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Bifeprunox (DU-127,090) is a novel atypical antipsychotic agent which, along with SLV313, aripiprazole, and SSR-181507 combines minimal D2 receptor agonism with 5-HT receptor agonism.
Bifeprunox has a novel mechanism of action. Conventional antipsychotics are classed into typical and atypical. The typical antipsychotics, such as chlorpromazine and haloperidol are potent D2 receptor antagonists. The atypical antipsychotics started with clozapine, these are classified as multireceptor interacting compounds, acting as an agonist towards 5-HT1A and an antagonist towards D2 receptors among other 5-HT and DA receptors. Bifeprunox and other novel atypical antipsychotics will instead of antagonizing D2 receptors, will act as partial agonists, as well as agonists towards 5-HT1A receptors.
In a multi-center, placebo-controlled study, 20 mg of bifeprunox was found to be significantly more effective than placebo at reducing symptoms of schizophrenia, with a low incidence of side effects.
An NDA for Bifeprunox was filed with the U.S. Food and Drug Administration in January 2007. The FDA rejected the application in August 2007. In June 2009, Solvay and Lundbeck decided to cease development because "efficacy data did not support pursuing the existing development strategy of stabilisation of non-acute patients with schizophrenia." 
Feenstra, R. W.; de Moes, J.; Hofma, J. J.; Kling, H.; Kuipers, W.; Long, S. K.;
Tulp, M. T. M.; van der Heyden, J. A. M.; Kruse, C. G.; Bioorg. Med. Chem. Lett.
2001, 11, 2345.
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- ↑ Cuisiat S, Bourdiol N, Lacharme V, Newman-Tancredi A, Colpaert F, Vacher B (2007). "Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities". J. Med. Chem. 50 (4): 865–76. doi:10.1021/jm061180b. PMID 17300168.
- ↑ Bardin L, Auclair A, Kleven MS; et al. (2007). "Pharmacological profiles in rats of novel antipsychotics with combined dopamine D2/serotonin 5-HT1A activity: comparison with typical and atypical conventional antipsychotics". Behav Pharmacol. 18 (2): 103–18. doi:10.1097/FBP.0b013e3280ae6c96. PMID 17351418.
- ↑ Lua error in package.lua at line 80: module 'Module:Citation/CS1/Suggestions' not found.
- ↑ Wyeth and Solvay say FDA rejects application for antipsychotic drug bifeprunox. Thomson Financial, August 10, 2007.
- ↑ Pipeline update - following an interim analysis the studies with bifeprunox for the treatment of schizophrenia is discontinued Lundbeck Press Release.