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Tranzyme Pharma’s
Ghrelin Agonist Demonstrates a Unique Selectivity Profile for
the Treatment of Gastrointestinal Disorders
Data Presented at the 20th International
Symposium on Neurogastroenterology & Motility
RESEARCH TRIANGLE PARK, N.C. and
SHERBROOKE, Québec (July 6, 2005) – Tranzyme Pharma Inc., a
leading biopharmaceutical company developing small molecule
therapeutics for the treatment of gastrointestinal (GI)
disorders, announced today new and exciting efficacy data for
TZP-101, the Company’s lead product for the treatment of
post-operative ileus and diabetic gastroparesis. TZP-101 is a
small molecule ghrelin receptor agonist, which has been shown to
selectively stimulate motility of the GI tract. In a
presentation at the 20th International Symposium on
Neurogastroenterology & Motility (Toulouse, France), Tranzyme
Pharma presented new in vivo data demonstrating that the potent
and selective gastroprokinetic activity of TZP-101 takes place
without the release of growth hormone.
Ghrelin is a peptide hormone known to stimulate both
gastrointestinal motility and growth hormone release. Tranzyme
Pharma has applied its proprietary chemistry technology to
dissociate these two aspects of ghrelin pharmacology resulting
in a product profile with selectivity for the treatment of
gastrointestinal disorders.
“Our discovery that TZP-101 effectively separates the
gastroprokinetic and endocrine effects of ghrelin is a
significant breakthrough in ghrelin receptor pharmacology,” said
Graeme L. Fraser, Ph.D., Vice President of Drug Discovery. “By
eliminating the growth hormone secretagogue aspects of ghrelin
receptor stimulation, we expect that TZP-101 will avoid
significant potential side-effects when it is used for chronic
therapeutic indications such as gastroparesis.”
“These data further validate the ability of Tranzyme Pharma’s
small molecule chemistry to design compounds with great
selectivity towards multimeric targets such as GPCRs, kinases
and ion channels,” said Lindsay N. Donald, DABT, Vice President
of Business and Preclinical Development. “Traditionally, this
sort of selectivity has only been possible with peptide or
protein therapeutics. Our chemistry technology allows us to
maintain the favorable binding characteristics of large
biomolecules while eliminating their drawbacks such as low oral
bioavailability, high manufacturing costs, and antigenicity.”
About the role of ghrelin in GI motility
Ghrelin is the most potent endogenous peptide known to stimulate
gastric motility. Recent independent clinical studies have
clearly demonstrated that infused ghrelin peptide potently
stimulates gastric emptying in both human volunteers and
diabetic gastroparesis patients. However, the ghrelin peptide
has limited utility as a therapeutic product for GI indications
due to its brief pharmacokinetic half-life, poor oral
bioavailability, and potent growth hormone-releasing activity.
About post-operative ileus (POI) and diabetic gastroparesis
POI is an impairment of gastrointestinal motility that is an
inevitable consequence of major abdominal surgery, especially
under conditions of bowel resection. POI has an annual economic
impact of $1.75 billion. There are no FDA-approved products for
the treatment of POI. Diabetic gastroparesis is the impairment
of stomach motility observed in both Type I and Type II
diabetics. Up to 10% of these patients require hospitalization
for nausea, vomiting abdominal pain and malnutrition. Existing
therapies for this condition offer poor efficacy and/or severe
side effects. TZP-101 is under development in both intravenous
and oral formulations for the treatment of these disorders.
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