Renzapride

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Renzapride
Clinical data
ATC code
  • none
Identifiers
  • 4-amino-N-[(4S,5S)-1-azabicyclo[3.3.1]nonan-4-yl]-5-chloro-2-methoxybenzamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC16H22ClN3O2
Molar mass323.818 g/mol g·mol−1
3D model (JSmol)
  • Clc1cc(c(OC)cc1N)C(=O)N[C@@H]3CC[N@]2C[C@@H]3CCC2
  • InChI=1S/C16H22ClN3O2/c1-22-15-8-13(18)12(17)7-11(15)16(21)19-14-4-6-20-5-2-3-10(14)9-20/h7-8,10,14H,2-6,9,18H2,1H3,(H,19,21)/t10-,14+/m0/s1 checkY
  • Key:GZSKEXSLDPEFPT-IINYFYTJSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Renzapride is a gastroprokinetic agent and antiemetic which acts as a full 5-HT4 full agonist and 5-HT3 antagonist.[1][2] It also functions as a 5-HT2B antagonist and has some affinity for the 5-HT2A and 5-HT2C receptors, though it is unlikely that these properties contribute to its therapeutic effects.[1]

Renzapride was being developed by Alizyme plc of the United Kingdom.

Clinical trials

Renzapride was being investigated for the treatment of constipation-predominant irritable bowel syndrome (IBS-C). It is also potentially effective for irritable bowel syndrome with alternating stool pattern (IBS-A). It is being developed by Alizyme plc of the United Kingdom.

As of 23 April 2008, Alizyme ceased all development of renzapride, after a Phase III trial in the U.S. did not show enough efficacy over placebo to justify further development.[3]

References

  1. ^ a b Meyers NL, Hickling RI (2008). "Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome". Drugs R D. 9 (1): 37–63. PMID 18095752.
  2. ^ Camilleri M., McKinzie S., Fox J., Foxx-Orenstein A., Burton D., Thomforde G., Baxter K. and Zinsmeister A. R. (2004). "Effect of Renzapride on Transit in Constipation-Predominant Irritable Bowel Syndrome", Clin. Gastroent. and Hepatology; 2:895-904
  3. ^ "Results from Renzapride" (Press release). Alizyme plc. 23 April 2008. Retrieved 7 May 2009.
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