The raft of drug reformulations follows the Italian company's success so far with reformulated mesalamine Lialda for ulcerative colitis, which was released in the US market on March 19 and by April 13 had already captured 1.2 per cent of the oral mesalamine market. The EU version of Lialda, Mezavant, is likely to be launched in the EU in the third quarter of this year. The eight drugs currently in the product pipeline include: the corticosteroid Budesonide; the antibiotic Rifamycin; the biologic Low Molecular Weight Heparin; the dietary supplement Zacol; an anti-Tumour Necrosis Factor-alpha CB-01-12; an immunosuppressant CB-01-09; a steroid ester androgen antagonist CB-03-01; and an antibiotic CB-01-13. Many of these new formulations will be world-firsts in some form. Using Cosmo's Multi Matrix System (MMX) technology, the drug reformulations, which cover every IBD level of symptom severity, "addresses the unmet medical needs in IBD", according to the company.
Conventional treatments either exist as oral dosage or suppository forms, which only have a limited site of action - the upper or the lower colon depending on treatment type. What the MMX technology provides is an oral dosage which treats the entire colon and has a lasting effect of 24 hours due to a controlled release action of the oral formulation. Specking to in-PharmaTechnologist.com, Cosmo chief scientific officer Dr Luigi Moro said: "MMX includes more than one release mechanism that allows the control of the rate and extent of drug leakage from the tablet matrices." Coated in an array of lipophilic, amphiphilic and hydrophilic matrices that delay and extend action, the drug is then packaged into the core of the tablet surrounded by a gastroprotectant layer. This layer protects the drugs from the stomach environment and only begins to dissolve once the tablet has reached the indicated intestinal location triggered by a change in the environment.
While the action allows for the topical application of the active pharmaceutical ingredient (API) to the whole bowel surface, the technology also allows "a controlled release rate to avoid absorption peaks and to obtain the so-called 'round the clock medication', a continuous patient therapeutic coverage", Moro said. The technology could also mean that in some circumstances less pill taking and lower doses could be achieved, he said. Lialda/Mezavant, which is licensed globally to Giuliani and Shire, allows patients to take as few as two tablets once daily to treat ulcerative colitis. Other mesalamine treatments in the market can require dosings of three or four times a day with patients taking up to 16 pills a day. Lialda/Mezavant, which is the first US Food and Drug Administration (FDA) approved once-daily oral formulation of mesalamine, is expected to hold a 9 per cent market share by the end of the year, according to the company.
The current mesalamine market is worth more than $1.6bn (€1.2bn) and is dominated by Procter's drug Asacol (mesalamine), which had a 60 per cent share of the ulcerative colitis drug market in 2003. Shire currently markets mesalamine as Pentasa in the US and Colazide in the UK, holding a 17.6 per cent and 6 per cent market share respectively in 2004. Meanwhile, Budesonide and Rifamycin are planned to be released worldwide in 2010, though Rifamycin could be in the market even earlier in selective EU countries, Moro said.
Rifamycin Phase II trial results are expected within the next few weeks.