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Bifeprunox

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Bifeprunox
Clinical data
ATC code
  • none
Identifiers
  • 7-[4-(biphenyl-3-ylmethyl)piperazin-1-yl]-1,3-benzoxazol-2(3H)-one
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC24H23N3O2
Molar mass385.467g·mol−1
3D model (JSmol)
  • O=C2Oc1c(cccc1N2)N5CCN(Cc4cccc(c3ccccc3)c4)CC5
  • InChI=1S/C24H23N3O2/c28-24-25-21-10-5-11-22(23(21)29-24)27-14-12-26(13-15-27)17-18-6-4-9-20(16-18)19-7-2-1-3-8-19/h1-11,16H,12-15,17H2,(H,25,28)checkY
  • Key:CYGODHVAJQTCBG-UHFFFAOYSA-NcheckY
☒NcheckY(what is this?)(verify)

Bifeprunox(INN) (code nameDU-127,090) is anatypical antipsychoticwhich, similarly toaripiprazole,combines minimalD2receptoragonismwithserotonin receptoragonism.[1]It was under development for the treatment ofschizophrenia,psychosis and Parkinson's disease.[2]

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.[3]An NDA for Bifeprunox was filed with theU.S. Food and Drug Administrationin January 2007. The FDA rejected the application in August 2007.[4]In June 2009, Solvay and Wyeth decided to cease development because "efficacy data did not support pursuing the existing development strategy of stabilisation of non-acute patients with schizophrenia."[5]

Pharmacodynamics

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Bifeprunox is an atypical antipsychotic that is a partial D2 agonist.

See also

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References

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  1. ^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.PMID17300168.
  2. ^"Bifeprunox".go.drugbank.com.Retrieved2023-11-16.
  3. ^Casey DE, Sands EE, Heisterberg J, Yang HM (October 2008). "Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study".Psychopharmacology.200(3): 317–31.doi:10.1007/s00213-008-1207-7.PMID18597078.S2CID23291727.
  4. ^Wyeth and Solvay say FDA rejects application for antipsychotic drug bifeprunox.Thomson Financial, August 10, 2007.
  5. ^Pipeline update - following an interim analysis the studies with bifeprunox for the treatment of schizophrenia is discontinuedArchived2011-07-14 at theWayback MachineLundbeck Press Release.
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