Pimavanserin

Pimavanserin
Clinical data
Trade namesNuplazid
Other namesACP-103; BVF-036; BVF-048
License data
Routes of
administration		Oral
Drug classSerotonin 5-HT2A receptor antagonist; Antipsychotic
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding94–97%
MetabolismHepatic (CYP3A4, CYP3A5, CYP2J2)
MetabolitesN-Desmethyl-pimavanserin
Onset of actionTmaxTooltip Time to peak levels: 6 hours
Elimination half-lifePimavanserin: 54–57 h
N-Desmethyl-pimavanserin (active): 200 h
Identifiers
  • N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC25H34FN3O2
Molar mass427.564 g·mol−1
3D model (JSmol)
  • CC(C)COc3ccc(cc3)CNC(=O)N(C(CC2)CCN2C)Cc(cc1)ccc1F
  • InChI=1S/C25H34FN3O2/c1-19(2)18-31-24-10-6-20(7-11-24)16-27-25(30)29(23-12-14-28(3)15-13-23)17-21-4-8-22(26)9-5-21/h4-11,19,23H,12-18H2,1-3H3,(H,27,30) N
  • Key:RKEWSXXUOLRFBX-UHFFFAOYSA-N N
  (verify)

Pimavanserin, sold under the brand name Nuplazid, is an atypical antipsychotic which is approved for the treatment of Parkinson's disease psychosis. It is taken by mouth.

Side effects of pimavanserin include peripheral edema and confusion. Unlike other antipsychotics, pimavanserin is not a dopamine receptor antagonist, but rather is a selective antagonist or inverse agonist of the serotonin 5-HT2A receptor and to a lesser extent of the serotonin 5-HT2C receptor.

Pimavanserin was first approved for medical use in 2016. It was approved as a generic medication in 2024.

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