The Haystack wanted to point readers to a nice piece on oral delivery strategies for biotherapeutics by our colleague Ann Thayer. An injection or IV drip may be perfectly reasonable for diseases like cancer, where drugs are usually given in a hospital setting, but for chronic diseases like diabetes or multiple sclerosis, which require daily or weekly injections, a pill would be much more palatable. That said, it is awfully tough to get effective oral delivery of a big, unwieldy protein. As Thayer writes, “Acids and enzymes in the gastrointestinal tract will chew up a valuable therapeutic protein as easily as they’ll tear into a bite of steak.”
Companies are especially keen to develop alternative delivery solutions for insulin. Not only would it represent a major advance for patients, but the market for a better-acting and easier-to-use insulin would be gigantic—insulin sales account for about $15 billion of the global diabetes market. Attempts at inhaled insulin have been a colossal failure. Thayer goes on to describe some of the methods biotech companies are using to enable oral delivery of insulin. Among the players:
–India’s Biocon is developing IN-105, an insulin molecule conjugated to a short-chain polyethylene glycol derivative. The technology was originally developed at N.C.-based Nobex, which Biocon bought in 2006.
–Ireland’s Merrion Pharmaceuticals is using technology acquired from Elan Corp. to enhance gastrointestinal permeation. In 2008, the company began working with Novo Nordisk on solid oral forms of insulin analogs; the first such analog was put into Phase I trials by Novo in late 2009.
–N.J.-based Emisphere Technologies is working with Novo Nordisk on GLP-1 analogs. In January, Novo started a Phase I trial of the first candidate using Emisphere’s Eligen technology.
–Isreal’s Oramed is using capsules with an enteric coating, which controls where in the intestinal tract a pill is absorbed. A Phase IIb trial of ORMD-0801 conducted in South Africa showed the drug to be safe and to have a clinical impact on insulin and gluose levels. Oramed hopes to do a Phase II study in the U.S. late this year.
–Dallas-based Access Pharmaceuticals is using insulin-containing nanoparticles coated with vitamin B-12 analogs, which pull the complex into circulation.
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