Tranzyme has discovered first-in-class small molecule therapeutics for the treatment of acute (hospital-based) and chronic gastrointestinal (GI) motility disorders with significant unmet medical need.

Tranzyme’s lead product candidates, ulimorelin and TZP-102, are the first small molecule ghrelin agonists to be developed specifically to improve multiple symptoms of upper gastrointestinal (GI) motility disorders. Pharmaceutical companies originally targeted ghrelin to treat growth hormone, or GH, deficiency disorders, such as short stature in children, but clinical trials in this area were unsuccessful. Most of these compounds had been optimized for their GH secretion properties, not their GI promotility activity. Tranzyme's compounds are from a completely new structural class, macrocycles, designed by them utilizing the Company's proprietary MATCH™ technology, not previously known to interact at the ghrelin receptor. Unlike the earlier ghrelin agonists, Tranzyme's compounds are highly selective and potent GI motility agents. 

Ulimorelin is an intravenous ghrelin agonist in Phase 3 clinical development for the accelertaion of GI recovery following abdominal surgery. Delayed GI recovery refers to the lack of GI motility after surgery before normal bowel function resumes. In addition, Tranzyme plans to evaluate the ability of ulimorelin to enhance recovery of GI function in patients suffering from other acute GI motility disorders, such as gastric stasis.

TZP-102 is an orally-administered ghrelin agonist in Phase 2 development for diabetic gastroparesis. Gastroparesis is a debilitating, chronic condition characterized by slow or delayed gastric emptying and gastric retention that can be caused by any disease that induces neuromuscular dysfunction of the GI tract, notably diabetes. Tranzyme intends to expand its development of TZP-102 in other chronic GI motility disorders as well.

In addition to the two clinical-stage candidates, 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.