Renzapride


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-HT2B antagonist and has some affinity for the 5-HT2A and 5-HT2C receptors.
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 planned 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.
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.
Endologic confirmed the cardiac safety of renzapride through a “Thorough QTc” study and sold the rights to Atlantic Healthcare in 2019.

Clinical trials

Renzapride was being investigated for the treatment of constipation-predominant irritable bowel syndrome. It is also potentially effective for irritable bowel syndrome with alternating stool pattern. It is being developed by Alizyme plc of the United Kingdom.
The renzapride Phase 3 trial in 2008 for the treatment of constipation-dominant irritable bowel syndrome demonstrated a small but statistically significant benefit in the Phase 3 study in IBS-C, however, Alizyme decided not to pursue development of the drug for this indication.