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.[1]

Renzapride was being developed by Alizyme plc of the United Kingdom. In May 2016, EndoLogic LLC, a US based pharmaceutical and medical device company acquired the US and world wide patent rights to Renzapride. EndoLogic plans to develop Renzapride for the treatment of gastroparesis.

Gastroparesis is a common condition affecting more than 20 million people in the US including 5 million diabetics. Currently, only one drug, metoclopramide, dopamine D2 receptor antagonist, is FDA approved for the treatment of gastroparesis in the US.

Unfortunately, patients treated with metoclopramide are at risk for serious side effects some of which are permanent, such as tardive dyskinesia, hence limiting the use of metoclopramide to no more than 12 weeks.

Renzapride could be a safer alternative to treat gastroparesis.

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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