SOURCE: Lpath, Inc.

October 16, 2008 08:29 ET

Lpath Initiates Dosing in Phase 1 Trial for AMD

Trial Marks First Time a Bioactive Lipid Antibody Has Been Dosed in the Human Eye

SAN DIEGO, CA--(Marketwire - October 16, 2008) - Lpath, Inc. (OTCBB: LPTN) announced that it has initiated dosing in its Phase 1 clinical trial with iSONEP™, the company's drug candidate for age-related macular degeneration (AMD) and possibly for other ocular diseases.

iSONEP is the ocular formulation of a monoclonal antibody that targets sphingosine-1-phosphate (S1P), a bioactive lipid that is dysregulated in cancer and other disorders of inappropriate angiogenesis and inflammation. S1P promotes angiogenesis, inflammation, cell survival, and cell proliferation, all of which have been implicated in AMD.

"We view this to be a historic moment for our company," noted Roger Sabbadini, Ph.D., founder and chief scientific officer of Lpath. "It represents the first time a patient has received an intraocular antibody that inhibits a bioactive lipid, and it also represents the first time a company has targeted the S1P pathway in a clinical trial for AMD."

A chronic disease, AMD is the leading cause of vision loss in people over 65 years of age. AMD is characterized by a choroidal neovascular (CNV) lesion that eventually leads to the degeneration of the macula, the area of the retina responsible for central vision. Pathologic disruption of the retina is caused collectively by (i) new-blood-vessel growth in the choroid layer under the retina, (ii) sub-retinal fibrosis, (iii) general inflammation in the retinal area, and (iv) edema caused by new blood vessels that do not form perfectly and are thereby permeable (or leaky).

It is the leakiness of blood vessels that distinguishes the wet form of AMD from the dry form of the disease. Currently, favored drugs for wet AMD are Lucentis® and off-label use of Avastin®, both of which target the protein VEGF, a validated promoter of permeable/leaky blood vessels. These drugs appear to exert most of their beneficial effect via an anti-permeability action that results in resolution of intra- and sub-retinal edema, but the actual CNV lesion does not regress. As a result, it is believed that anti-VEGF drugs, while improving vision in some patients for a period of time, are not affecting the progression of the disease.

In contrast, iSONEP has been shown in various animal models of disease not only to reduce blood-vessel growth and leakiness, but to significantly mitigate ocular fibrosis (Grant et al, Experimental Eye Research, August 2008) and to substantially reduce inflammation in the eye (Campochiaro et al, Journal of Cellular Physiology, October 2008). As such, iSONEP has the potential to be an effective wet AMD treatment that may offer significant advantages over exclusively anti-VEGF approaches. It may also act synergistically with them as a combination therapy to address the complex processes and multiple steps that ultimately lead to vision loss for both wet and dry AMD patients.

Glenn Stoller, MD, head of Lpath's ocular division, stated, "The treatment of AMD with an anti-S1P antibody is an extremely novel approach. Given that the average patient treated with Lucentis in its key pivotal trials (ANCHOR and MARINA) failed to regain the ability to read or drive without visual aids, there is a significant unmet medical need here. A growing body of literature suggests an anti-S1P approach like iSONEP could meet that need by contributing to both the early and the late stages of retinal damage. Because iSONEP has anti-angiogenic, anti-inflammatory, and anti-fibrotic actions it could prove to be a valuable therapeutic agent for the treatment of wet AMD, dry AMD, diabetic eye disease as well as other ocular disorders where fibrosis and inflammation are involved."

"iSONEP is our second compound to enter the clinic," noted Scott Pancoast, Lpath's president and chief executive officer. "We now have ongoing trials in two important areas -- oncology and ophthalmology -- demonstrating the potential applicability of bioactive-lipid-targeted antibodies in a broad range of disease."

Lucentis® and Avastin® are registered trademarks of Genentech, Inc.

About Lpath

Lpath, Inc., headquartered in San Diego, California, is the category leader in bioactive-lipid-targeted therapeutics, an emerging field of medical science whereby bioactive signaling lipids are targeted for treating important human diseases. ASONEP™ is an antibody against S1P that is presently in Phase 1 clinical trials for the treatment of cancer and also holds promise against multiple sclerosis and various other disorders. A second product candidate, iSONEP™ (the ocular formulation of the S1P antibody), has demonstrated superior results in various preclinical AMD and retinopathy models and is in Phase 1 clinical trials for the treatment of wet AMD. Lpath's third product candidate, Lpathomab™, is an antibody against LPA, a key bioactive lipid that has been long recognized as a valid disease target (fibrosis, cancer, neuropathic pain). The company's unique ability to generate novel antibodies against bioactive lipids is based on its ImmuneY2™ drug-discovery engine, which the company is leveraging to add to its pipeline. For more information, visit www.Lpath.com.

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