Oral Insulin Effective in Early Trial
Oral Insulin Effective in Early Trial
By Deena Beasley
LOS ANGELES (Reuters) - An early-stage clinical trial of an oral form of insulin shows that it is safe and effective, Emisphere Technologies Inc. (Nasdaq:EMIS - news), the maker of the experimental capsule, said on Friday.
Tarrytown, New York-based Emisphere said the trial, the first of three Phase I trials of its method for delivering insulin orally by changing its molecular shape, produced a therapeutic response that was comparable to what was observed in a typical subcutaneous dose of insulin.
``The fundamental problem with oral delivery of insulin is how to get across the intestinal membrane. What we have done is take advantage of the chemical fact that if you change a molecule's shape, you change its activity,'' Michael Goldberg, the company's chief executive, told Reuters.
Emisphere uses a ``carrier'' molecule to keep insulin, which is a protein, in a fat-soluble state inside its delivery capsule, but allows it to fold into a water-soluble shape once it is digested, the CEO explained.
Insulin is a hormone produced by the pancreas that helps convert food into energy. In diabetes, affecting about 16 million Americans, the body is unable to produce or properly use insulin, resulting in too much sugar in the blood.
Currently, insulin is usually administered as an injection, but it is also delivered through infusion pumps and inhaled forms have been tested in advanced clinical trials.
Worldwide insulin sales total about $3.5 billion annually, according to IMS Health Inc., which tracks drug sales.
Goldberg said Emisphere's oral form is quicker-acting than other types of insulin, achieving peak levels about 20-25 minutes after administration, compared with 100 minutes for a typical injection or 40-45 minutes for faster-acting injected insulins or inhaled formulations.
He said the experimental product may offer a replacement to insulin injections before meals for people with Type 1, or juvenile onset, diabetes. ``If we can do the heavy lifting, the insulin in the pancreas can be conserved,'' Goldberg said.
Less of Emisphere's orally-delivered insulin is absorbed by the bloodstream than is the case with subcutaneous injections, which have absorption rates of 30-80 percent, but the exact amount is unknown because much of the oral insulin is directly absorbed into the liver rather than into the circulatory system, the CEO said.
``Whatever is not absorbed is treated like sushi. Insulin is an active protein that gets rapidly digested,'' Goldberg said.
Questions have arisen about the safety of experimental inhaled forms of insulin after reports of pulmonary fibrosis, or scarred lung tissue, in a small number of clinical trial patients. ``They have a problem we don't have, in that the excess insulin is still active in the lungs and it may cause inflammation,'' Goldberg said.
The CEO said Emisphere wants to bring in a major pharmaceutical company -- one with either an insulin or diabetes product franchise -- to help it move forward with clinical trials and drug development.
He said there have so far been no negative side effects associated with Emisphere's oral insulin product.
The 12-patient trial was conducted by Hadassah University in Israel. Emisphere also conducted an eight-patient Phase 1 trial in The Netherlands and a third trial of 10 patients in the United Kingdom
