First-in-class Therapeutics for Unmet Medical Needs

Tranzyme is a clinical-stage biopharmaceutical company focused on discovering, developing and commercializing novel, first-in-class small molecule therapeutics for the treatment of acute (hospital-based) and chronic gastrointestinal (GI) motility disorders. GI motility disorders are conditions which disrupt the normal movement of food throughout the GI tract. Tranzyme’s two most advanced product candidates, ulimorelin, which is in Phase 3, and   TZP-102, which is entering Phase 2b, are being evaluated for the treatment of predominantly upper GI motility disorders. Approximately 20 percent of adults worldwide are affected by conditions these product candidates are designed to treat. While upper GI motility disorders are a highly prevalent group of persistent and recurring conditions, there are currently a limited number of treatment options for patients suffering from these conditions.

In addition to ulimorelin and TZP-102, Tranzyme is also developing a motilin antagonist, TZP-201, for the treatment of various forms of moderate-to-severe diarrhea, and a ghrelin antagonist, TZP-301, for the treatment of obesity and other metabolic diseases.

Pipeline Focused on Key Validated Targets

Tranzyme’s current pipeline of drug candidates targets two key validated receptors, ghrelin and motilin, which regulate GI motility, appetite and metabolism. The ghrelin receptor is responsible for upper gut motility, appetite regulation and energy balance. The motilin receptor is associated with the general regulation of gastrointestinal transit.

Tranzyme's ghrelin agonists, ulimorelin and TZP-102, have been uniquely optimized for their GI activity and are potential breakthrough blockbuster drugs. Ghrelin agonists are considered one of the most exciting new drug prospects by gastroenterologists and leading clinical experts have expressed a high degree of interest in them.

Likewise, the motilin receptor has been identified as a key pharmaceutical target for GI disorders due to its critical regulatory role in the GI physiological system where it governs fasting motor activity. This receptor controls gastric motility by inducing the contraction of gastrointestinal smooth muscle thereby decreasing intestinal transit time and initiating phase III of the migrating motor complex (MMC) in the small bowel. However, to date, the development of small molecule therapeutic agents designed to effectively modulate this receptor has proven elusive. Motilin antagonists in particular would be quite useful in treating GI diseases characterized by hypermotility. Tranzyme's motilin antagonist, TZP-201, has demonstrated efficacy in multiple animal models of disease, including chemotherapy-induced diarrhea and functional GI disorders.

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Products Based on Proprietary Macrocyclic Technology

Tranzyme’s pipeline of products originates from its proprietary Macrocyclic Template Chemistry (MATCH™) technology platform, which enables the construction of synthetic libraries of drug-like, macrocyclic compounds in a predictable and efficient manner. MATCH™ is a drug design and medicinal chemistry platform which exploits the potential of macrocycles, a distinct compound class that displays the favorable characteristics exhibited by large biomolecules, while maintaining the benefits typically associated with small molecule drugs. Outside of Tranzyme's current development focus, MATCH™ has broad applicability in the treatment of other diseases that involve hormones, peptides, ion channels, or protein-protein interaction pathways.

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Product Focused Business Objective and Strategy

Tranzyme’s objective is to develop and bring to market products to treat acute and chronic GI motility disorders that are not satisfactorily or safely treated with current therapies and that represent significant market opportunities.

Tranzyme's strategy is to license certain rights to its drug development programs once proof of concept in man is achieved, or when a program may benefit from the research, development and commercialization capabilities of a partner. Through these strategic partnerships, Tranzyme intends to balance risk while preserving the potential for significant returns.