Emisphere’s broad-based oral drug delivery technology platform, known as the eligen^® technology, is based on the use of proprietary, synthetic chemical compounds, known as EMISPHERE^® delivery agents, or “carriers.” These delivery agents facilitate or enable transport of therapeutic macromolecules across biological membranes such as those of the gastrointestinal tract, allowing the therapeutic molecules to exert their desired pharmacological effect. The delivery agents have no known pharmacological activity themselves at the intended clinical dose levels. Emisphere’s eligen^® technology makes it possible to orally deliver a therapeutic molecule without altering its chemical form or biological integrity.

Proposed Delivery Agent Mechanism
Drug molecules exist in many different shapes, or “conformations”. Some conformations can be transported across the cell membranes while others are too large or too charged to do so. The eligen^® technology uses the body’s natural passive transcellular transport process to enable large or highly charged molecules to cross cell membranes. Once the drug molecule crosses the membrane, the EMISPHERE^® delivery agent dissociates from the drug molecule, which then reestablishes its natural conformation and returns to its therapeutically active state. Studies have shown that this process does not involve chemical modification of the drug molecule and the integrity of cell membrane and cytoskeletal structure are maintained.

The eligen^® Library
Emisphere has designed and synthesized a library of approximately 4,000 EMISPHERE^® delivery agents. These carrier molecules vary in their chemical structure, solubility, hydrophobicity, electrostatic and other physical and chemical properties. Through a rational scientific process, Emisphere can identify, select and customize carriers to facilitate the oral delivery of a broad range of therapeutic agents. Using this technology, Emisphere has demonstrated oral delivery in humans of unfractionated heparin, low molecular weight heparin, insulin, PTH 1-34, human growth hormone, cromolyn, salmon calcitonin and a small molecule for the treatment of bone disease. Emisphere has demonstrated also oral delivery of over 60 other compounds in animal models.

View Proposed Delivery Agent Mechanism