Tranzyme’s TZP-102 is a Ghrelin receptor agonist designed for treatment of Gastroparesis in diabetic patients. Phase IIb trials are currently underway to further test it’s efficacy.

Ghrelin is a hormone that is generated within the walls of the stomach. It’s mainly responsible for the feeling of hunger along with helping to gear up the digestive system for food intake. Leptin is another digestive hormone that is almost the opposite of  Ghrelin in that it promotes feelings of satiety & lowers appetite. Those with Gastroparesis often have problems with loss of appetite & early feelings of fullness along with nausea & vomiting. While it’s known that usually a loss of digestive motility is the reason for these symptoms, it is not often known where the loss of motility came from. In some cases motility is not an issue, yet symptoms remain.  It is possible that those suffering from Gastroparesis may be dealing with an underproduction of Ghrelin or an overproduction of Leptin. It is also possible that these hormone levels are fine but some other issue exists like nerve or muscle damage. Regardless of the cause, increasing production of Ghrelin may be beneficial to those dealing with Gastroparesis as it may allow the digestive system to regain some lost motility while improving appetite & reducing feelings of fullness.

Tranzyme’s TZP-102 is a Ghrelin receptor agonist. It’s goal is to coax the body to produce more of the Ghrelin hormone. It is currently listed as being designed for the treatment of diabetes related Gastroparesis. I personally think this labeling of the drug might have been a tactic to receive fast track status from the FDA. I would not be surprised if doctors later prescribe it “off label” for those who do not have diabetes, if TZB-102 makes it to market.

The Phase IIb trials of TZP-102 will be looking to test efficacy of 10mg, 20mg & placebo dosages. In September 2011 Tranzyme released information from a study done at Aarhus University Hospital in Denmark which suggested promising early results.

  • Oral administration of TZP-102 for 28 days significantly improved gastroparesis symptoms;
  • The observed effects were similar in type 1 and type 2 diabetic patients;
  • TZP-102 was well tolerated with no impact on body weight or glucose control parameters; and
  • Overall, TZP-102 represents a promising pharmacological option to address an unmet medical need for patients whose day-to-day life is impaired by gastroparesis.

Tranzyme is not alone in their attempts to use Ghrelin to treat Gastroparesis, although they appear to be the furthest along. Rhythm Pharmaceuticals is working on RM-131, another Ghrelin agonist. Meanwhile GalaxoSmithKline is working on GSK962040 which is a Motilin agonist. Motilin is another digestive hormone, similar to Ghrelin.

Sources: Tranzyme Press Releases 611224 & 604457