentration (Cmax) of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Half-Life Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Half-Life Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Cmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Cmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]AUC 0→∞ Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]AUC 0→∞ Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC 0→∞) of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Total Body Clearance (CL/F) of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Tmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Tmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Time to Maximum Plasma Concentration (Tmax) of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Plasma Half-Life (T1/2) of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Volume of Distribution (Vz/F) of Radiolabelled Prucalopride Succinate
NCT01807000 (16) [back to overview]Percent Total Radioactivity Excreted in Urine of Radiolabelled Prucalopride Succinate
NCT02047045 (14) [back to overview]the Proportion of Overall CSBM Responders Over Weeks 1-8
NCT02047045 (14) [back to overview]the Proportion of Participants With ≥3 Mean Weekly CSBMs Over Weeks 3-8
NCT02047045 (14) [back to overview]the Proportion of Sustained CSBM Responder Over Weeks 1-8
NCT02047045 (14) [back to overview]Time to the First CSBMs
NCT02047045 (14) [back to overview]Average Dosage of Bisacodyl Used Weekly Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.
NCT02047045 (14) [back to overview]Average Dosage of Glycerine Enema Used Weekly Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.
NCT02047045 (14) [back to overview]Change From Baseline in Mean Score of Patient Assessment of Constipation Quality of Life
NCT02047045 (14) [back to overview]Mean Weekly CSBMs and Its Change From Baseline Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.
NCT02047045 (14) [back to overview]Mean Weekly SBMs and Its Change From Baseline Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.
NCT02047045 (14) [back to overview]Proportion of Patients Using Rescue Medicine Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.
NCT02047045 (14) [back to overview]the Change From Baseline in Mean Score of Stool Consistency for Each SBM Over Weeks 1-2 and 3-8.
NCT02047045 (14) [back to overview]the Change From Baseline in Mean Score of Straining for Each SBM Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.
NCT02047045 (14) [back to overview]the Proportion of Participants With ≥1 Increase in Mean Weekly CSBMs From Baseline Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.
NCT02047045 (14) [back to overview]the Proportion of Participants With ≥3 Mean Weekly CSBMs Over Weeks 1-2, 11-12, 15-16, 19-20, 31-32.

Percent of Subjects With an Average Frequency of >=3 Spontaneous Bowel Movements Per Week

A bowel movement (BM) was defined as spontaneous if no laxatives were taken in the 24 hours preceding that BM. (NCT01117051)
Timeframe: 12 weeks

Interventionpercentage of subjects (Number)
Placebo39.8
Prucalopride48.8

[back to top]

Plasma Concentration of Prucalopride at Week 2

(NCT01117051)
Timeframe: Week 2

Interventionng/ml (Mean)
pre-dose5 hours post-dose
Prucalopride2.8276.107

[back to top]

Plasma Concentration of Prucalopride at Week 8

(NCT01117051)
Timeframe: Week 8

Interventionng/ml (Mean)
pre-dose5 hours post-dose
Prucalopride3.1796.615

[back to top]

Bisacodyl Tablets Taken Per Week

(NCT01147926)
Timeframe: Over 12 week treatment period

InterventionTablets/week (Mean)
PLACEBO1.0
PRUCALOPRIDE0.6

[back to top]

Days With Rescue Medication Taken Per Week

(NCT01147926)
Timeframe: Over 12 week treatment period

InterventionDays/week (Mean)
PLACEBO0.6
PRUCALOPRIDE0.3

[back to top]

Percent of Subjects on the Subject Global Evaluation on Efficacy of Treatment Score Rating Treatment as Quite a Bit to Extremely Effective at Final On-Treatment Assessment

The subject was asked to rate his global evaluation of the efficacy of treatment using the following 5-point scale: 0=not at all effective 1=a little bit effective 2=moderately effective 3=quite a bit effective 4=extremely effective. (NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of subjects (Number)
PLACEBO30.4
PRUCALOPRIDE46.7

[back to top]

Percent of Subjects on the Subject Global Evaluation on Severity of Constipation Score Rating Constipation as Severe to Very Severe at Final On-Treatment Assessment

Subject was asked to rate the severity of his constipation using a 5-point Likert scale: 0=absent, 1=mild, 2=moderate, 3=severe, 4=very severe (NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of subjects (Number)
PLACEBO30.4
PRUCALOPRIDE21.9

[back to top]

Percent of Subjects With an Improvement of ≥ 1 Point on the Patient Assessment of Constipation - Quality of Life (PAC-QOL) Total Score at Final On Treatment Assessment

The PAC-QOL is a validated 28-item questionnaire for the evaluation of quality of life in subjects with constipation. Items are rated on a 5-point Likert scale: 0=not at all/none of the time, 1=a little bit/a little bit of the time, 2=moderately/some of the time, 3=quite a bit/most of the time, 4=extremely/all of the time. Total score ranges from 0-112. Lower scores indicate improvement in symptoms. A 1-point improvement in PAC-QOL total score was considered clinically meaningful. (NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of subjects (Number)
PLACEBO32.7
PRUCALOPRIDE40.2

[back to top]

Percent of Subjects With an Improvement of ≥ 1 Point on the Patient Assessment of Constipation - Symptom (PAC-SYM) Questionnaire Total Score at Final On Treatment Assessment

The PAC-SYM is a validated 12-item questionnaire for the evaluation of severity of symptoms of constipation in subjects with constipation. Items are rated on a 5-point Likert scale: 0=absent, 1=mild, 2=moderate, 3=severe, 4=very severe. Total score ranges from 0 to 48. Lower scores indicate improvement in symptoms. A 1-point improvement in PAC-SYM total score was considered clinically meaningful. (NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of subjects (Number)
PLACEBO30.4
PRUCALOPRIDE34.9

[back to top]

Percent SBM With Sensation of Complete Evacuation

(NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of SBM (Mean)
PLACEBO43.2
PRUCALOPRIDE46.7

[back to top]

Percentage of Subjects With an Average Weekly Frequency of at Least 3 SCBM Per Week and an Increase of ≥ 1 SCBM Per Week for ≥ 75% of the 12-week Treatment Period and ≥ 75% of the Last Third of the 12-week Treatment Period

(NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of subjects (Number)
PLACEBO12.2
PRUCALOPRIDE27.7

[back to top]

Percentage of Subjects With an Increase of at Least 1 SCBM Per Week

(NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of subjects (Number)
PLACEBO45.3
PRUCALOPRIDE53.7

[back to top]

SCBM Per Week

(NCT01147926)
Timeframe: Over 12 week treatment period

InterventionSCBM/week (Mean)
PLACEBO1.8
PRUCALOPRIDE2.6

[back to top]

The Percentage of Subjects With an Average of ≥3 Spontaneous Complete Bowel Movements (SCBM) Per Week

Spontaneous Bowel Movements defined as a bowel movement that is not preceded within a period of 24 hours by the intake of a laxative agent or by the use of an enema. (NCT01147926)
Timeframe: Over 12 week treatment period

Interventionpercentage of subjects (Number)
PLACEBO17.7
PRUCALOPRIDE37.9

[back to top]

Time to First SCBM After Investigational Product Intake on Day 1

(NCT01147926)
Timeframe: Day 1

Interventionhours (Median)
PLACEBO218.9
PRUCALOPRIDE110.3

[back to top]

Percent SBM With a Consistency of Normal and Hard/Very Hard

Consistency measured using the 7-point Bristol scale where 1-2 indicate constipation (=hard/very hard), 3-4 are ideal stools (=normal), and 5-7 tending toward diarrhea. (NCT01147926)
Timeframe: Over 12 week treatment period

,
Interventionpercentage of SBM (Mean)
Normal consistencyHard/Very hard consistency
PLACEBO50.831.9
PRUCALOPRIDE47.526.9

[back to top]

Percent SCBM With No Straining and Severe/Very Severe Straining

Straining was evaluated on a 5-point scale (0=none, 1=mild, 2=moderate, 3=severe, or 4=very severe) (NCT01147926)
Timeframe: Over 12 week treatment period

,
Interventionpercentage of SBM (Mean)
No strainingSevere/Very severe straining
PLACEBO9.523.7
PRUCALOPRIDE9.720.6

[back to top]

Efficacy of Treatment for Final On Treatment Assessment in Open-Label Treatment Period

(NCT01330381)
Timeframe: Over the 16 week open label treatment period

,
Interventionpercentage of subjects (Number)
Not at all effectiveLittle bit effectiveModerately effectiveQuite a bit effectiveExtremely effective
PEG 400015.15.411.821.546.2
Prucalopride29.910.320.618.620.6

[back to top]

Efficacy of Treatment for Final On Treatment Assessment in Double-Blind Treatment Period

(NCT01330381)
Timeframe: Over the 8 week double blind treatment period

,
Interventionpercentage of subjects (Number)
Not at all effectiveLittle bit effectiveModerately effectiveQuite a bit effectiveExtremely effective
Placebo32.718.725.214.09.3
Prucalopride33.014.615.522.314.6

[back to top]

Convenience of Treatment for Final On Treatment Assessment in Open-Label Treatment Period

(NCT01330381)
Timeframe: Over the 16 week open label treatment period

,
Interventionpercentage of subjects (Number)
NeutralVery difficultQuite difficultQuite easyVery easy
PEG 400015.62.25.628.947.8
Prucalopride16.51.00.027.854.6

[back to top]

Time to First SBM in the Double-Blind Treatment Period

After intake of the trial medication on Day 1. (NCT01330381)
Timeframe: Day 1 onwards

Interventionhours (Median)
Prucalopride67.00
Placebo99.75

[back to top]

Stool Consistency Per SBM Score in Children Without Diapers in the Double-Blind Treatment Period

Measured using the 7-point Bristol scale where 1-2 indicate constipation, 3-4 are ideal stools, and 5-7 tending toward diarrhea. (NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventionunits on a scale (Mean)
Prucalopride3.8
Placebo3.6

[back to top]

Stool Consistency Per SBM Score in Children With Diapers in the Double-Blind Treatment Period

Measured on a 4-point scale where 1 is constipation, 2-3 is ideal, and 4 is diarrhea. (NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventionunits on a scale (Mean)
Prucalopride2.1
Placebo2.0

[back to top]

Percent of Subjects With Fecal Incontinence Episodes of 1 or Less Per 2 Weeks in the Last Four Weeks of the Double-Blind Treatment Period

Fecal incontinence is a lack of control over defecation, leading to involuntary loss of bowel contents (only for subjects after acquisition of toileting skills). (NCT01330381)
Timeframe: Last 4 weeks of double-blind treatment period

Interventionpercentage of subjects (Number)
Prucalopride43.0
Placebo43.0

[back to top]

Percent of Subjects With Bowel Frequency of 3 or More Spontaneous Bowel Movements (SBM) Per Week in the Last Four Weeks of the Double-Blind Treatment Period

Spontaneous Bowel Movements defined as a bowel movement that is not preceded within a period of 24 hours by the intake of a laxative agent or by the use of an enema. (NCT01330381)
Timeframe: Last 4 weeks of double-blind treatment period

Interventionpercentage of subjects (Number)
Prucalopride29.2
Placebo35.5

[back to top]

Percent of Responders in the Last Four Weeks of the Double-Blind Treatment Period

Responders are defined as subjects with an average spontaneous defecation frequency is ≥3 times per week AND the average number of fecal incontinence episodes per 2 weeks is ≤ 1 episode (only for subjects after acquisition of toileting skills). (NCT01330381)
Timeframe: Last 4 weeks of double-blind treatment period

Interventionpercentage of subjects (Number)
Prucalopride17.0
Placebo17.8

[back to top]

Painful Bowel Movements Score in the Double-Blind Treatment Period

Pain was rated on a 6-point scale (0=no hurt, 1=hurts little bit, 2=hurts little more, 3=hurts even more, 4=hurts whole lot, 5=hurts worst) in subjects of 3 years and older. Lower scores represent less pain. (NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventionunits on a scale (Mean)
Prucalopride1.3
Placebo1.7

[back to top]

Number of Retentive Posturing or Excessive Volitional Stool Retention in the Double-Blind Treatment Period

Purposefully avoiding defecation. (NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventionretentions/week (Mean)
Prucalopride1.1
Placebo1.2

[back to top]

Number of Rescue Medications Taken in the Double-Blind Treatment Period

(NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventionrescue medications/week (Mean)
Prucalopride1.2
Placebo1.3

[back to top]

Large Diameter Stools in the Double-Blind Treatment Period

Large diameter stools make defecation more difficult. Small diameter stools are better. (NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventionlarge diameter stools/week (Mean)
Prucalopride1.7
Placebo1.7

[back to top]

Frequency of Toilet Training in the Double-Blind Treatment Period

Only for subjects after acquisition of toileting skills. (NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventiontoilet trainings/week (Mean)
Prucalopride4.9
Placebo5.1

[back to top]

Change From Baseline in the Number of SBM Per Week Over the 8 Week Double Blind Treatment Period

(NCT01330381)
Timeframe: Baseline and over the 8 week double blind treatment period

InterventionSBM/week (Mean)
Prucalopride1.5
Placebo1.0

[back to top]

Abdominal Pain Score in Double-Blind Treatment Period

Pain was rated on a 6-point scale (0=no hurt, 1=hurts little bit, 2=hurts little more, 3=hurts even more, 4=hurts whole lot, 5=hurts worst) in subjects of 3 years and older. Lower scores represent less pain. (NCT01330381)
Timeframe: Over the 8 week double blind treatment period

Interventionunits on a scale (Mean)
Prucalopride0.9
Placebo1.1

[back to top]

Number of SBM Per Week in the Double-Blind Treatment Period

(NCT01330381)
Timeframe: Over the 8 week double blind treatment period

InterventionSBM/week (Mean)
Prucalopride2.3
Placebo2.1

[back to top]

Severity of Constipation Over the Past 2 Weeks for the Final On Treatment Assessment in the Double-Blind Treatment Period

(NCT01330381)
Timeframe: 2 weeks

,
Interventionpercentage of subjects (Number)
AbsentMildModerateSevereVery severe
Placebo5.618.727.124.324.3
Prucalopride15.521.419.427.216.5

[back to top]

Severity of Constipation Over the Past 2 Weeks for the Final On Treatment Assessment in the Open-Label Treatment Period

(NCT01330381)
Timeframe: 2 weeks

,
Interventionpercentage of subjects (Number)
AbsentMildModerateSevereVery severe
PEG 400046.216.19.715.112.9
Prucalopride24.717.517.515.524.7

[back to top]

Change From Baseline in Spontaneous Complete Bowel Movements Per Week at Up to 24 Weeks

(NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

InterventionSCBM/week (Mean)
Placebo1.3
Prucalopride1.7

[back to top]

Change From Baseline in Straining Per SCBM at Up to 24 Weeks

Straining was evaluated on a 5-point scale (0=none, 1=mild, 2=moderate, 3=severe, or 4=very severe) (NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

Interventionunits on a scale (Mean)
Placebo-0.44
Prucalopride-0.23

[back to top]

Change From Baseline in the Number of Bisacodyl Tablets Taken Per Week at Up to 24 Weeks

(NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

Interventiontablets/week (Mean)
Placebo-0.68
Prucalopride-0.97

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Change From Baseline in the Number of Days With Rescue Medication Taken Per Week at Up to 24 Weeks

Rescue medications include laxatives and enemas. (NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

Interventiondays/week (Mean)
Placebo-0.42
Prucalopride-0.54

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Change From Baseline in the Patient Assessment of Constipation - Quality of Life (PAC-QOL) Score at Up to the Final On Treatment Assessment Value

The PAC-QOL is a validated 28-item questionnaire for the evaluation of quality of life in subjects with constipation. Items are rated on a 5-point Likert scale: 0=not at all/none of the time, 1=a little bit/a little bit of the time, 2=moderately/some of the time, 3=quite a bit/most of the time, 4=extremely/all of the time. Total score ranges from 0-112. Lower scores indicate improvement in symptoms. A 1-point improvement in PAC-QOL total score was considered clinically meaningful. (NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

Interventionunits on a scale (Mean)
Placebo-0.73
Prucalopride-0.67

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Change From Baseline in the Patient Assessment of Constipation - Symptom (PAC-SYM) Questionnaire Score at Up to the Final On Treatment Assessment Value

The PAC-SYM is a validated 12-item questionnaire for the evaluation of severity of symptoms of constipation in subjects with constipation. Items are rated on a 5-point Likert scale: 0=absent, 1=mild, 2=moderate, 3=severe, 4=very severe. Total score ranges from 0 to 48. Lower scores indicate improvement in symptoms. A 1-point improvement in PAC-SYM total score was considered clinically meaningful. (NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

Interventionunits on a scale (Mean)
Placebo-0.68
Prucalopride-0.55

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Percentage of Subjects With an Increase of ≥1 Spontaneous Complete Bowel Movement (SCBM) Per Week Up to 24 Weeks

(NCT01424228)
Timeframe: Over 24 week treatment period

Interventionpercentage of subjects (Number)
Placebo42.0
Prucalopride48.0

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The Percentage of Subjects With an Average of ≥3 Spontaneous Complete Bowel Movements (SCBM) Per Week Over the 24 Week Treatment Period

Spontaneous Bowel Movements defined as a bowel movement that is not preceded within a period of 24 hours by the intake of a laxative agent or by the use of an enema. (NCT01424228)
Timeframe: Over 24 week treatment period

Interventionpercentage of subjects (Number)
Placebo20.7
Prucalopride25.1

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Change From Baseline in Percent SCBM With a Consistency of Normal and Hard/Very Hard at Up to 24 Weeks

(NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

,
Interventionpercentage of SCBM (Mean)
Normal consistencyHard/Very Hard consistency
Placebo16.82-9.11
Prucalopride25.71-13.82

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Change From Baseline in Average Consistency Per SCBM at Up to 24 Weeks

Consistency measured using the 7-point Bristol scale where 1-2 indicate constipation (=hard/very hard), 3-4 are ideal stools (=normal), and 5-7 tending toward diarrhea. (NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

Interventionunits on a scale (Mean)
Placebo-0.1
Prucalopride-0.1

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Change From Baseline in the Short Form-36 Health Survey (SF-36) Score at Up to the Final On Treatment Assessment Value

The SF-36 consists of eight scaled scores, which are the weighted sums of the questions in their section. Total score ranges from 0 (lowest level of health) - 100 (highest level of health) on the assumption that each question carries equal weight. The lower the score the more disability. The higher the score the less disability (i.e. a score of zero is equivalent to maximum disability and a score of 100 is equivalent to no disability). Higher scores are associated with better quality of life. (NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

,
Interventionunits on a scale (Mean)
Mental componentPhysical component
Placebo3.7863.331
Prucalopride3.1792.965

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Percent of Subjects With an Average Weekly Frequency of at Least 3 SCBM by 4-Week Treatment Period

(NCT01424228)
Timeframe: Over 24 week treatment period

,
Interventionpercentage of subjects (Number)
First 4-week periodSecond 4-week periodThird 4-week periodFourth 4-week periodFifth 4-week periodSixth 4-week period
Placebo18.323.723.722.523.724.9
Prucalopride26.925.729.229.233.326.9

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Percent of Subjects With an Average Weekly Frequency of at Least 3 SCBM by Week

(NCT01424228)
Timeframe: Over 24 week treatment period

,
Interventionpercentage of subjects (Number)
Week 1Week 2Week 3Week 4Week 5Week 6Week 7Week 8Week 9Week 10Week 11Week 12Week 13Week 14Week 15Week 16Week 17Week 18Week 19Week 20Week 21Week 22Week 23Week 24
Placebo18.323.122.523.126.628.429.026.027.826.025.427.223.730.224.929.628.430.232.024.926.627.830.232.0
Prucalopride32.234.532.231.627.529.229.830.433.330.437.433.930.435.729.235.135.132.732.237.430.432.731.031.6

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Time to First SCBM After Investigational Product Intake on Day 1 and Day 28

(NCT01424228)
Timeframe: Day 1 and 28

,
Interventionhours (Median)
Day 1Day 28
Placebo359.67100.58
Prucalopride100.8381.78

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Change From Baseline in Percent SCBM With No Straining and Severe/Very Severe Straining at Up to 24 Weeks

(NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

,
Interventionpercentage of SCBM (Mean)
No strainingSevere/Very Severe straining
Placebo11.14-9.85
Prucalopride6.61-4.49

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Average Number of Spontaneous Complete Bowel Movements (SCBM) Per Week Up to 24 Weeks

(NCT01424228)
Timeframe: Over 24 week treatment period

InterventionSCBM/week (Mean)
Placebo1.7
Prucalopride2.1

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Change From Baseline in Percent SBM With Sensation of Complete Evacuation at Up to 24 Weeks

(NCT01424228)
Timeframe: Baseline and Over 24 week treatment period

Interventionpercentage of SBM (Mean)
Placebo20.94
Prucalopride24.22

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Propagation Velocity of HAPC

Propagation velocity was calculated as the extension divided by the duration for each HAPC. Mean propagation velocity is the sum of the propagation velocities divided by the number of HAPCs. (NCT01707667)
Timeframe: over 12 hours post-dose

Interventioncm/sec (Least Squares Mean)
Prucalopride0.467
PEG 33500.646

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Duration of HAPC

The mean duration of all HAPCs was calculated as the sum of the duration of each HAPC divided by the number of HAPCs. (NCT01707667)
Timeframe: over 12 hours post-dose

Interventionsec (Least Squares Mean)
Prucalopride84.9
PEG 335069.1

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Area Under the Concentration Curve (AUC) of All HAPCs

The AUC of all HAPCs during the first 12 hours after treatment was calculated as the sum of the AUC at all sensors of each HAPC at the ≥100mmHg and ≥20cm threshold. (NCT01707667)
Timeframe: over 12 hours post-dose

InterventionmmHg.sec (Least Squares Mean)
Prucalopride110204.1
PEG 335041152.7

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The Mean Amplitude of HAPC

The mean amplitude of all HAPCs was calculated as the sum of the mean amplitude for each HAPC divided by the number of HAPCs. (NCT01707667)
Timeframe: over 12 hours post-dose

InterventionmmHg (Least Squares Mean)
Prucalopride199.0
PEG 3350189.8

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The Number of High-Amplitude Propagating Contractions (HAPC)

Manometry recordings were read by an experienced gastroenterologist who was blinded to the treatment each subject received. The tracings were analyzed using computer-based validated software. HAPC and manometry data were available for every sensor as well as average values for each HAPC and manometry time point. The primary outcome analysis of HAPC data used the following threshold: Mean amplitude ≥100mmHg and extension ≥20cm (9 sensors). (NCT01707667)
Timeframe: over 12 hours post-dose

InterventionNumber of HAPC with amplitude ≥100mmHg (Least Squares Mean)
Prucalopride8.7
PEG 33502.9

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Time to First HAPC

The median (95% CI) time to first HAPC after administration of investigational product with amplitude ≥100mmHg and extension ≥20cm. (NCT01707667)
Timeframe: over 12 hours post-dose

Interventionhours (Median)
Prucalopride4.5
PEG 3350NA

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Motility Index

Motility index (mmHg) was summarized for the following 3 time points: pre-dose, 0-5 hours post-dose, and 5-12 hours post-dose. The motility index is defined as the natural logarithm of all peak amplitudes of every contraction +1. (NCT01707667)
Timeframe: over 12 hours post-dose

,
InterventionmmHg (Least Squares Mean)
Pre-Dose0-5 hours post-dose5-12 hours post-dose
PEG 33508.31213.34914.390
Prucalopride9.46713.66114.208

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Percent Total Radioactivity Excreted in Stool of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionpercentage of radioactivity (Mean)
[14C] PRUCALOPRIDE SUCCINATE13.3

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Maximum Plasma Concentration (Cmax) of Radiolabelled Prucalopride Succinate

Cmax is a term that refers to the maximum (or peak) concentration that a drug achieves in the body after the drug has been administered. (NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionng/ml (Mean)
[14C] PRUCALOPRIDE SUCCINATE3.79

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Half-Life Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionhours (Mean)
[14C] PRUCALOPRIDE SUCCINATE18.0

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Half-Life Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionhours (Mean)
[14C] PRUCALOPRIDE SUCCINATE19.7

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Cmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionng equivalents/ml (Mean)
[14C] PRUCALOPRIDE SUCCINATE7.74

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Cmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionng equivalents/ml (Mean)
[14C] PRUCALOPRIDE SUCCINATE4.14

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AUC 0→∞ Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionng equivalents*h/ml (Mean)
[14C] PRUCALOPRIDE SUCCINATE192

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AUC 0→∞ Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionng equivalents*h/ml (Mean)
[14C] PRUCALOPRIDE SUCCINATE102

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Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity (AUC 0→∞) of Radiolabelled Prucalopride Succinate

AUC can be used as a measure of drug exposure. It is derived from drug concentration and time so it gives a measure how much and how long a drug stays in a body. (NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionng*h/ml (Mean)
[14C] PRUCALOPRIDE SUCCINATE96.5

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Total Body Clearance (CL/F) of Radiolabelled Prucalopride Succinate

The rate at which a drug is removed from the body. (NCT01807000)
Timeframe: Over 240 hours post-dose

InterventionL/h (Mean)
[14C] PRUCALOPRIDE SUCCINATE20.9

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Tmax Whole Blood Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionhours (Median)
[14C] PRUCALOPRIDE SUCCINATE2.75

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Tmax Plasma Total Radioactivity of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionhours (Median)
[14C] PRUCALOPRIDE SUCCINATE2.25

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Time to Maximum Plasma Concentration (Tmax) of Radiolabelled Prucalopride Succinate

Tmax is the time after administration of a drug when the maximum plasma concentration in the body is reached. (NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionhours (Median)
[14C] PRUCALOPRIDE SUCCINATE2.75

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Plasma Half-Life (T1/2) of Radiolabelled Prucalopride Succinate

The time it takes for the blood plasma concentration of a substance to halve. (NCT01807000)
Timeframe: Over 240 hours post-dose

Interventionhours (Mean)
[14C] PRUCALOPRIDE SUCCINATE20.6

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Volume of Distribution (Vz/F) of Radiolabelled Prucalopride Succinate

The distribution of a medication between plasma and the rest of the body. (NCT01807000)
Timeframe: Over 240 hours post-dose

InterventionLiters (Mean)
[14C] PRUCALOPRIDE SUCCINATE623

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Percent Total Radioactivity Excreted in Urine of Radiolabelled Prucalopride Succinate

(NCT01807000)
Timeframe: 240 hours post-dose

Interventionpercentage of radioactvity (Mean)
[14C] PRUCALOPRIDE SUCCINATE84.2

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the Proportion of Overall CSBM Responders Over Weeks 1-8

A weekly CSBM responder was defined as a patient who had ≥3 CSBMs for a given week and an increase from baseline of ≥1 CSBM for that same week. An overall CSBM responder was a patient who was a weekly CSBM responder for at least 6 of the 8 treatment weeks (75%). (NCT02047045)
Timeframe: over weeks 1-8

Interventionpercentage of participants (Number)
Electro-acupuncture24.91
Prucalopride25.54

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the Proportion of Participants With ≥3 Mean Weekly CSBMs Over Weeks 3-8

"Abbreviation: CSBMs, complete spontaneous bowel movements. Calculation method: First, the mean weekly CSBMs of each patient were calculated over weeks 3-8. Second, we got the number of patients with 3 or more mean weekly CSMBs. Third, we got the proportion of participants through dividing that number by the total cases at baseline, and multiplying by 100%.~Assessing time frame: the latter 6 weeks of treatment (weeks 3-8)." (NCT02047045)
Timeframe: over weeks 3-8 (the latter 6-week treatment)

Interventionpercentage of participants (Number)
Electro-acupuncture36.2
Prucalopride37.8

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the Proportion of Sustained CSBM Responder Over Weeks 1-8

(NCT02047045)
Timeframe: over weeks 1-8

Interventionpercentage of participants (Number)
Electro-acupuncture24.91
Prucalopride24.46

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Time to the First CSBMs

Abbreviation: CSBMs, complete spontaneous bowel movements. Time to the first CSBMs was counted by days. Rescue medicine or other measurements for constipation is not allowed to be used 48 hours before and after the first treatment for evaluating the time to the first complete spontaneous bowel movement. Participants were assessed after the first treatment until they having their first CSBMs. (NCT02047045)
Timeframe: from the time of their first treatment to the time they having their first CSBMs

Interventiondays (Median)
Electro-acupuncture4
Prucalopride5

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Average Dosage of Bisacodyl Used Weekly Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

(NCT02047045)
Timeframe: over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

,
Interventiontablet (Median)
weeks 1-2weeks 3-8weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture0.750.170.500.500.500.50
Prucalopride0.500.670.750.501.001.00

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Average Dosage of Glycerine Enema Used Weekly Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

(NCT02047045)
Timeframe: over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

,
Interventionml (Median)
weeks 1-2weeks 3-8weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture40.0018.3330.0055.0052.5055.00
Prucalopride55.0018.3320.0022.5045.0037.50

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Change From Baseline in Mean Score of Patient Assessment of Constipation Quality of Life

The change from baseline of the score of Patient Assessment of Constipation Quality of Life (PAC-QOL) at week 4 and week 8. PAC-QOL is a self-report questionnaire to evaluate the quality of life in patients with constipation, which was distributed by Mapi Research Trust in France. This questionnaire contains 28 items including 4 basic parts of physical discomfort, worries and concerns, psychosocial discomfort, and satisfaction. We use the Chinese version in our trial. Assessing point: baseline, week 4 and week 8. The score of PAC-QOL ranged from 1 to 5 (1 indicates no discomfort or feeling very satisfied, 5 indicates extreme severity and always appears or feeling very dissatisfied). (NCT02047045)
Timeframe: week 4 and week 8

,
Interventionscore (Mean)
week 4week 8
Electro-acupuncture-0.71-1.09
Prucalopride-0.72-1.00

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Mean Weekly CSBMs and Its Change From Baseline Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

(NCT02047045)
Timeframe: over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

,
Interventionbowel movements (Mean)
weeks 1-2weeks 3-8weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture1.271.962.001.931.901.94
Prucalopride1.781.972.012.072.001.99

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Mean Weekly SBMs and Its Change From Baseline Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

(NCT02047045)
Timeframe: over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

,
Interventionbowel movements (Mean)
weeks 1-2weeks 3-8weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture1.852.131.871.651.591.50
Prucalopride2.912.602.432.382.332.24

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Proportion of Patients Using Rescue Medicine Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

(NCT02047045)
Timeframe: over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

,
Interventionpercentage of participants (Number)
weeks 1-2weeks 3-8weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture13.7219.499.7510.4710.8310.11
Prucalopride7.9117.996.837.195.766.47

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the Change From Baseline in Mean Score of Stool Consistency for Each SBM Over Weeks 1-2 and 3-8.

"The change from baseline in the mean score of stool consistency of each SBM over weeks 1-2 and weeks 3-8. Assessing time: baseline, weeks 1-2 and weeks 3-8. Patients will self-report their stool consistency of each SBM according to the 7-type Bristol Stool Form Scale (scored by 1 to 7 respectively). Type 1: Separate hard lumps, like nuts (hard to pass); Type 2: Sausage-shaped, but lumpy; Type 3: Like a sausage but with cracks on its surface; Type 4: Like a sausage or snake, smooth and soft; Type 5: Soft blobs with clear cut edges (passed easily); Type 6: Fluffy pieces with ragged edges, a mushy stool; Type 7: Watery, no solid pieces. Entirely liquid.~Type 3 and 4 were deemed as a normal stool." (NCT02047045)
Timeframe: over weeks 1-2, 3-8.

,
Interventionscore (Median)
weeks 1-2weeks 3-8
Electro-acupuncture0.480.78
Prucalopride0.670.74

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the Change From Baseline in Mean Score of Straining for Each SBM Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

The change from baseline in the mean score of straining of each SBM over weeks 1-2, 3-8, 9-12, 9-16, 9-20, 9-32. Assessing time: baseline, weeks 1-2, 3-8, 9-12, 9-16, 9-20, 9-32. Patients will self-report their straining degree of each SBM in the defecation diaries according to the following scale. 0 = not difficult; 1 = a little difficult, need some straining to defecate; 2 = difficult, need straining to defecate; 3 = very difficult, need hard straining to defecate. Higher scores mean a worse outcome. (NCT02047045)
Timeframe: over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

,
Interventionscore (Median)
weeks 1-2week 3-8weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture-0.33-0.54-0.60-0.59-0.67-0.67
Prucalopride-0.52-0.63-0.58-0.57-0.67-0.67

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the Proportion of Participants With ≥1 Increase in Mean Weekly CSBMs From Baseline Over Weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

"Abbreviation: CSBMs, complete spontaneous bowel movements. Calculation method: First, the increase in mean weekly CSBMs of each patient from baseline were calculated over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32. Second, we got the number of patients with ≥1 increase in the mean weekly CSMBs from baseline. Third, we got the proportion of participants through dividing that number by the total cases at baseline, and multiplying by 100%.~Assessing time frame: weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32." (NCT02047045)
Timeframe: over weeks 1-2, 3-8, 11-12, 15-16, 19-20, 31-32.

,
Interventionpercentage of participants (Number)
weeks 1-2weeks 3-8weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture49.566.463.565.761.461.0
Prucalopride61.563.363.766.264.061.5

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the Proportion of Participants With ≥3 Mean Weekly CSBMs Over Weeks 1-2, 11-12, 15-16, 19-20, 31-32.

"Abbreviation: CSBMs, complete spontaneous bowel movements. Calculation method: First, the mean weekly CSBMs of each patient were calculated over weeks 1-2, 11-12, 15-16, 19-20, 31-32. Second, we got the number of patients with 3 or more mean weekly CSMBs. Third, we got the proportion of participants through dividing that number by the total cases at baseline, and multiplying by 100%.~Assessing time frame: weeks 1-2, 11-12, 15-16, 19-20, 31-32." (NCT02047045)
Timeframe: over weeks 1-2, 11-12, 15-16, 19-20, 31-32.

,
Interventionpercentage of participants (Number)
weeks 1-2weeks 11-12weeks 15-16weeks 19-20weeks 31-32
Electro-acupuncture27.138.338.035.737.6
Prucalopride33.843.241.042.138.5

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