Neurocrine says studies show indiplon has high affinity, selectivity to sleep agent receptor

By E. Janene Geiss

Philadelphia, April 5 - Neurocrine Biosciences, Inc. announced Wednesday that studies on the mechanism of action of indiplon confirm its high affinity and selectivity for the subtype of the GABA receptor that is responsible for the principal effect of "non-benzodiazepine" sleep agents.

Results demonstrate that indiplon has an enhanced combination of affinity and selectivity for alpha 1 containing GABA-A receptors compared to the currently marketed non-benzodiazepine sleep agents zolpidem (Ambien), zaleplon (Sonata) and zopiclone (Imovane, which is the racemic form of s-zopiclone [Lunesta]), according to a company news release.

These results further support and partially elucidate the consistent efficacy and safety of indiplon that has been demonstrated throughout multiple clinical studies and support the conclusion that indiplon is a novel GABA-A receptor potentiator for the treatment of insomnia, officials said.

Officials added that the selectivity profile of indiplon revealed in this study suggests a low propensity for unwanted side effects.

The results are published in the April 2006 edition of the Journal of Pharmacology and Experimental Therapeutics.

The new paper builds on earlier publications that showed indiplon to have high affinity for the benzodiazepine site on the GABA-A receptor and selectivity for receptors containing the alpha 1 subunit, the subunit principally responsible for the hypnotic effects of "non-benzodiazepine" drugs, officials said.

Neurocrine Biosciences is a San Diego product-based biopharmaceutical company focused on neurological and endocrine diseases and disorders.

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