gepirone gepirone gepirone is an antidepressant and anxiolytic drug of the azapirone group that was synthesized by bristol-myers squibb in 1986 and has been under development for the treatment of depression but has yet to be marketed. it 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 been rejected multiple times by the food and drug administration (fda) during the drug approval process. however, in march 2016, the fda reversed course and ruled favorably on the efficacy of gepirone. gepironeclinical dataother namesbmy-13805, mj-13805, org-13011; ariza, variza, velexity, gepirone hydrochloride (usan us)routes ofadministrationoralatc coden06ax19 (who) pharmacokinetic dataelimination half-life2–3 hours (ir)identifiers iupac name 4,4-dimethyl-1-piperidine-2,6-dione cas number83928-76-1 ypubchem cid55191chemspider49836 yuniijw5y7b8z18chemblchembl284092 ycomptox dashboard (epa)dtxsid90232813 chemical and physical dataformulac19h29n5o2molar mass359.474 g·mol−13d model (jsmol)interactive image 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 ykey:qoigkgmmagjznz-uhfffaoysa-n y (verify) in addition to its antidepressant and anxiolytic properties, gepirone has been found to improve symptoms of sexual dysfunction in men and women. moreover, the pro-sexual effects appear to be independent of its antidepressant and anxiolytic effects. pharmacology pharmacodynamics like other azapirones, gepirone acts as a selective partial agonist of the 5-ht1a receptor. unlike its relative buspirone, however, gepirone has greater efficacy in activating the 5-ht1a and has negligible affinity for the d2 receptor (30- to 50-fold lower in comparison to buspirone). however, similarly to buspirone, gepirone metabolizes into 1-(2-pyrimidinyl)piperazine, which is known to act as a potent antagonist of the α2-adrenergic receptor. history gepirone was originally developed by bristol-myers squibb, but was out-licensed to fabre-kramer in 1993. the 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 2009. however, in 2012 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. however, in march 2016, the fda reversed its decision and gave gepirone er a positive review. during its development it has been called bmy 13805, mj 13805, org 33062, and tgfk07ad and it has had two proposed trade names: travivo and variza.