Oral Insulin

Insulin is an essential hormone for the regulation of carbohydrate metabolism. In contrast to injected insulin, oral insulin is delivered directly to the liver, its primary site of action, via portal circulation. The insulin delivered to the liver moderates hepatic glucose production, a major contributor to hyperglycemia in Type 2 diabetes. In theory, oral insulin should require less insulin per dose to produce the desired effect of reaching the liver. Furthermore, the amount of insulin that reaches the systemic circulation should be smaller and the peak shorter-lived than is the case with injectable insulin, thus reducing the chance of hypoglycemia.

Oral insulin could represent a significant opportunity for Emisphere and, in theory, would meet unmet market needs. However, realistically, at this stage in its development and based on what has been and perhaps what hasn't been done with this product candidate, it presents significant challenges. At this time, the Company is exploring its strategic options for the oral insulin compound. In particular, the Company's research indicates that GLP-1 may represent an opportunity for Emisphere. Rather than continuing to pursue oral insulin, the Company believes that a potentially more productive pathway is to move forward with GLP-1 and its analogs, an oral form of which might be used for Type 2 diabetes and other metabolic conditions.