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Gepirone

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Gepirone
Clinical data
Other namesBMY-13805, MJ-13805, ORG-13011; Ariza, Variza
Routes of
administration		Oral
ATC code
Pharmacokinetic data
Elimination half-life2–3 hours (IR)
Identifiers
  • 4,4-Dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H29N5O2
Molar mass359.46586 g/mol g·mol−1
3D model (JSmol)
  • O=C1N(C(=O)CC(C)(C)C1)CCCCN3CCN(c2ncccn2)CC3
  • 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 checkY
  • Key:QOIGKGMMAGJZNZ-UHFFFAOYSA-N checkY
  (verify)

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.[1] Like other azapirones, it acts as a selective partial agonist of the 5-HT1A receptor.[1] 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,[1] 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-HT1A receptor agonist flibanserin.[2][3] Moreover, the pro-sexual effects appear to be independent of its antidepressant and anxiolytic effects.[2][3]

See also

References

  1. ^ a b c Kishi, T.; Meltzer, H. Y.; Matsuda, Y.; Iwata, N. (2013). "Azapirone 5-HT1A receptor partial agonist treatment for major depressive disorder: systematic review and meta-analysis". Psychological Medicine. 44 (11): 2255–2269. doi:10.1017/S0033291713002857. ISSN 0033-2917.
  2. ^ a b Fabre, Louis F.; Brown, Candace S.; Smith, Louis C.; DeRogatis, Leonard R. (2011). "Gepirone-ER Treatment of Hypoactive Sexual Desire Disorder (HSDD) Associated with Depression in Women". The Journal of Sexual Medicine. 8 (5): 1411–1419. doi:10.1111/j.1743-6109.2011.02216.x. ISSN 1743-6095.
  3. ^ a b Fabre, Louis F.; Clayton, Anita H.; Smith, Louis C.; Goldstein, Irwin; Derogatis, Leonard R. (2012). "The Effect of Gepirone‐ER in the Treatment of Sexual Dysfunction in Depressed Men". The Journal of Sexual Medicine. 9 (3): 821–829. doi:10.1111/j.1743-6109.2011.02624.x. ISSN 1743-6095.



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