Resolvyx Compounds Show Promise In Treatment of Ocular Disease

BEDFORD, Mass. & FORT LAUDERDALE, Fla.--(BUSINESS WIRE)--Resolvyx Pharmaceuticals, Inc., the leading resolvin therapeutics company, today announced the presentation of data on its novel resolvin therapeutics for the treatment of eye disease. The newly-reported results demonstrate the efficacy of resolvins in multiple animal models of ocular disease, including age-related macular degeneration (AMD) and dry eye. In addition, the data demonstrate that, upon topical dosing, resolvin compounds achieve therapeutic concentrations at the level of the retina, offering the potential for a topical drug, administered as eye drops, to treat retinal disease. Data on the company’s resolvin drug candidates, including the lead development candidate for eye disease, RX-10008, were presented in eight oral and poster sessions at the Association for Research in Vision and Ophthalmology (ARVO) Annual Meeting in Fort Lauderdale, Florida, being held April 27 to May 1, 2008.

“We are highly encouraged by these findings, which illustrate the potential for resolvins to treat a number of ocular indications, based on their unique ability to naturally inhibit key inflammatory processes, preserve the integrity of eye tissue and promote tissue repair,” said Per Gjorstrup, M.D., Ph.D., Chief Medical Officer of Resolvyx Pharmaceuticals. “We look forward to initiating human clinical trials this year in ocular disease and expect top-line Phase 2 data by the end of 2008.”

Key findings from the studies being presented at ARVO include:

Corneal Disease. In vivo studies demonstrated that the resolvin drugs RX-10008 and RX-10001 (RvE1) were highly effective in preventing clinical signs of dry eye – the most common corneal disease. Resolvins act by decreasing corneal inflammation, reducing corneal epithelial damage and preventing loss of goblet cells (the cells responsible for maintaining tear film integrity). In a second study, RX-10008 and RX-10001 (RvE1) accelerated corneal tissue repair with an effect level comparable to that seen with epidermal growth factor (EGF), the most potent previously-known mediator of corneal tissue repair. In a third study, RX-10008 and RX-10001 (RvE1) potently blocked several key proinflammatory mediators in dry eye syndrome. Together, these data form the basis for initiating clinical evaluation of resolvins for the treatment of dry eye. Clinical trials will begin later this year.

Retinal Disease. In vivo studies demonstrated that RX-10008 and RX-10001 (RvE1) are highly effective in preventing vascular leakage and neovascularization, the main contributors to age-related macular degeneration (AMD) and other degenerative retinal diseases. In a second study, the resolvin NPD1 was also shown to be efficacious in preventing vascular leakage and neovascularization. In a third study, RX-10008 and RX-10001 (RvE1) significantly reduced apoptosis of retinal pigmented epithelial (RPE) cells. Loss of RPE cells is an important contributor to vision loss resulting from several retinal diseases, including both wet and dry AMD, diabetic retinopathy and retinitis pigmentosa. These data suggest that resolvins have important cell survival effects that could offer a therapeutic benefit in a wide range of retinal diseases.

“These are promising new data which demonstrate that resolvins provide robust inhibition of inflammation and promote cell survival in models of a major ocular disease, AMD,” said Nicholas G. Bazan, M.D., Ph.D., Director, Louisiana State University Neuroscience Center of Excellence. “These data support continued development of resolvins for the treatment of AMD and other retinal diseases.”

Ocular Pharmacokinetics. Specific pharmacokinetic studies showed that resolvins and resolvin analogs can be delivered topically as eye drops with excellent penetration to the cornea, aqueous humor and vitreous, suggesting that topical administration of resolvins would be possible for the treatment of both corneal and retinal eye diseases.

About Dry Eye Syndrome

Dry eye syndrome is one of the most common problems treated by eye physicians; 25-30 million Americans suffer from dry eyes and worldwide, the incidence rate closely parallels that of the United States.

Dry eye is a consequence of insufficient tear production or an increased evaporation of the tear film. The ensuing stress on the corneal surface causes an inflammatory response which leads to corneal lesions, pain and occasionally to vision loss. Dry eye can make it more difficult to perform some visual activities for an extended period of time, and it can decrease tolerance for dry environments.

About AMD

Each year 1.2 million of the estimated 12 million people with macular degeneration will suffer severe central vision loss, and 200,000 individuals will lose all central vision in one or both eyes.

AMD causes deterioration of the macula in the eye, which is a tiny structure in the middle of the retina that is responsible for central vision. Macular degeneration leads to a gradual loss of the sharp, central vision. AMD occurs in two forms, dry and wet. Ninety percent of all people with AMD have the dry type in which an area of the retina becomes diseased, leading to the slow breakdown of cells in the macula, and a gradual loss of central vision. While less prevalent, wet AMD is more severe; it accounts for the majority of all blindness from the disease. As dry AMD worsens, new blood vessels may begin to grow and cause "wet" AMD. These new blood vessels often leak blood and fluid under the macula. This leakage can lead to permanent damage of the macular region.

About Resolvins

Resolvins are a recently discovered family of naturally-occurring, small molecule lipid mediators that can be targeted to treat a wide range of diseases. In particular, resolvins act to protect healthy tissue during an immuno-inflammatory response to infection, injury or other environmental challenge, and then act to resolve inflammation and promote healing after the insult has passed. Resolvins are shown to be highly potent and efficacious in pre-clinical models of asthma, atherosclerosis, rheumatoid arthritis, inflammatory bowel disease, dry eye and retinal disease, among others.

Resolvins are potential drug candidates to treat a broad range of acute and chronic diseases caused by a failure to resolve the inflammatory response and restore immune homeostasis. Such diseases include auto-immune diseases (like Crohn’s disease, psoriasis and rheumatoid arthritis), allergic diseases (like asthma) and chronic inflammatory diseases (like atherosclerosis, degenerative retinal diseases, chronic dry eye and Alzheimer’s disease). Resolvins offer an entirely novel biological approach to treating significant inflammatory diseases, with a decreased potential for immuno-suppression.

About Resolvyx Pharmaceuticals

Resolvyx Pharmaceuticals is a privately-held biopharmaceutical company dedicated to the discovery, development and commercialization of resolvins, a novel class of therapies to treat inflammatory diseases and their complications. Resolvyx's drug R&D programs are focused on characterizing and developing resolvin-based compounds. With its experienced management team, world-class scientists and leading investors, Resolvyx is well-positioned to capitalize on its extensive portfolio of more than 55 patents and applications. The company's headquarters are in Bedford, Massachusetts.

For additional information, please visit www.resolvyx.com.