Swedish research wins USA patent: Cyclosporin-The New Brain Drug

HONOLULU- March 2, 1999 -Cyclosporin protects brain and spine from a multitude of neurological insults including stroke, trauma, and possibly neurodegenerative diseases in animal models. Maas BiolAB, LLC received United States Patent and Trademark Office's "Notice of Allowability" for their patent application for cyclosporin as neuroprotectant.

The patent provides two decades protection to Maas BiolAB, LLC for the exclusive use of cyclosporin to treat acute and chronic brain diseases. Patents were already granted in New Zealand and Africa and are pending for Europe, Japan, Russia, and China. Maas BiolAB, LLC adds to Hawaii's growing biotechnology presence.

Cyclosporin is well known as an immunosuppressant preventing rejection of transplanted organs. The Novartis cyclosporin manufacture patent has expired and several companies now make it in Europe, America and Asia.

"Cyclosporin is the most effective drug found in animal studies to treat stroke and head trauma. Maas BiolAB will bring it to the emergency room and bedside as soon as possible," said Marcus F. Keep, M.D., chief executive officer.

Cyclosporin has three complementary mechanisms that limit brain damage:

1. Prevents calcium-dependent enzymes from becoming destructive by inhibiting the phosphatase calcineurin.

2. Inhibits the production of nitric oxide (NO), reducing the formation of intracellular free radicals.

3. Blocks nerve cell damage by stabilizing mitochondrial membranes and preventing release of apoptogenic factors from mitochondria.

The mitochondrial aspect makes cyclosporin unique in the class "neuroimmunophilin ligands." Other ligands include Fujisawa's FK506, Amgen/Guilford and Schering/Vertex's small molecules, which while useful in neurological disorders, lack mitochondrial protection.

Like Maas' cyclosporin, Fujisawa recently patented their immunosuppressant, FK506, as a neuroprotectant. Last year Amgen licensed neuroimmunophilin compounds from Guilford Pharmaceuticals for $50 million ($500 million when milestones are met). Vertex Pharmaceuticals licensed their neuroimmunophilin compounds to Schering for $88 million.

"It is remarkable that a drug long used as an immunosuppressant would turn out to be much more important as a neuroprotectant when one gets it into the brain." observed inventor Eskil Elmer, Ph.D., Scientific Advisor to Maas BiolAB. It was Elmer's research while still a graduate student at Lund University, Sweden that led to his discovery.

Maas BiolAB was incorporated in Hawaii in 1997 to develop the intellectual property.

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