Oral Vitamin B12Vitamin B12 is poorly absorbed by relatively normal, healthy people. Many older people lose their natural ability to absorb this important nutrient. Younger people may also have difficulty absorbing B12 as a result of taking certain widely-used medications, chemotherapy, or for many other reasons. Vitamin B12 deficiency is a significant health issue. Nearly 40 percent of the U.S. population has been estimated to be B12 deficient (Tufts University, Boston). This includes a sizable number of patients who are severely deficient and are being treated for anemia and other conditions. Further, many people are unaware that they are B12 deficient and will likely eventually need treatment. It is estimated that five million people in the United States take 40 million injections of B12 per year to treat a variety of debilitating medical conditions. Another estimated five million consume more than 600 million tablets of B12 orally. We believe that the worldwide market is likely to be double these numbers. Recent studies suggest that the prevalence of B12 deficiency in young adults may be greater than previously thought. Some medications may also decrease absorption of Vitamin B12. Among the most serious repercussions of B12 deficiency is pernicious anemia. Other health problems associated with B12 deficiency include fatigue, weakness, loss of appetite, neurological changes such as numbness and tingling in the hands and feet, confusion, and dementia. Preclinical studies suggest that oral delivery of Vitamin B12 using the Eligen® Technology will be more efficient, more convenient and less costly than B12 injections. In early February 2008, Emisphere announced the results of animal studies that demonstrated proof of concept that absorption of oral Vitamin B12 using its technology was 15-30 times greater than with the same dose of oral Vitamin B12 administered alone. In March 2008, the Company released the results of a second phase of its animal studies demonstrating that its proprietary technology enhanced the absorption of oral B12 at considerably lower doses than the previous study and at levels that are likely to be more physiologically relevant. Confirming the original proof-of-concept study, overall absorption of B12 using Emisphere's technology was 18 times greater than with the same dose administered alone. Absorption time also improved - from 24-36 minutes vs. 72 minutes alone. In April 2008, Emisphere reported that it had completed preclinical studies in dogs that confirmed the increased absorption of Vitamin B12 and the Eligen® Technology. Emisphere announced new human clinical data in July 2008 demonstrating that the Eligen® B12 formulation avoids the normal specialized absorption process that limits absorption of Vitamin B12 from current formulations. By circumventing the current absorption process, Eligen® 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. Emisphere's pharmacokinetic study demonstrated that mean Vitamin B12 peak blood levels were more than 10 times higher for the Eligen® 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® B12 5mg and 6.8 hours for the commercial 5mg product. Mean AUC_(24h) values were 54618 for Eligen® 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® B12 was well-tolerated. Emisphere anticipates a number of important milestones for oral B12, including:
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