Chemeq compound shows liquid promise

By Graeme O'Neill
Thursday, 20 February, 2003

The antimicrobial compound developed by Perth-based pharmaceutical company Chemeq (ASX: CMQ) is beginning to look it might be a useful addition to domestic water supplies.

Chemeq announced today that its experiments have confirmed that its polymer-based antimicrobial, originally developed to protect piglets against pathogenic E. coli bacterial infections, is also active in vitro against an antibiotic-resistant strain of Helicobacter pylori.

Chemeq's press release said its researchers had found that a 0.1 per cent solution of the polymer compound completely killed all cells of a strain of H. pylori to an emergent H. pylori strain that exhibits resistance to two of the fast shrinking arsenal of antibiotics still capable of eliminating H. pylori infections.

In the 1980s, Perth medicos Robin Warren and Barry Marshall famously indicted H. pylori as the chief agent of chronic gastritis (reflux) and gastric ulcers. Tissue damage from chronic ulcers can in turn trigger gastric adenocarcinoma -- cancer of the stomach and duodenum.

For more than a decade, many Australian doctors have used Marshall's recommended therapy -- a two-antibiotic cocktail mixed with bismuth -- to cure chronic gastric ulcers in Australia.

Overseas, doctors continued to treat stomach ulcers with the acid-suppressing drugs like Tagamet and Zantac, two of the 20th century's most lucrative drugs. While they temporarily healed ulcers, they did not eliminate H. pylori, and the ulcers invariably returned.

According to Chemeq chairman and CEO Dr Graham Melrose, the highly successful antibiotic-cocktail therapy, now used worldwide, is encountering problems with the emergence of multi-resistant strains of H. pylori.

While Melrose pointed out that Chemeq's latest results relate only to in vitro experiments, the earlier indications of the compound's activity against the Helicobacter species that infects pigs hints that it should also be active in vivo against H. pylori in humans.

That promise is reinforced by compound's novel, generic mode of action against pathogenic bacteria in the gastrointestinal tract. It is active against all bacterial pathogens of the upper gastrointestinal tract, not just in pigs, but in poultry.

The compound is not an antibiotic, but a large polymer molecule that binds to protein molecules -- including the integral protein molecules that stud the coats of all bacteria species.

These coat proteins are essential for adhering to host tissues, and signalling processes involved in bacterial replication and pathogenesis.

It is literally impossible for bacteria to mutate and evolve resistance; the latest results confirm that even antibiotic-resistant species are susceptible,

Antibiotic therapies disrupt the complex communities of benevolent bacteria that live harmlessly in the lower gut, and can lead to the emergence of resistant, pathogenic strains, as well as leaving residues in livestock meat.

Melrose said the compound was active only in the stomach and the upper digestive tract, where most pathogenic bacteria tended to establish -- it is inactivated by binding to large proteins in the lower digestive tract, where 'friendlies' reside.

Chemeq's compound cannot generate resistance, nor will it contaminate the environment with potentially harmful residues. The molecule is too large to enter the bloodstream, so it is also non-toxic and non-immunogenic.

The US Food and Drug Administration (FDA) has speeded its regulatory procedures for the compound, which is seen as a bright hope for avoiding the serious problem of multi-antibiotic resistance in human and livestock pathogens.

Chemeq has estimated the global market for the antimicrobial at more than $AUD1 billion for pigs alone, with the poultry market being worth perhaps 10 times as much.

The global market for a safe new H. pylori therapeutic is potentially much larger -- Melrose said the microbe infects an estimated 50 per cent of the world's population.

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