The Canada-based Tranzyme Pharma, developing novel mechanism-based therapeutics for the treatment of gastrointestinal disorders, is moving forward with the development of TZP-101, a potent and selective ghrelin receptor agonist, which the company is developing for the treatment of post-operative ileus (POI) and gastroparesis. The company is planning for the initiation of Phase I trial for POI in the first quarter of 2006, said, Dr Vipin K Garg, president & CEO of Tranzyme.

"The preclinical studies have demonstrated that TZP-101 is a promising novel small molecule ghrelin agonist for the treatment of post-operative ileus and diabetic gastroparesis,”Dr Gordana Kosutic, vice president of Clinical and Regulatory Affairs, said.

POI is the impairment of gastrointestinal motility that routinely occurs following abdominal, gynaecological and pelvic surgeries. During this time, patients are neither able to tolerate oral feeding nor have bowel movements. An estimated number of five million surgeries of all types result in some degree of POI, driving the economic impact to over $1 billion.

Ghrelin is an endogenous hormone released by the stomach that stimulates gastric emptying. Studies have demonstrated the ability of ghrelin peptide to restore gut function in both rat and dog models of POI. Tranzyme is developing TZP-101 for use in the immediate post-operative period to accelerate normalization of gut function and enable more rapid discharge from the hospital with significant pharmaco-economic benefits.

Tranzyme is developing novel orally bio-available, small molecule therapeutics for the treatment of gastrointestinal (GI) diseases. The company’s candidate drugs originate from its discovery pipeline of proprietary compounds with affinity for validated and druggable targets in the GI tract.

The company is developing mechanism-based therapeutics for post-operative ileus, diabetic gastroparesis, irritable bowel syndrome (diarrhoea-type) and functional dyspepsia and is on track to enter the clinic with its first product in the first quarter of 2006.