Eligen(R) B12 oral formulation demonstrates 240% improvement in
bioavailability versus standard oral Vitamin B12 tablet and different
absorption characteristics
Eligen(R) B12 absorption time was 30 minutes
- Public Conference Call to discuss results and future direction set
for July 29 -
CEDAR KNOLLS, N.J., July 28 /PRNewswire-FirstCall/ -- Emisphere
Technologies, Inc. (Nasdaq: EMIS) today announced new human clinical data
demonstrating a new, more bioavailable oral form Vitamin B12 and a
potential new avenue for addressing the problems with B12 supplementation.
As demonstrated by the data, the Eligen(R) B12 formulation avoids the
normal specialized absorption process that limits absorption of Vitamin B12
from current formulations.
"By circumventing the current absorption process, Eligen(R) B12 may
present an opportunity to reduce the potential uncertainty associated with
oral megadoses of Vitamin B12 and may prevent dependence on the substantial
number of injections being taken by millions of individuals," said Michael
V. Novinski, President and Chief Executive Officer of Emisphere.
Emisphere's pharmacokinetic study was conducted with 20 healthy male
subjects divided into four groups - four subjects received 5mg B12
intravenously, four subjects received 10mg Eligen(R) B12, six subjects
received 5mg Eligen(R) B12 and six subjects received a commercially
available 5mg B12 tablet. "The 10mg Eligen(R) group served essentially as a
pilot group to determine appropriate measurements and assess our protocol,"
said Gary Riley, DVM, Ph.D., Vice President of Nonclinical Development and
Applied Biology at Emisphere. "Following these results, we reduced the
amount administered by 50% to a level that is being used in certain
commercially available formulations. We expect to be able to reduce the
dose further based on the data we have received, including the linear
relationship that appears between the two Eligen(R) groups."
Mean Vitamin B12 peak blood levels were more than 10 times higher for
the Eligen(R) B12 5mg formulation than for the 5mg commercial formulation
(12847 pg/ml and 1239 pg/ml, respectively). The time to reach peak
concentration (Tmax) was reduced by over 90%; the mean was 0.5 hours for
the Eligen(R) B12 5mg and 6.8 hours for the commercial 5mg product. Mean
AUC_(24h) values were 54618 for Eligen(R) B12 and 23131 for the commercial
5mg product. Improvement in bioavailability was approximately 240%, with
absorption time at 30 minutes and a mean bioavailability of 5%. The study
was conducted with a single administration of Vitamin B12; there were no
adverse reactions, and Eligen(R) B12 was well-tolerated.
"These data hold real promise for improving the way we approach Vitamin
B12 supplementation, including maintenance of adequate Vitamin B12 status
in individuals at risk or already defined as B12 deficient," Donald W.
Jacobsen, Ph.D., Staff, Cleveland Clinic and Professor of Molecular
Medicine, Case Western Reserve University "In these populations we can
expect the differences between the Eligen(R) B12 and the regular oral
formulations to be greater as this study was performed in healthy male
volunteers."
This human study follows a number of animal studies that also indicated
the advantages of the Eligen(R) Technology when applied to a poorly
absorbed but essential nutrient such as Vitamin B12. "Emisphere is
committed to further demonstrating the value of the Eligen(R) Technology
and commercializing it, especially for restoring B12 levels in those at
risk, those who are identified as deficient, and for people who are
genuinely concerned about this significant and essential vitamin," said Mr.
Novinski. "Furthermore, this data clearly show how broadly the Eligen(R)
Technology can be applied and how it serves as a solution to hurdles with
difficult to absorb molecules, whether they are prescription drug products
or essential minerals and nutrients."
Currently, it's estimated that five million people in the United States
are taking 40 million injections of B12 per year to treat a variety of
debilitating medical conditions (as noted above). Another estimated five
million are consuming more than 600 million tablets of B12 orally.
Emisphere's broad-based delivery technology platform, known as the
Eligen(R) Technology, uses proprietary, synthetic chemical compounds, known
as Emisphere delivery agents, sometimes called carriers. Emisphere's
Eligen(R) Technology makes it possible to deliver a target molecule
(vitamin, therapeutic drug, etc.) without altering its chemical form or
biological integrity.
CONFERENCE CALL
A teleconference to discuss these data further will be held on Tuesday,
July 29, 2008 at 10:00 AM EDT. A live webcast of the conference call can be
accessed through the company's Web site at: http://www.emisphere.com. The live
conference call dial-in number is: 1-800-895-0198 (United States and
Canada) or 1-785-424-1053 (International).
ABOUT EMISPHERE
Emisphere Technologies, Inc. is a biopharmaceutical company that
focuses on a unique and improved delivery of target molecules and
pharmaceutical compounds using its Eligen(R) Technology. Some of these
molecules or compounds can only be given by injection; when combined with
our technology; convenient oral versions may be safe, effective and provide
significant advantages. The benefits of other compounds are limited due to
poor bioavailability, slow on-set of action or variable absorption. In
those cases, use of Emisphere's technology can improve the therapeutic
effectiveness of the compounds. The Eligen(R) Technology can be applied to
the oral route of administration as well other delivery pathways. The web
site is: http://www.emisphere.com.
Safe Harbor Statement Regarding Forward-looking Statements
The statements in this release and oral statements made by
representatives of Emisphere relating to matters that are not historical
facts (including without limitation those regarding the timing or potential
outcomes of research collaborations or clinical trials, any market that
might develop for any of Emisphere's product candidates and the sufficiency
of Emisphere's cash and other capital resources) are forward-looking
statements that involve risks and uncertainties, including, but not limited
to, the likelihood that future research will prove successful, the
likelihood that any product in the research pipeline will receive
regulatory approval in the United States or abroad, the ability of
Emisphere and/or its partners to develop, manufacture and commercialize
products using Emisphere's drug delivery technology, Emisphere's ability to
fund such efforts with or without partners, and other risks and
uncertainties detailed in Emisphere's filings with the Securities and
Exchange Commission, including those factors discussed under the caption
"Risk Factors" in Emisphere's Annual Report on Form 10-K (file no. 1-10615)
filed on March 17, 2008 and our Quarterly Report on Form 10-Q for the
quarter ended March 31, 2008, filed on May 7, 2008.
SOURCE Emisphere Technologies, Inc.
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Related links:
http://www.emisphere.com
CONTACT:
Bob Madison, Senior Director Corporate
Communications of Emisphere Technologies, Inc., +1-973-532-8001,
bmadison@emisphere.com; or Adam Friedman of Adam Friedman
Associates for Emisphere Technologies, Inc., +1-212-981-2529,
extension 18, adam@adam-friedman.com
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