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Last updated on April 24, 2014 at 1:21 EDT

Tranzyme Pharma’s Ghrelin Agonist TZP-101 Shows Potential As a Potent Agent for Cancer Cachexia

October 16, 2008

Tranzyme Pharma, a biopharmaceutical company engaged in the discovery and clinical development of first-in-class small molecule therapeutics, announced that Dr. Helmut Thomas, Senior Vice President of Research and Preclinical Development will present results of a significant proof-of-concept study in cancer cachexia with its novel ghrelin agonist, TZP-101. The presentation will take place at the 20th EORTC-NCI-AACR Symposium on “Molecular Targets and Cancer Therapeutics” in Geneva, Switzerland on October 23, 2008.

In progressively-cachectic female BALB/c nu/nu mice bearing the aggressively-growing metastatic human G361 melanoma, TZP-101, administered subcutaneously, twice-daily, dose-dependently prevented weight loss, increased food and water intake, and, most impressively, increased mean survival time from 4 to 25 days in control and treated animals, respectively. These effects were accompanied by significant changes in clinical chemistry parameters indicative of a shift from the catabolic to the anabolic state. TZP-101 was superior to positive-control ghrelin peptide throughout the study. The ghrelin receptor has been associated with the proper regulation of appetite and the generation of a positive overall energy balance and, hence, agonism of this receptor is considered an attractive new approach for overcoming wasting disorders associated with severe illness, such as cancer cachexia.

“This is a fascinating result”, commented Dr. Thomas, “which may, once clinically confirmed, have a substantial impact on the quality of life of end-stage cancer patients and open up new horizons for extended cancer therapy with greatly increased chances for treatment success and cancer survival.”

TZP-101, Tranzyme’s intravenously-administered lead clinical product, has recently completed a successful international Phase IIb study for the management of postoperative ileus with plans for initiation of Phase III in the first quarter of 2009. A Phase IIb study of TZP-101 in gastroparesis is ongoing. TZP-102, an orally-available compound that shares the potent pro-kinetic attributes of TZP-101, is poised to enter Phase II clinical trials for selected additional indications.

About Cancer Cachexia

Cancer cachexia is a complex metabolic syndrome characterized by weight loss, anorexia, negative energy balance, and progressive loss of adipose tissue and muscle mass in patients with malignancies. This common syndrome has a profoundly negative impact on quality of life and limits the aggressiveness with which anti-cancer therapeutic regimens can be deployed. Approximately half of all cancer patients experience cachexia during treatment, affecting almost 100% as death approaches. Current therapeutic agents for cancer cachexia have highly limited efficacy.

About Tranzyme Pharma

Tranzyme Pharma is a clinical stage biopharmaceutical company engaged in the discovery and development of first-in-class small molecule therapeutics for the treatment of both acute care (hospital-based) and chronic indications with significant unmet medical needs.

Tranzyme has developed a pipeline of novel drugs through its proprietary MATCH(TM) drug discovery technology which accelerates the progression of compounds from discovery to commercial track by generating small molecule drug candidates that display the favorable characteristics exhibited by large biomolecules, such as tight receptor binding for high potency and exquisite target selectivity, while maintaining the benefits typically associated with small molecule drugs including oral bioavailability, cost of synthesis, and ease of formulation. For more information, please visit: www.tranzyme.com.