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Gepirone

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Gepirone
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Systematic (IUPAC) name
4,4-dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione
Clinical data
  • Uncontrolled
Oral
Pharmacokinetic data
Half-life 2-3 hours
Identifiers
83928-76-1
N06AX19
PubChem CID 55191
ChemSpider 49836 7pxY
UNII JW5Y7B8Z18 7pxY
ChEMBL CHEMBL284092 7pxY
Chemical data
Formula C19H29N5O2
359.46586 g/mol
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Gepirone (Ariza, Variza; BMY-13,805, ORG-13,011) is an antidepressant and anxiolytic of the azapirone class. Like other azapirones, it acts as a selective partial agonist of the 5-HT1A receptor. Gepirone was under development in the U.S. in an extended release form, but despite completing phase III clinical trials, it failed to pass the drug approval process. As a result, gepirone, despite already having brand names picked out, did not manage to reach the pharmaceutical market.

Gepirone was originally developed by Bristol-Myers Squibb, but was out-licensed to Fabre-Kramer in 1993. The U.S. Food and Drug Administration (FDA) rejected approval for gepirone in 2004. It was submitted for the preregistration (NDA) phase again in May 2007 after adding additional information from clinical trials as the FDA required in 2004. However, in 2007 it once again failed to convince the FDA of its qualities for treating anxiety and depression. There have been no updates on gepirone since.

Synthesis

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Ormaza, V. A.; 1986, ES 8606333 .

See also

References



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