About Emisphere Technologies

Emisphere Technologies, Inc. operates as a commercial stage pharmaceutical and drug delivery company. The company is in partnership with global pharmaceutical companies to develop oral formulations of existing injectable bio-pharmaceutical products, as well as chemical entities, using its Eligen Technology. The company launched its first prescription medical food product, oral Eligen B12 in the U.S. in 2015, and it engages in strategic business collaborations discussions to optimize its economic value in the U.S. and global markets. Beyond Eligen B12, the company utilizes its proprietary Eligen Technology to create oral formulations of therapeutic agents. The company’s product pipeline includes prescription drug and medical food product candidates that are being developed in partnership or internally. The Eligen Technology The Eligen Technology is a proprietary oral drug delivery technology based on the use of proprietary synthetic chemical compounds known as Eligen delivery agents, or carriers. These carriers facilitate and enable the transport of therapeutic macromolecules (proteins, peptides, and polysaccharides) and poorly absorbed small molecules across biological membranes, such as those of the gastrointestinal tract. These molecules are delivered by injection, and in majority of cases their benefits are limited due to poor bioavailability, slow on-set of action or variable absorption. The Eligen Technology facilitates absorption and might improve bioavailability. Moreover, it acts in the upper sections of the gastrointestinal tract where absorption is thought to occur. Using Eligen Technology, majority of therapeutic macromolecules reach the general circulation in approximately an hour post-dose, which could limit enzymatic degradation that affects macromolecules. In the Eligen technology absorption takes place through a transcellular pathway, as opposed to passing between cells, preserving the integrity of the tight junctions within the cell walls and reducing the likelihood of inflammatory processes and autoimmune gastrointestinal diseases. Furthermore, Eligen Technology carriers are absorbed, distributed, metabolized and eliminated from the body, and they do not accumulate in the organs and tissues and are considered safe at anticipated doses and dosing regimens. The Eligen Technology could be applied to the oral route of administration, as well as other delivery pathways, such as buccal, rectal, inhalation, intra-vaginal or transdermal. Product Pipeline GLP-1 The company’s collaborative partner, Novo Nordisk, is using its Eligen Technology in combination with semaglutide, one of its proprietary GLP-1 receptor agonists, and its insulins. During 2015, Novo Nordisk initiated a global Phase 3a development program with oral semaglutide, a once daily oral formulation of the long-acting GLP-1 analog for the treatment of Type 2 diabetes, using its absorption-enhancing carrier, monosodium N-[8-(2-hydroxybenzoyl) amino] caprylate (SNAC carrier). Novo Nordisk initiated ten clinical trials containing approximately 9,300 patients with Type-2 diabetes in its global Phase 3a program. Novo Nordisk’s decision to initiate this global phase 3a program follows results from the proof of concept Phase 2 program and consultations with regulatory authorities. In February 2016, Novo Nordisk initiated the first Phase 3a trial or oral semaglutide, combined with its SNAC carrier. Novo Nordisk has initiated all 10 clinical trials, including PIONEER 6 (a pre-approval long term cardiovascular outcomes trial in approximately 3,100 subjects), PIONEER 8 (an insulin add-on trial in approximately 700 subjects), PIONEER 9 (a monotherapy trial in approximately 200 subjects) and PIONEER 10 (an oral anti-diabetic combination trial in approximately 300 subjects). Oral Eligen B12 The company is evaluating potential strategic transactions and collaborations with third parties for oral Eligen B12, which it launched in the U.S. in 2015. Oral Eligen B12 is a once-daily oral prescription medical food tablet shown to normalize B12 levels without the need for an injection. Eligen B12 meets significant unmet patient and medical needs by combining vitamin B12 with the company’s Eligen technology. Eligen B12 is indicated for the dietary management of patients who have a medically-diagnosed vitamin B12 deficiency, associated with a disease or condition that could not be managed by a modification of the normal diet alone. Eligen B12 is the first prescription product to market using an Eligen carrier, SNAC, to chaperone B12 through the gastric lining and directly into the bloodstream independent of intrinsic factor, a protein made in the stomach that normally facilitates B12 absorption. Preclinical Programs In 2015, the company entered into a development and license agreement with Novo Nordisk to develop and commercialize oral formulations of four classes of Novo Nordisk’s investigational molecules targeting major metabolic disorders, including diabetes and obesity, using its oral Eligen Technology. Under the terms of the Expansion License Agreement, the company licensed to Novo Nordisk the right to develop potential product candidates in three molecule classes, and the non-exclusive right to develop potential product candidates in a fourth molecule class, using the Eligen Technology. Novo Nordisk is responsible for the development and commercialization of all product candidates. In addition, the company granted Novo Nordisk the option to obtain exclusive and non-exclusive rights to develop and commercialize oral formulations of additional investigational molecules for the treatment of diabetes, obesity, and indications in other important therapeutic areas using the Eligen Technology. Strategy The company’s core business strategy is to build new, high-value partnerships and continue to expand upon existing partnerships, optimize Eligen B12’s economic value to shareholders, evaluate commercial opportunities for new prescription medical foods, and promote new uses for its Eligen Technology, a broadly applicable proprietary oral drug delivery platform, which makes it possible to avoid injections for drug administration. Patents and Other Forms of Intellectual Property As of March 1, 2017, the company had been granted approximately 120 U.S. patents and approximately 200 foreign patents. It also has approximately 25 pending U.S. patent applications, as well as approximately 150 counterpart applications pending in foreign countries. The company has five trademarks registered with the U.S. Patent and Trademark Office. They include three registrations for Emisphere in connection with drug delivery agents and research and development in the field of drug delivery systems, and two registrations for ELIGEN in connection with drug delivery agents and research and development in the field of drug delivery systems. Government Regulation The company’s operations and product candidates under development are subject to extensive regulation by the FDA, other governmental authorities in the U.S. and governmental authorities in other countries. History The company was founded in 1985. The company was incorporated as Clinical Technologies Associates, Inc. under the laws of Delaware in 1986 and changed its name to Emisphere Technologies, Inc. in 1991.