Zinc Carnosine A New Peptic Ulcer Treatment

At the intersection of research and intellectual property commercialisation is Nutracon's tech transfer forum. It brings together buyers and sellers of proprietary and technology-based product opportunities.

From mass-scale food and supplement innovation to niche technology applications, tech transfer is packed with potentially exclusive product development opportunities. Business development executives, licensing and new product development managers find competitive advantages in the presentations. The following is one example of the Nutracon tech transfer's science, technology, intellectual property and licensing opportunities.

Peptic ulcer disease and nonulcer dyspepsia (NUD) wreak havoc on millions of individuals worldwide. They are a source of morbidity and expense from over-the-counter (OTC) and prescription drugs, diagnosis and treatment.

One of the prime causative factors of ulcers, both in the stomach and upper small intestine, is the spiral-shaped bacterium Helicobacter pylori. More than 75 per cent of people with gastric ulcers are infected with H. pylori. Infected humans (estimated to be at least half of the global population) are the likely vector for infecting others.

Perhaps the second most significant causative factor in ulcers is the use of non-steroidal anti-inflammatory drugs (NSAIDs), including aspirin and similar OTC substances. These drugs inhibit the beneficial enzyme cyclooxygenase, which maintains the integrity of the upper GI tract and promotes blood flow to the stomach. Despite the advent of a class of NSAIDs that display greater inhibition in affecting one of the forms of cyclooxygenase (COX-2 inhibitors), all NSAIDs are attended by the risk of ulcerative complications.

Technology: A specific chelate of zinc with the dipeptide L-carnosine (beta-alanine-L-histidine), known as zinc carnosine, or polaprezinc, has been used as an anti-ulcer/mucosal healing drug in Japan for several years. Not being a simple admixture of a zinc salt and L-carnosine, it displays a slow breakdown profile, liberating free zinc ion and L-carnosine with a "prolonged release" profile. It has been the subject of numerous in vitro, preclinical and clinical trials. It has demonstrated anti-H. pylori activity in vitro and has been shown to reduce or prevent gastric erosions in animals infected with H. pylori or exposed to hydrogen peroxide, ethanol or NSAIDs. It also prevents stress-induced ulcers.

In humans with either peptic ulcers or H. pylori-associated NUD, it has been shown to increase the response to combination H. pylori eradication therapy (Aliment Pharmacol Ther, 1999). Distinctively, zinc carnosine has been shown to exert superior biological activity to admixtures of zinc sulfate and L-carnosine, indicating that the coordination complex unique to zinc carnosine confers a different pharmacodynamic 'signature.'

Intellectual Property: As seen in nearly all innovator drug preparations, zinc carnosine enjoys a composition-of-matter patent, the equivalent of a drug patent. This essentially confers upon the controller of the patent (the patentee or licensor) the right to exclude others from engaging not only in the communication of claims associated with the use of zinc carnosine but also its manufacture, sale, marketing or importation.

These patents have been issued in Europe (0303380), the US (4981846) and Canada (1313725). Going down the GI tract, one also finds patents covering use of zinc carnosine for the prevention and treatment of inflammatory bowel disease: EP 0466029, US 5238931 and Canada 2046397.

Finally, adding the liver, to complete the gastro-entero-hepatic circuit, there are patents describing hepatoprotective effects: EP 03136554 and US 4927817.

In a recent clinical trial, researchers found that six months of supplementation with zinc carnosine increased the response induced by alpha-interferon in hepatitis C patients, manifesting as decreased viral burden and liver enzymes (J Viral Hepat, 2001).


Lonza Group ( www.lonza group.com) of Switzerland has obtained exclusive rights from the patent holder, Hamari Chemicals (Osaka, Japan), for distribution in Europe and North America. The company is seeking strategic marketing partners with distribution in various sales channels. For more information, contact Dan Murray (USA) at [email protected]
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