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GlaxoSmithKline Presents Innovative Neuroscience Pipeline
Date:12/13/2007

e portfolio has more than 25 compounds in clinical development and spans a wide variety of central nervous system (CNS) diseases. Many of these compounds have novel mechanisms of action, with the potential to offer significant benefits to patients.

GSK presented new data and development plans for several compounds during the seminar, including:

773812 - A potential major new treatment for schizophrenia:

Schizophrenia is a chronic psychiatric disorder. People with the disease often suffer terrifying symptoms such as delusions, hallucinations, and jumbled or illogical thoughts.

773812 is from the atypical antipsychotic class of medicines, and has the potential to become a major new treatment. Current atypical antipsychotic medicines work by blocking receptors for a variety of neurotransmitters in the brain. However, they have variable receptor binding affinity resulting in different efficacy and safety profiles. GSK has developed '812 as a compound with selectivity towards those receptors that are associated with efficacy, such as the dopamine D2 and serotonin 5HT2 receptors, whilst having minimal activity on receptors believed to be responsible for side-effects, such as dopamine D1, histamine H1, muscarinic M1, alpha and beta adrenergic receptors. This profile has the potential to deliver efficacy similar to the present antipsychotics without troublesome tolerability problems such as sedation, metabolic disturbance, impaired cognition and orthostatic hypotension.

Two studies to assess the efficacy and safety of '812 compared to placebo and olanzapine, a commonly used atypical antipsychotic, in patients with acute schizophrenia have been completed. In these studies, '812 produced a statistically significant improvement in patients compared to placebo (p<0.05), as measured by the Positive and Negative Symptom Scale (PANSS).

Compound '812 was generally well tolerated. In particular, '812 was not associated in either study with m
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SOURCE GlaxoSmithKline
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