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. 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: 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: 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.
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
Web site: http://www.emisphere.com/
