Gepirone

Gepirone

Systematic (IUPAC) name
4,4-Dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione
Clinical data
Routes of administration	Oral
Pharmacokinetic data
Biological half-life	2-3 hours
Identifiers
CAS Number	83928-76-1
ATC code	N06AX19
PubChem	CID 55191
ChemSpider	49836 Y
UNII	JW5Y7B8Z18 Y
ChEMBL	CHEMBL284092 Y
Chemical data
Formula	C19H29N5O2
Molar mass	359.46586 g/mol
SMILES O=C1N(C(=O)CC(C)(C)C1)CCCCN3CCN(c2ncccn2)CC3
InChI InChI=1S/C19H29N5O2/c1-19(2)14-16(25)24(17(26)15-19)9-4-3-8-22-10-12-23(13-11-22)18-20-6-5-7-21-18/h5-7H,3-4,8-15H2,1-2H3 Y Key:QOIGKGMMAGJZNZ-UHFFFAOYSA-N Y
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Gepirone (INN) (developmental code names BMY-13805, MJ-13805, ORG-13011, TGFK07AD; proposed brand names Ariza, Variza) or gepirone hydrochloride (USAN) is an antidepressant and anxiolytic drug of the azapirone group that has never been marketed. Like other azapirones, it acts as a selective partial agonist of the 5-HT_1A 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 chosen, 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. In December 2015, the FDA once again gave gepirone a negative review for depression due to concerns of efficacy.[1]

See also

• Buspirone
• Tandospirone

References