pimavanserin   Click here for help

GtoPdb Ligand ID: 8423

Synonyms: ACP 103 | ACP-103 | Nuplazid (proposed trade name)
Approved drug
pimavanserin is an approved drug (FDA (2016))
Compound class: Synthetic organic
Comment: Pimavanserin is an inverse agonist of the serotonin 5-HT2A receptor [4]. Pharmaceutical formulations contain pimavanserin tartrate (PubChem CID 67017013) .
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 10
Topological polar surface area 44.81
Molecular weight 427.26
XLogP 4.46
No. Lipinski's rules broken 0
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Canonical SMILES CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C
Isomeric SMILES CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C
InChI 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)
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Summary of Clinical Use Click here for help
In 2014 US FDA granted breakthrough therapy status for pimavanserin as a potential treatment for Parkinson's disease psychosis, following the completion of Phase 2I clinical trials for this indication. A Phase 2 trial administering pimavanserin as an adjunctive treatment for schizophrenia (in combination with antipsychotic medications such as risperidone and haloperidol) has also been completed. A further Phase 2 trial in patients with Alzheimer's disease psychosis is underway.
In November 2015, the US FDA confirmed that the New Drug Application (NDA) for Nuplazid® branded pimavanserin will be considered under it's 'Priority Review' process, to expedite its approval as a treatment of psychosis associated with Parkinson's disease, a condition for which there was no previous FDA-approved therapy. This Priority Review resulted in a 2016 approval for treating hallucinations and delusions associated with Parkinson's disease.