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Tranzyme Pharma Presents Positive Preclinical Efficacy Data for Its Lead GI Therapeutic, TZP-101; Data Presented at Digestive Disease Week 2005

Posted on: Thursday, 19 May 2005, 09:00 CDT

Tranzyme Pharma, a leading biopharmaceutical company developing small molecule therapeutics for the treatment of gastrointestinal (GI) disorders, presented positive data highlighting the effectiveness of its TZP-101 in promoting gastrointestinal (GI) motility in animal models of post-operative ileus (POI). The data was presented by scientists from the University of Oklahoma and Tranzyme Pharma at the Digestive Disease Week 2005 Conference (Chicago, IL). TZP-101 is a novel small molecule ghrelin agonist being developed by Tranzyme Pharma as a first-in-class treatment for both POI and diabetic gastroparesis, serious medical conditions in which motility of the GI tract is severely impaired.

Dr. Beverly Greenwood-Van Meerveld, a leading GI researcher at the University of Oklahoma Health Sciences Center, presented the results of her studies utilizing a validated rat model of POI. The data demonstrate that TZP-101 induced a dose-dependent increase of gastric emptying that effectively reversed the delay caused by surgically induced POI. Treatment levels as low as 30ug/kg were shown to be effective in stimulating GI transit in this model. Furthermore, TZP-101 significantly stimulated gastric emptying in naive rats with 100-fold greater potency than metoclopramide, a compound currently marketed as a prokinetic treatment for gastroparesis.

"I am impressed with the results of this proof-of-concept study. POI is one example of a GI motility disorder where a new class of gastroprokinetic agent, such as TZP-101, may offer great therapeutic potential," stated Dr. Greenwood-Van Meerveld.

In a separate presentation by Graeme L. Fraser, Ph.D., Vice President of Drug Discovery for Tranzyme Pharma, TZP-101 shows highly favorable pharmacokinetic profile including excellent oral availability.

"These are exciting preclinical results that independently confirm the efficacy of TZP-101," said Vipin K. Garg, Ph.D., President & CEO for Tranzyme Pharma. "Our development program remains on track to file an IND for TZP-101 for POI by Q4 2005. The goal is to initiate Phase I clinical trials for this indication by the end of 2005, followed shortly thereafter by Phase I trials for diabetic gastroparesis."

About POI and diabetic gastroparesis

POI is an impairment of gastrointestinal motility that is an inevitable consequence of major abdominal surgery, especially under conditions of bowel resection. POI has an annual economic impact of $1.75 billion. There are no FDA-approved products for the treatment of POI. Diabetic gastroparesis is the impairment of stomach motility observed in both Type I and Type II diabetics to the extent that up to 10% of these patients require hospitalization at some stage for nausea, vomiting abdominal pain and malnutrition. Existing therapies for this condition offer poor efficacy and/or severe side effects. Moreover, the two most popular products for the treatment of gastroparesis (cisapride and domperidone) have been removed from the U.S. market due to their adverse side effects.

About the role of ghrelin in GI motility

Ghrelin is the most potent endogenous peptide known to stimulate gastric motility. Recent independent clinical studies have clearly demonstrated that infused ghrelin peptide potently stimulates gastric emptying in both human volunteers and diabetic gastroparesis patients. However, the ghrelin peptide has limited utility as a therapeutic product for GI indications due to its brief pharmacokinetic half-life and poor oral bioavailability, problems overcome by TZP-101.

Tranzyme Pharma is a leading biopharmaceutical company developing novel orally bioavailable, small molecule therapeutics for the treatment of gastrointestinal (GI) diseases. The Company's candidate drugs originate from its own discovery pipeline of proprietary compounds with high affinity for validated and druggable targets in the GI tract. Tranzyme is developing mechanism-based therapeutics for post-operative ileus, diabetic gastroparesis, irritable bowel syndrome (diarrhea-type) and functional dyspepsia and is on track to enter the clinic with its first product, TZP-101, by the end of 2005. Tranzyme is leveraging its technologies through internal programs and partnerships to drive the discovery and development of new therapeutics. For more information visit: www.tranzyme.com.

Source: Business Wire

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