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 (IR)
Identifiers
CAS Number	83928-76-1
ATC code	N06AX19 (WHO)
PubChem	CID: 55191
ChemSpider	49836 Y
UNII	JW5Y7B8Z18 Y
ChEMBL	CHEMBL284092 Y
Synonyms	BMY-13805, MJ-13805, ORG-13011; Ariza, Variza
Chemical data
Formula	C19H29N5O2
Molecular 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) (current developmental code name TGFK07AD; proposed brand name Travivo) or gepirone hydrochloride (USAN) is an antidepressant and anxiolytic drug of the azapirone group that has been under development for the treatment of depression for a number of years but has yet to be marketed. Like other azapirones, it acts as a selective partial agonist of the 5-HT_1A receptor. Gepirone has been under development in the U.S. in an extended release form (referred to as gepirone ER), but despite completing phase III clinical trials and demonstrating efficacy, it has rejected multiple times by the FDA during the drug approval process.

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] However, in March 2016, the FDA reversed its decision, clearing the way for the drug to finally gain market approval in the U.S.[2]

In addition to its antidepressant and anxiolytic properties, gepirone has been found to improve symptoms of sexual dysfunction in men and women, similarly to the 5-HT_1A receptor agonist flibanserin. Moreover, the pro-sexual effects appear to be independent of its antidepressant and anxiolytic effects.

See also

• Buspirone
• Tandospirone