NEW YORK, Jan 13 (Reuters Health) -- The successful use of a particular
protein in an oral rather than injected or inhaled form is an important first
step towards making oral drug treatments available for more diseases, report US
scientists.
Proteins are broken down by stomach acids, so taking some drugs by mouth,
such as the blood-thinning drug heparin or hormones such as insulin or
calcitonin, have not been possible.
But this week, Novartis Pharma and Emisphere Technologies, Inc. announced
the successful use of a solid, oral form of calcitonin utilizing Emisphere's
drug delivery technology.
According to an Emisphere statement, results from the study demonstrated
that therapeutic blood levels of calcitonin were achieved using the new method,
indicating that the active form of the drug had not been broken down by stomach
acids. The study of 20 healthy people conducted in the UK was designed to
determine the safety and efficacy of the drug delivery system.
In an interview with Reuters Health, Emisphere Chairman and CEO Dr.
Michael Goldberg said that the results were significant because "it is the first
time, we believe, that anyone has ever orally delivered a protein (drug) in
which they didn't damage the protein or damage the patient as a result of the
delivery."
He said that the results prove "unequivocally that oral protein delivery
is possible, has been accomplished and is commercializable." He noted that
calcitonin has been around for several decades and researchers already know that
it works for treatment of osteoporosis.
Novartis holds an option, which expires in March 2000, to license
exclusive development and commercialization rights for oral calcitonin utilizing
Emisphere's technology. Goldberg told Reuters Health that he expects that
Novartis would exercise the option and that they have expressed significant
interest and have invested significant amounts of money on early development of
the product.
According to Tarrytown, New York-based Emisphere, annual worldwide sales
of salmon calcitonin, which is a synthetic version of the natural hormone, is
estimated to be in excess of $800 million.
Goldberg noted that the company's oral heparin product in liquid form is
also currently being studied. As reported by Reuters Health last August, the
product demonstrated comparable safety and activity to subcutaneous injections
of heparin in studies. Goldberg told Reuters Health at that time that the study
proved for the first time that an orally delivered macromolecule could provide
comparable safety and activity.
The company is currently negotiating marketing rights for the oral heparin
product. Goldberg said that the company hopes to file for Food and Drug
Administration marketing approval for oral heparin in the second half of 2001.
