Prucalopride

Prucalopride
Clinical data
Trade namesResolor, Resotran, Motegrity
Other namesR-093877, R-108512
AHFS/Drugs.comMonograph
MedlinePlusa619011
License data
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)[1]
  • UK: POM (Prescription only)
  • US: ℞-only[2]
  • EU: Rx-only[3]
  • In general: ℞ (Prescription only)
Identifiers
  • 4-Amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H26ClN3O3
Molar mass367.87 g·mol−1
3D model (JSmol)
  • COCCCN1CCC(CC1)NC(=O)C2=CC(=C(C3=C2OCC3)N)Cl
  • InChI=1S/C18H26ClN3O3/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14/h11-12H,2-10,20H2,1H3,(H,21,23) ☒N
  • Key:ZPMNHBXQOOVQJL-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Prucalopride, sold under brand names Resolor and Motegrity among others, is a medication acting as a selective, high affinity 5-HT4 receptor agonist[4] which targets the impaired motility associated with chronic constipation, thus normalizing bowel movements.[5][6][7][8][9][10] Prucalopride was approved for medical use in the European Union in 2009,[3] in Canada in 2011,[11] in Israel in 2014,[12] and in the United States in December 2018.[13] The drug has also been tested for the treatment of chronic intestinal pseudo-obstruction.[14][15]

  1. ^ "Prucalopride succinate (MedTAS Pty Ltd)". Therapeutic Goods Administration (TGA). 7 October 2022. Archived from the original on 18 March 2023. Retrieved 29 April 2023.
  2. ^ "Motegrity- prucalopride tablet, film coated". DailyMed. 28 October 2022. Retrieved 13 September 2024.
  3. ^ a b "Resolor EPAR". European Medicines Agency (EMA). 17 November 2009. Archived from the original on 31 January 2010.
  4. ^ Briejer MR, Bosmans JP, Van Daele P, Jurzak M, Heylen L, Leysen JE, et al. (June 2001). "The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound". European Journal of Pharmacology. 423 (1): 71–83. doi:10.1016/S0014-2999(01)01087-1. PMID 11438309.{{cite journal}}: CS1 maint: overridden setting (link)
  5. ^ Clinical trial number NCT00793247 for "Efficacy Study of Prucalopride to Treat Chronic Intestinal Pseudo-Obstruction (CIP)" at ClinicalTrials.gov
  6. ^ Emmanuel AV, Kamm MA, Roy AJ, Kerstens R, Vandeplassche L (January 2012). "Randomised clinical trial: the efficacy of prucalopride in patients with chronic intestinal pseudo-obstruction--a double-blind, placebo-controlled, cross-over, multiple n = 1 study". Alimentary Pharmacology & Therapeutics. 35 (1): 48–55. doi:10.1111/j.1365-2036.2011.04907.x. PMC 3298655. PMID 22061077.
  7. ^ Smart CJ, Ramesh AN (August 2012). "The successful treatment of acute refractory pseudo-obstruction with prucalopride". Colorectal Disease. 14 (8): e508. doi:10.1111/j.1463-1318.2011.02929.x. PMID 22212130. S2CID 29060148.
  8. ^ Bouras EP, Camilleri M, Burton DD, McKinzie S (May 1999). "Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans". Gut. 44 (5): 682–6. doi:10.1136/gut.44.5.682. PMC 1727485. PMID 10205205.
  9. ^ Bouras EP, Camilleri M, Burton DD, Thomforde G, McKinzie S, Zinsmeister AR (February 2001). "Prucalopride accelerates gastrointestinal and colonic transit in patients with constipation without a rectal evacuation disorder". Gastroenterology. 120 (2): 354–60. doi:10.1053/gast.2001.21166. PMID 11159875.
  10. ^ Tack J, van Outryve M, Beyens G, Kerstens R, Vandeplassche L (March 2009). "Prucalopride (Resolor) in the treatment of severe chronic constipation in patients dissatisfied with laxatives". Gut. 58 (3): 357–65. doi:10.1136/gut.2008.162404. PMID 18987031. S2CID 206948212.
  11. ^ "Health Canada, Notice of Decision for Resotran". hc-sc.gc.ca. Archived from the original on 18 March 2017. Retrieved 1 May 2018.
  12. ^ "Digestive Remedies in Israel". www.euromonitor.com. Archived from the original on 13 March 2018. Retrieved 1 May 2018.
  13. ^ "Drug Approval Package: Motegrity (prucalopride)". U.S. Food and Drug Administration (FDA). 28 December 2018. Archived from the original on 8 October 2020. Retrieved 3 October 2020.
  14. ^ Briejer MR, Prins NH, Schuurkes JA (October 2001). "Effects of the enterokinetic prucalopride (R093877) on colonic motility in fasted dogs". Neurogastroenterology and Motility. 13 (5): 465–72. doi:10.1046/j.1365-2982.2001.00280.x. PMID 11696108. S2CID 13610558.
  15. ^ Oustamanolakis P, Tack J (February 2012). "Prucalopride for chronic intestinal pseudo-obstruction". Alimentary Pharmacology & Therapeutics. 35 (3): 398–9. doi:10.1111/j.1365-2036.2011.04947.x. PMID 22221087. S2CID 5526239.