Emisphere initiates clinical studies for oral insulin candidate

US biopharmaceutical company Emisphere Technologies is initiating clinical testing of an oral insulin formulation in type 2 diabetic patients in the US under an Investigational New Drug (IND) application filed with the FDA.

The formulation uses Emisphere's eligen oral drug delivery technology to deliver the insulin in a capsule. This is the first oral insulin clinical study in the US using Emisphere's technology.

The eligen technology, is based on the use of proprietary, synthetic chemical compounds, known as EMISPHERE delivery agents, or 'carriers'. These molecules facilitate the transport of the therapeutic macromolecules across biological membranes such as the small intestine.

The Phase I study is a single-blind, open-label cross-over study designed to assess the safety, tolerability and pharmacokinetics of Emisphere's oral insulin formulation with an EMISPHERE delivery agent in 12 type 2 diabetic patients. During the treatment phase, the oral insulin capsules will be administered after an overnight fast. Each subject will receive one of three treatments consisting of escalating doses of insulin and an EMISPHERE delivery agent, or a treatment of EMISPHERE delivery agent alone.

Previous studies with an unformulated oral insulin capsule showed peak plasma insulin concentrations within 20-25 minutes. This was significant in that it was an improvement in rate over the leading rapid-acting injectable insulin product. A rapid and consistent rate of absorption of a mealtime insulin could allow oral insulin to be administered closer to a meal, which is an important feature for increasing patient compliance.

Emisphere's oral insulin is said to best mimic the natural physiology of insulin release by travelling directly to the liver so that the rate and location of secreted insulin release are replicated. Orally delivered insulin potentially provides a therapeutically more effective alternative to existing medical treatments with fewer complications.