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Drugs that Melt in Your Mouth: MonoSolRx Has Its Sights Set on Oral Insulin

Xconomy New York — 

[Corrected 5/12/11, 9:00 am. See below.] The sample packets of the anti-nausea drug that are strewn across the desk of Mark Schobel, CEO of MonoSol Rx, don’t look anything like your standard pharmaceutical product. Each dose of the drug, called ondansetron (Zuplenz)—which is prescribed to cancer patients undergoing chemotherapy and other harsh treatments—is a small, thin piece of film that’s packaged in its own plastic packet. A patient can slip the film in his mouth and it will dissolve in seconds, with no need for water.

MonoSol Rx’s drug-delivery technology, called PharmFilm, is reminiscent of Johnson & Johnson’s popular breath freshener Listerine PocketPaks, except that MonSol Rx’s films have a much more valuable payload: They deliver precise doses of prescription drugs. MonoSol Rx’s business plan is built on the idea that patients would rather let a film dissolve on their tongues or cheeks than have to swallow a pill or take an injection. “We are taking drugs to the next level,” Schobel says. “It’s about convenience, ease of administration, portability—making medication a non-event.”

MonoSol Rx’s version of ondansetron, which was developed in conjunction with two European drug companies and approved by the FDA in July 2010, became the Warren, NJ-based firm’s first marketed product. It helped the tiny pharma company reach a milestone in the fourth quarter of last year: profitability. Now MonoSol Rx is bringing its film into entirely new markets, including diabetes, where it hopes to be the first company to successfully make oral insulin—long the holy grail of the pharmaceutical industry.

MonoSol Rx was spun off from Merillville, IN-based materials maker MonoSol in 2004, and it began engineering a polymer-based, edible film that could dole out uniform doses of medicine. The company secured more than 20 patents covering everything from the composition of the film to the flavoring that’s used to mask medicines’ often bitter tastes. Some MonoSol Rx films dissolve quickly on or under the tongue, while others stick to the inside of the cheek, delivering a drug dosage over a longer period of time.

The company’s journey from a research-based organization to commercial success was far from smooth. After raising $36 million privately in 2006, MonoSol Rx attempted an initial public offering in 2007. But like so many small pharma companies trying to go public in a difficult market, it was forced to abandon its Wall Street dream. “It was a terrible market,” recalls Schobel, adding that the company had to cut its employee count from 100 to 75 and raise debt so it could continue on its development path.

Last year was a banner one for MonoSol Rx. Just six weeks after Zuplenz was approved, the FDA gave the green light to a film combining the drugs buprenorphine and naloxone—a treatment for opioid dependence that MonoSol Rx developed with Richmond, VA-based Reckitt Benckiser Pharmaceuticals, which markets the drug as Suboxone Film.

A spokesperson for Reckitt Benckiser says that in under a year on the market, the film product has captured 37.5 percent of total sales of buprenorphine, which is also available as a dissolving tablet. The film formulation, the spokesperson says, dissolves twice as fast as the tablet. Additionally, she says, it helps lessen public concerns that children will get ahold of the drug accidentally, since each film is packaged in “highly child-resistant pouches.” The film also cannot be abused by crushing and snorting, as tablets can, and each unit-dose pouch bears a unique 10-digit code that helps doctors make accurate medication counts. [This paragraph has been updated to correct the detail about the film product’s market share and clarify the comments from Reckitt Benckiser.]

As excited as Schobel is about his company’s marketed products, he becomes even more animated when he talks about the effort to develop oral insulin. “You and I know how many people have shouted from the highest building that they have the answer to oral insulin, but it’s been an uphill climb,” he says. Indeed, many efforts to develop an insulin pill have faltered because the protein degrades too quickly in the digestive tract. And Pfizer’s inhaled insulin product, Exubera, failed in the wake of safety issues and lagging demand.

Last year, MonoSol Rx formed a joint venture with UK-based Midatech, which developes nanoparticles—tiny synthetic molecules that are designed to carry drugs safely through the body. The two companies developed a film containing evenly distributed insulin-bearing nanoparticles. When the film is placed on the inside of the cheek, it slowly delivers the drug into the body.

In January, at the JP Morgan Healthcare conference in San Francisco, MonoSol Rx and Midatech announced positive results from a study of the insulin film in monkeys. The two companies are currently applying for permission to run human trials in Switzerland, which they hope will begin in the third quarter.

Schobel is well aware of the pitfalls of developing oral insulin. One problem is that every patient with diabetes is different. Some require more insulin, some less, and their needs can vary depending on their diet and lifestyle—a challenge that has complicated development efforts for inhaled insulin, which can be difficult to titrate. Schobel says he believes his films could be made in a variety of sizes, so patients can more easily adjust their doses on the fly.

But he also knows it will take a lot of work for MonoSol Rx and Midatech to prove their technology can work in diabetes. “We are going in a very stepwise fashion,” Schobel says. “We need to demonstrate it’s safe and get a view of the pharmaco-dynamics before we can determine how far we can go.”

Meanwhile, MonoSol Rx is diversifying the rest of its pipeline. It’s working on transforming a number of existing drugs into films, including montelukast (Singulair) for allergy and asthma, and zolmitriptan (Zomig) for migraine.

And on April 25, the company formed a partnership with Iowa City, IA-based KemPharm to develop a completely new treatment for attention deficit/hyperactivity disorder (ADHD). Unlike MonoSol Rx’s other products, which are based on drugs that already exist in other forms, this one is being designed from the start as a film. Schobel believes the ADHD market is ideal for his drug-delivery method. “To get kids to take a proper dose of medicine is difficult,” he says. “With film, you put just put it in, it dissolves, you swallow it, it’s done. It’s not a pill or liquid on a spoon. And if Mom needs to carry the product, it’s very easy and discreet.”

That’s not to say MonSol Rx is free from competition. Some big pharma companies are doing their own work with film, including Novartis, which has made over-the-counter film versions of Triaminic, Theraflu, and other famous products. Schobel, who once worked in Novartis’ consumer division, says he’s mindful of competition, but not worried. “I feel we have a very strong proprietary position in the delivery technology,” he says. “We have a huge IP portfolio on a global basis.”

The company isn’t shy about defending its IP, either. Earlier this year, MonoSol Rx filed a lawsuit against three companies alleging that their drug-infused film infringed one of MonoSol Rx’s patents. “We will vigorously defend our proprietary patent-protected position,” Schobel says.

The occasional patent dispute is unlikely to dampen Schobel’s enthusiasm for film-based drugs, however. “We’re not saying its going to take over existing tablets and the like, but we believe that even if we get single-digit market penetration, it will be a huge opportunity for us,” he says. “Film is here to stay.”