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COMPANY HIGHLIGHTS

  First-in-class Therapeutics for Unmet Medical Needs

Tranzyme Pharma’s strategy is to use its unique drug discovery capabilities to find effective and safe drugs to treat diseases where there is a significant unmet medical need. Our business objectives are to continue to expand and solidify our drug discovery and development expertise in order to advance our high value drug candidates through the clinical development process and to make breakthrough mechanism-based therapeutics available to patients.

Tranzyme has launched two Phase IIb clinical trials to test the safety and efficacy of TZP-101, a ghrelin receptor agonist being investigated for the treatment of severe gastroparesis and post-operative ileus. TZP-101 has potent prokinetic properties that represent the first in its class to enter clinical trials. The FDA recently granted fast-track designation to TZP-101 for severe gastroparesis.

Tranzyme is also developing therapeutics to treat chronic gastroparesis, moderate-to-severe diarrhea, functional gastrointestinal disorders and obesity.



  Pipeline Focused on Key Validated Targets

Tranzyme Pharma is developing novel small molecule drugs targeting key validated receptors that regulate gastrointestinal motility, appetite and metabolism. These receptors include ghrelin (responsible for upper gut motility, appetite stimulation, and energy balance) and motilin (responsible for regulation of gastrointestinal transit).

The ghrelin receptor is considered a drug target of high interest in the pharmaceutical industry. Tranzyme’s ghrelin agonists, TZP-101 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 Drugs

Tranzyme’s pipeline of products originates from its proprietary Macrocyclic Template Chemistry (MATCH™). MATCH is a drug design and medicinal chemistry platform which exploits macrocycles, a distinct compound class. Tranzyme has created the first library of synthetic, low molecular weight macrocyclic molecules which has proven highly effective in drug target screening programs to supply novel chemical diversity along with necessary conformational control. We have demonstrated the ability to develop orally bioavailable small molecules from this chemistry, with particular success on GPCR targets. Our chemistry and R&D expertise can produce clinical candidates in a shorter time and more efficiently than current standard drug discovery approaches. This chemistry also has potential broad applicability in the treatment of other diseases that involve hormones, peptides or protein-protein interaction pathways.

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  Product Focused Business Strategy

Tranzyme’s objective is to build a pipeline of clinical stage drugs with multiple therapeutic opportunities. The Company has worked closely with academic clinical researchers and industry experts to design product development programs that address the typical hurdles of drug development in the GI therapeutic area. Tranzyme will develop these products to an optimal stage and then seek partnerships for further development and commercialization.

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