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SST breaks transdermal charged molecule delivery barrier

Mar 14, 2012 Tags: Business development Next Generation Companies

Strategic Science & Technologies, LLC (SST) has developed a transformational and potentially disruptive technology that successfully delivers charged therapeutic molecules transdermally. That capability has been the holy grail of transdermal drug delivery.

Until SST developed this delivery platform, it was almost impossible to deliver a charged molecule—like ibuprofen—transdermally. The transdermal drug delivery technology that made nicotine patches common doesn’t work for charged molecules like ibuprofen, explained Eric Fossel, PhD, Founder and CEO.

Eric Fossel, SST

Eric Fossel, Founder and CEO, SST

This proprietary platform technology is called KNOSIS, for the Greek word meaning “self-emptying.” KNOSIS combines two approaches to deliver drugs through the outer layer of skin, the stratum corneum. First, KNOSIS raises the free energy of the active pharmaceutical ingredient (API) in a cream, creating an elevated chemical potential that drives the therapeutic into the tissue. Some have referred to this feature as “iontophoresis in a tube.” In addition, properties of the cream prevent the API from hydrogen-bonding to the surface of the stratum corneum. That thwarts the skin’s second level of defense and allows the API to cross this barrier.

“This energy-driven approach transports the drug across the skin. Once across the skin, the nitric oxide derived from L-Arginine helps move the API into the tissue by enhancing local blood flow,” Fossel said. KNOSIS is transformational because, “quite frankly, it works. People have been trying to get ibuprofen to work transdermally since the 1980s, and KNOSIS does this successfully.”

The first NDA product to be commercialized will be a transdermal non-steroidal anti-inflammatory drug (NSAID) for muscle and joint pain and inflammation. A transdermal L-Arginine for treatment of poor peripheral circulation in diabetic and non-diabetic patients with neuropathy and cold hands or feet already is in the marketplace.

Benefits

The benefits of local delivery are well-documented and include more targeted delivery, lower systemic exposure and, therefore, lower toxicity than oral medications. The therapeutic is delivered where it is needed at therapeutic levels. “For example, if your knee hurts why expose the rest of the body to therapeutic levels of a drug when it is not needed?” he asked. Exposure to other tissues or to the blood stream is, therefore, minimal.

“In the case of ibuprofen, KNOSIS delivers only 1% of the oral dose and achieves a comparable local therapeutic benefit,” he said. By enabling a significantly lower systemic dosage, there are no gastrointestinal side effects. Such dose reductions hold the potential for some drugs to become available over the counter. This also can significantly reduce the side effects of other potent therapeutics. Consequently, APIs that failed because of toxicity now can become potential drug candidates.

Drug developers may realize competitive advantages by employing the KNOSIS platform to create new topically applied drugs, as well as to extend the effective life of patents by reformulating existing drugs that are administered orally or topically.

Applied as a cream, the KNOSIS delivery platform coupled with ibuprofen can provide relief quickly, often within 5 to 15 minutes, depending upon the type of pain. “There’s no sense in delivering a drug systemically for something like pain,” Fossel said. This delivery system also may be used to help treat genital herpes, neuropathic pain, hives, acne, nail fungus, erectile dysfunction, Raynaud’s disease, psoriasis, inflammation and pain, migraine headaches, female sexual dysfunction and hair loss. SST is interested in working with partners to continue to expand the list of conditions that could benefit from local, topical delivery.

Partnering

Because the KNOSIS delivery platform improves the efficiency and safety of therapeutics for a wide range of conditions while expanding the delivery options for charged molecules, it has enormous commercial potential, Fossel said.

SST is looking to partner with a range of companies in a variety of therapeutic areas. “Our business model is to develop a product either to the point of clinical trials or New Drug Application (NDA) approval and then out-license it. We’ve done this with ibuprofen, which is in Phase III trials and is expected to be commercialized in the near future,” he says. SST is discussing licensing opportunities with several companies in relevant branded and generic therapeutic areas. SST is particularly interested in partnering with companies with proven expertise in marketing in the relevant therapeutic areas.

In partnership and licensing arrangements, SST brings a proven platform that can be applied to many different APIs, and the opportunity for exclusive, global licensing rights to a given drug or class of drugs, Fossel said. Importantly, “we have vast intellectual property, with far more patents than we can leverage ourselves.” To date, ten patents have been issued—six in the United States, two in Australia, one in Europe and one in Japan—and many others are in process.

Funding

SST is a virtual company financed by what Fossel calls “archangels”— angel investors who contribute significantly more than typical angel investors. These investors know that, over the life of the patent, ibuprofen alone has the potential to generate hundreds of millions of dollars in milestone and royalty payments. “The excitement is in delivering ibuprofen locally,” Fossel said, “but a local topical treatment of erectile dysfunction could be even more successful.”

Management

Like many of today’s savviest companies, SST focuses upon its core competencies—designing an innovative drug delivery platform for a wide variety of compounds. Non-core activities are outsourced to trusted experts. Consequently, this virtual company in Cambridge, Massachusetts, runs lean. “We didn’t want to build a marketing or manufacturing organization. This business model fits well with our goals,” Fossel said.

Fossel’s commitment to developing this technology was so strong that, after 25 years, he left his position as a Harvard Medical School professor as well as his position as director of radiology research at Boston’s Beth Israel Hospital to found SST. In 1997, he perfected and patented the KNOSIS transdermal delivery system. It was first applied to L-Arginine and, subsequently, to other pharmaceutical agents.

While SST’s management team includes skilled scientists, it also includes executives with pharmaceutical industry experience. “Our alliance manager, for example, has taken several drugs through the FDA’s regulatory review process to approval, and our regulatory consultant has had some 20 NDAs approved,” Fossel pointed out. As such, SST combines the scientific know-how necessary to develop a breakthrough delivery platform with the business and regulatory acumen required to see it commercialized.