Cyclosporin - The New Brain Drug: Maas BiolAB of Hawaii Gets U.S. Patent

Business Editors and Health/Medical Writers

HONOLULU - (Business Wire) - Feb. 24, 1999 - Cyclosporin protects brain and spine from a multitude of neurological insults including stroke, trauma, and neurodegenerative diseases. MaasBiolAB, LLC received the 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 eight African countries and are pending for Europe, Japan, Russia, and China. Maas BiolAB, LLC joins other new companies in Hawaii and adds to the islands' growing biotechnology presence.

Cyclosporin is well known as an immunosuppressant preventing rejection of transplanted organs. The Novartis cyclosporin manufacture patent expired in 1995 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. Inhibits calcineurin, preventing destructive calcium-dependent enzyme cascades.

2. Inhibits NO synthetase, reducing intracellular free radicals.

3. Prevents release of mitochondrial enzymes like cytochrome c, blocking apoptotic neuron death.

The mitochondrial aspect makes cyclosporin unique in the class "neuroimmunophilin ligands." Other ligands include Fujisawa's FK 506, Amgen/Guilford and Schering/Vertex's small molecules, which while useful in neurological disorders, lack mitochondrial protection.

Like Maas' cyclosporin, Fujisawa patented another immunosuppressant - FK 506 - as a neuroprotectant. Last year Amgen licensed neuroimmunophilin compounds from Guilford Pharmaceuticals for $50 million (and total $500 million when all milestones are met). Vertex Pharmaceuticals licensed their own neuroimmunophilin compounds to Schering AG of Germany 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 based on that invention.

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