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February 25,2002

Taisho and Merck tie up on mGluR agonists



Tokyo, Japan, February 25, 2002 – Taisho Pharmaceutical Co, Ltd. today announced that Merck & Co., Inc. has exercised its option under an exclusive option agreement and initiated development of Taisho’s novel mGluR (metabotropic glutamate receptor) agonists for potential use in treating diseases of the central nervous system, including schizophrenia. Financial terms of the agreement were not disclosed.

mGluR is a metabotropic glutamate receptor of which eight subtypes are currently known. Although the mechanism of action is not completely understood, mGluR receptors are believed to play a variety of key roles in brain pathology. The subtypes known as mGluR2 and mGluR3 are related to the neurotransmission of glutamate in the brain. Because abnormal neurotransmission of glutamate is believed to be a factor in the pathology of schizophrenia, mGluR agonists may be potential new treatments for this disease.Taisho has synthesized and characterized several compounds that show high affinity to mGluR.

Schizophrenia is a major public health problem throughout the world.It is estimated that this disease affects about one percent of the world’s population.Schizophrenia is more prevalent than Alzheimer’s disease, diabetes, or multiple sclerosis.A significant medical need exists for better treatments for schizophrenia that are more efficacious and tolerable.Many of the currently used medications are associated with side effects, such as weight gain, muscle spasms, and the disease is often not controlled with currently available therapies.

Taisho is the leading non-prescription pharmaceutical company in Japan and the second ranking in the world.Taisho has also been strengthening its research and development efforts in the area of prescription drugs through steady internal growth. Taisho is active in collaborations with bio-venture companies, and with domestic and foreign pharmaceutical companies.The mGluR agonists and the collaboration with Merck are examples of these efforts.