Emisphere Technologies Inc. said Tuesday that its researchersearlier this month managed what is thought to be the first oraldelivery of an active monoclonal antibody (MAb) into thebloodstream of an animal.
The company said tests of its proprietary oral delivery system(ODS) showed that encapsulated compounds produced the samelevel of biological activity in rats as the same compoundsdelivered by injection -- although at necessarily higherdosages.
Emisphere researchers presented data Tuesday to theControlled Release Society, meeting in Orlando, Fla., from itsstudies comparing ODS to injection in administering the MAb,plus heparin and the influenza virus M-protein.
"We clearly proved we can orally deliver in a microcapsulationsystem equivalent amounts to what you can get with an IV,"Michael M. Goldberg, Emisphere's president and chief executiveofficer, said Tuesday. In the case of the MAb, about five timesthe dosage of an injection were needed for the ODS to achievematching biological activity, he said.
The variability of results among individual test animals was nogreater than what would be expected from administering a pillor capsule, Goldberg said. The test compounds were deliveredto the stomach through a feeding tube. The MAb was thelargest of the compounds tested, with a 150,000-daltonmolecular size, he said.
Still, the company's success improves the prospects for the oraldelivery of MAbs and smaller proteins, which would otherwisebe intravenously administered, Goldberg said. Drug-deliverytechnology has become a major issue in the effective use ofmany fragile biotechnology-based drugs.
A search of the scientific literature found "nothing to indicatethat anyone else has delivered an active MAb to thebloodstream through the oral route," Goldberg said. "It reallyproves the versatility of our system."
Emisphere's ODS is a patented technology for shieldingtherapeutic compounds in a microsphere encapsulationcomposed of amino acids. The microspheres are designed withthe goal of protecting their drug payloads from the harshgastrointestinal tract and delivering them unchanged into thebloodstream.
Emisphere of Hawthorne, N.Y., intends to submit the study'sresults for publication in a scientific journal, Goldberg said. Thecompany's stock (NASDAQ:EMIS) closed Tuesday at $18.25 ashare, up 25 cents.
Emisphere has research contracts with Sandoz PharmaceuticalCorp., Schering-Plough Corp., Upjohn Co. and Genetics Instituteto develop its ODS for use with various undisclosed compounds.
On its own, Emisphere is developing an ODS system for heparin,an anti-coagulant drug, which it aims to take into clinical trialsthis year in Europe. "We wanted to control one product so wecan prove the concept," Goldberg said.
-- Ray Potter Senior Editor
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