Metformin is one of the most commonly prescribed diabetes treatments worldwide and is the only oral antidiabetic of its type that has been shown to reduce both the number of deaths and vascular complications associated with the disease. However, despite the compound's therapeutic efficacy, tablet-based metformins can induce considerable gastrointestinal side effects, causing diarrhea, nausea and vomiting in about 30 per cent of those treated. While this mechanism is not fully understood, it is believed to be linked to the release of the drug's active component exclusively in the gastrointestinal tract.
Generex and co-developer, Danish medicinal gum specialist Fertin Pharma which manufactured trial stocks using its patented in-house technologies, hope that delivery of metformin via the buccal mucosa (the inner lining of the mouth) will help bypass some of these gastrointestinal side effects. Generex also unveiled the protocol for the MetControl clinical trials, which are expected to start in the third quarter this year. The first assessment will be a bioequivalence study that has been designed to compare the product with various immediate release metformins in between 75 and 100 healthy volunteers.
Demand for improved side effect profile George Markus, Generex's vice president of regulatory affairs, told in-PharmaTechnologist.com that the firm "recognized that patients with Type 2 diabetes have a number of limitations regarding fast-acting medications that are not unpleasant to take and have very few side effects."
Markus said that MetControl is intended to provide a pleasant way of administering metformin that has a rapid onset of action and minimal gastric irritation. He added that the aim was to formulate the drug in a convenient gum-tablet size that conforms to tight dosage controls. Markus explained that "as metformin does not naturally have a pleasant taste, the development of a good-tasting product that the end-user must take on a daily bases was a major hurdle." He said that Generex' R&D staff has created a product that is both rapidly absorbed and appealed to taste-testers.
Markus also said that assuming development of the product is successful "Generex sees no limitations from a global standpoint when considering market penetration and eventual sales," he added that, "metformin is a $2bn market."
As the active material is off patent and is used in products that are globally available on a commercial level, there are likely to be fewer regulatory issues to address than would be associated with a new chemical entity (NCE). As such, Generex anticipates that the registration path for MetControl will be significantly reduced.