Emisphere Technologies, Inc. Reports Clinical Data on Oral Delivery of GLP-1 and PYY

Study shows orally-delivered GLP-1 is able to stimulate insulin release
Results to be published in peer-reviewed journal
Proof of concept efficacy study on reduction of food intake planned for 2007

TARRYTOWN, NY, USA | Mar 29, 2007 |
Emisphere Technologies, Inc. (Nasdaq: EMIS) reported today results of two clinical studies conducted in collaboration with Professor Christoph Beglinger, M.D. Division of Gastroenterology and Hepatology, University Hospital Basel in Basel, Switzerland. The objective of the study with glucagon-like peptide-1 (7-36 amide) (GLP-1) was to establish the initial pharmacological profile and the insulin releasing activity of increasing oral doses of GLP-1 in healthy volunteers. In addition, the pharmacokinetic effects of GLP-1 were investigated after intravenous administration. The objective of the study with peptide YY 3-36 (PYY) was to establish the PYY plasma concentrations following increasing oral doses of the peptide.

The results showed that Emisphere's eligen(R) technology can orally deliver the incretin hormones GLP-1 and PYY. The oral administration of both peptides induced a rapid and dose-dependent, statistically significant increase in plasma drug concentrations (p<0.05) at all doses tested versus placebo. Additionally, the orally delivered GLP-1 induced a statistically significant effect on insulin release in all healthy male volunteers (p<0.05) at all doses tested versus placebo. The Company expects these results to be published in a leading peer-reviewed scientific journal later this year.

GLP-1 was given orally to six healthy male subjects in a six way cross-over design. The treatment arms consisted of oral doses of GLP-1 (0.5, 1.0, 2.0 and 4.0 mg of drug) with Emisphere's delivery agent administered as a single tablet versus placebo. Only one dose was given per day. On a separate day, subjects received an intravenous infusion of GLP-1 (0.4 pMol/kg/min infused for 45 minutes). Blood samples were obtained for GLP-1 and insulin concentrations. The Cmax plasma concentration for the 4 mg oral dose of GLP-1 was 300 pMol/L.

In the PYY study, the drug was given orally to six healthy male subjects in a six way cross-over design. The treatment arms consisted of oral doses (0.25, 0.5, 1.0, 2.0 and 4.0 mg) of PYY with Emisphere's delivery agent administered as a single tablet versus placebo. The Cmax value of PYY for the 4 mg oral dose had a plasma concentration of 629 pg/ml. In addition, there was a reduction of Ghrelin in all groups administered PYY with the largest percent reduction in Ghrelin levels observed in the 4 mg PYY dose.

"This study showed for the first time that GLP-1 was active with regard to stimulation of insulin releases in humans after oral administration. In the subjects receiving the highest doses of oral GLP-1, we observed nausea effects similar to those seen when the subjects received high levels of injectable GLP-1. The biodynamic results on insulin release and blood concentrations indicate that oral GLP-1 could be an effective treatment in diabetes. The PYY results in combination with the GLP results could mean that oral PYY and oral GLP-1 could also be an effective treatment for other diseases such as obesity. We will seek to publish these results," said Dr. Christoph Beglinger of the University Hospital in Basel.

"We are very pleased to be working on the oral delivery of GLP-1 and PYY with a leading academic researcher such as Dr. Beglinger in the field of gastroenterology. The compounds GLP-1 and PYY are gastrointestinally produced hormones and GLP-1 is already an important compound in the treatment of diabetes as an injectable agent. Non-oral forms of these compounds are being explored in the treatment of obesity. We are looking forward in 2007 to initiating and completing a proof-of-concept efficacy study on the reduction of food intake using our oral incretin products with Dr. Beglinger," said Lewis H. Bender, President and CEO of Emisphere Technologies, Inc.

About GLP-1

Glucagon-like peptide-1 is synthesized in intestinal endocrine cells in two principal major molecular forms, as GLP-1(7-36) amide and GLP-1(7-37). The peptide was first identified following the cloning of cDNAs and genes for proglucagon in the early 1980s. The main target of action of glucagon-like peptide-1 (GLP-1) is the islet, where the hormone stimulates insulin secretion, promotes beta cell proliferation and neogenesis, and inhibits glucagon secretion. However, GLP-1 receptors are also expressed outside the islets, increasing the likelihood that GLP-1 also plays a role in other organs. These functions are mainly the inhibition of gastric emptying, gastric acid secretion and exocrine pancreatic secretion, indicating that the hormone acts as an enterogastrone -- a hormone released from the distal portion of the small intestine that inhibits proximal gastrointestinal events. Another important action of GLP-1 is to induce satiety.

About PYY

Peptide YY 3-36 is produced by the gut and is released into the circulation in response to food ingestion. Food intake is regulated by the hypothalamus, including the melanocortin and neuropeptide Y (NPY) systems in the arcuate nucleus. The NPY Y2 receptor (Y2R), a putative inhibitory presynaptic receptor, is highly expressed on NPY neurons in the arcuate nucleus, which is accessible to peripheral hormones. Peptide YY 3-36, a Y2R agonist, is released from the gastrointestinal tract postprandially in proportion to the calorie content of a meal. It is believed that PYY may be an important regulator of food intake.

About Diabetes

According to statistics provided by the World Health Organization and the American Diabetes Association, approximately 177 million people worldwide are afflicted by diabetes, with approximately 18 million of those afflicted residing in the United States. Nearly one-third of all individuals in the United States suffering from diabetes are unaware that they have this chronic disease. Type 2 diabetics account for approximately 90-95% of diabetes cases. According to the publicly filed annual reports of leading insulin manufacturers, worldwide sales of insulin were approximately $5.6 billion in 2004. Currently, there are no approved insulin therapies in oral form.

About Obesity

Obesity is a complex, multi-factorial chronic disease involving environmental (social and cultural), genetic, physiologic, metabolic, behavioral and psychological components. It is the second leading cause of preventable death in the U.S. According to the American Obesity Association approximately 127 million adults in the U.S. are overweight, 60 million obese, and 9 million severely obese. Body Mass Index (BMI) is a measurement tool used to determine excess body weight. Overweight is defined as a BMI of 25 or more, obesity is 30 or more, and severe obesity is 40 or more. Obesity increases the risk of illness from about 30 serious medical conditions. Overweight or obese individuals experience social stigmatization and discrimination in employment and academic situations.

About Emisphere Technologies, Inc.

Emisphere Technologies, Inc. is a biopharmaceutical company pioneering the oral delivery of otherwise injectable drugs. Emisphere's business strategy is to develop oral forms of injectable drugs, either alone or with corporate partners, by applying its proprietary eligen(R) technology to those drugs or licensing its eligen(R) technology to partners who typically apply it directly to their marketed drugs. Emisphere's eligen(R) technology has enabled the oral delivery of proteins, peptides, macromolecules and charged organics. Emisphere and its partners have advanced oral formulations or prototypes of salmon calcitonin, heparin, insulin, parathyroid hormone, human growth hormone and cromolyn sodium into clinical trials. Emisphere has strategic alliances with world-leading pharmaceutical companies. For further information, please visit the Emisphere website, http://www.emisphere.com.

Safe Harbor Statement Regarding Forward-looking Statements

The statements in this release and oral statements made by representatives of Emisphere relating to matters that are not historical facts (including without limitation those regarding the timing or potential outcomes of research collaborations or clinical trials, any market that might develop for any of Emisphere's product candidates and the sufficiency of Emisphere's cash and other capital resources) are forward-looking statements that involve risks and uncertainties, including, but not limited to, the likelihood that future research will prove successful, the likelihood that any product in the research pipeline will receive regulatory approval in the United States or abroad, the ability of Emisphere and/or its partners to develop, manufacture and commercialize products using Emisphere's drug delivery technology, Emisphere's ability to fund such efforts with or without partners, and other risks and uncertainties detailed in Emisphere's filings with the Securities and Exchange Commission, including those factors discussed under the caption "Risk Factors" in Emisphere's Annual Report on Form 10-K (file no. 1-10615) filed on March 5, 2007.

SOURCE Emisphere Technologies, Inc.

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