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Investigational Agent Targeting Metabotropic Glutamate 2/3 Receptors Demonstrates Antipsychotic Activity in Humans, Study in Nature Medicine Finds
Date:9/2/2007

tinuation due to lack of efficacy, however, discontinuation due to adverse events was not significantly different across the three treatment groups (P = 0.66).

Adverse Events

Overall, the study showed that LY2140023 40mg, given twice daily, was found to be safe and well-tolerated, with most adverse events being mild to moderate in severity and not treatment-limiting. The most common treatment- emergent adverse events in the LY2140023 group were insomnia, affect lability (P = 0.038), nausea, headache, somnolence and blood creatine phosphokinase increase. The adverse event profile of LY2140023 did not include prolactin increase or worsening of extrapyramidal symptoms (EPS). Although mood lability seems to represent the most important potential adverse event, it should be noted that this outcome was observed primarily at one clinical site. In the olanzapine group, treatment-emergent adverse events included elevation in blood triglyceride levels (P = 0.005), insomnia, weight gain (P = 0.034), somnolence, akathisia, agitation and periodontitis (P = 0.03).

About LY2140023

LY2140023 is an investigational drug from Lilly, which is being developed as a new treatment option for schizophrenia. LY2140023 is an oral "prodrug," meaning it is devoid of intrinsic biological activity and, once administered, is metabolized to provide the active mGlu2/3 receptor agonist called LY404039. Most currently approved antipsychotic medications work by affecting the neurotransmitters dopamine or serotonin. For LY2140023, the active substance, LY404039, is thought to work by reducing the presynaptic release of another neurotransmitter, glutamate, in brain regions where mGlu2/3 receptors are expressed. Further studies are planned or are ongoing to learn more about the safety and effectiveness, including determining an optimal therapeutic dose for LY2140023.

About Olanzapine

Olanzapine is marketed by Lilly as Zyprexa. Zyprexa is indicated in the United States f
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SOURCE Eli Lilly and Company
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