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Cardax Pharmaceuticals: Astaxanthin Eliminates Adverse Effects of Vioxx on LDL Oxidation; Oxidized LDL Levels Strongly Correlated With Cardiovascular Disease

Posted on: Wednesday, 28 June 2006, 15:00 CDT

Elucida Research LLC, a private laboratory in Beverly, Mass., dedicated to independent and innovative biomedical research, and Cardax(TM) Pharmaceuticals, Inc., a drug discovery and development company targeting inflammatory cardiovascular disease, announced today publication of an article in a special edition of the Journal of Cardiovascular Pharmacology (vol. 47, supplement 1) focusing on the adverse cardiovascular effects of rofecoxib (Vioxx). The article, titled "Rofecoxib Increases Susceptibility of Human LDL and Membrane Lipids to Oxidative Damage: A Mechanism of Cardiotoxicity," demonstrated the ability of astaxanthin, a key metabolite of Cardax(TM), to prevent the pro-oxidant effects of rofecoxib (Vioxx) on lipids. Oxidative damage to membrane lipids and LDL contributes to the progression of atherosclerosis, as well as coronary plaque instability and the incidence of acute coronary syndromes.

"This study and other direct comparator studies showed a consistently worse outcome for Vioxx with respect to mechanisms of cardiotoxicity, as compared to other COX-selective and non-selective agents, such as celecoxib (Celebrex), naproxen, and ibuprofen, among others," said lead researcher R. Preston Mason, PhD, the President and Founder of Elucida Research LLC in Beverly, MA. Dr. Mason is also a faculty member at Harvard Medical School.

"Homochiral (3S,3'S)-astaxanthin completely eliminated the pro-oxidant activity of rofecoxib in the model system at low absolute concentration," said Samuel F. Lockwood, MD, MSc, Vice President and Chief Scientific Officer of Cardax Pharmaceuticals, Inc. "The dose of astaxanthin (and therefore oral CardaxTM) required for this beneficial effect in humans would be in the low milligram (mg) range." The co-formulation of Vioxx with astaxanthin may be the only immediately implementable pharmacologic solution to this problem, as novel agents to counteract these effects must await standard FDA regulatory drug testing. Astaxanthin is an FDA-approved feed additive (1987). Patients who derived tremendous clinical analgesic benefit from Vioxx (e.g. rheumatoid arthritis patients) might be able to continue therapy, if the current results were confirmed in a properly-conducted co-formulation trial in humans.

As the study abstract summarizes, experimental findings from independent laboratories now indicate that the cardiotoxicity of Vioxx may not be a class effect, but due to its intrinsic chemical properties. Specifically, Vioxx has been shown to increase the susceptibility of human LDL and cellular membrane lipids to oxidative modification, a contributing factor to plaque instability and thrombus formation. Other investigators have also shown that Vioxx readily forms a reactive metabolite that is capable of reactions with biological molecules, especially amino groups, causing disruption in essential cellular structure-function relationships. This reactive metabolite could not be derived from other COX-2 selective agents, including celecoxib (Celebrex), valdecoxib, and lumaricoxib, due to differences in their chemical structure.

The published study further confirms these findings by demonstrating that the pro-oxidant activity of Vioxx can be blocked by the potent antioxidant astaxanthin in homochiral form (all-trans 3S,3'S), on which CardaxTM is based.

About Elucida Research LLC.

Elucida Research LLC is a privately held biotechnology research company that provides contract and proprietary research to a wide range of pharmaceutical and biotechnology clients. The company uses advanced biophysical and biochemical methods to identify new chemical leads for the pharmaceutical industry. Elucida's research team also explores novel mechanisms of action for currently marketed drugs in the areas of cardiology and neurology. The company has an impressive record of delivering substantial value in the areas of drug discovery and development to pharmaceutical and biotechnology clients from around the world.

About Cardax(TM) Pharmaceuticals, Inc.

Cardax(TM) Pharmaceuticals is a drug discovery and development company focused on developing effective therapeutics for large, unmet needs in the area of inflammatory medicine. The Company's first products target cardiovascular disease, the largest (and growing) sector of the pharmaceutical industry with annual sales worldwide of more than $70 billion. Cardax Pharmaceuticals' first product, Cardax(TM) oral, has completed pre-clinical proof-of-concept testing and is poised for clinical development. Cardax(TM) oral, a proprietary compound based on an astaxanthin pharmacophore or scaffold, is being developed as a first-in-class anti-inflammatory treatment to reduce cardiovascular inflammation and subsequent cardiovascular events associated with elevations in circulating C-reactive protein (CRP) in at-risk patients.

For more information, please visit http://www.cardaxpharma.com.

Source: Business Wire

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