Renzapride

Renzapride

Clinical data
ATC code	none
Identifiers
IUPAC name 4-amino-N-[(4S,5S)-1-azabicyclo[3.3.1]nonan-4-yl]-5-chloro-2-methoxybenzamide
CAS Number	109872-41-5 N
PubChem CID	3086547
IUPHAR/BPS	244
ChemSpider	16736758 Y
UNII	9073C0W4E9
ChEMBL	CHEMBL289753 N
Chemical and physical data
Formula	C16H22ClN3O2
Molar mass	323.818 g/mol
3D model (Jmol)	Interactive image
SMILES Clc1cc(c(OC)cc1N)C(=O)N[C@@H]3CC[N@]2C[C@@H]3CCC2
InChI 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 Y Key:GZSKEXSLDPEFPT-IINYFYTJSA-N Y
NY (what is this?)

Renzapride is a gastroprokinetic agent and antiemetic which acts as a full 5-HT₄ full agonist and 5-HT₃ antagonist. It also functions as a 5-HT_2B antagonist and has some affinity for the 5-HT_2A and 5-HT_2C receptors, though it is unlikely that these properties contribute to its therapeutic effects.

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, , 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.

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.