pimavanserin (nuplazid) Report issue

Small molecule Approved FDA Priority Review FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem

Active Ingredient History

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Pimavanserin, marketed under the trade name Nuplazid, a non-dopaminergic atypical antipsychotic developed by Acadia Pharmaceuticals is the first and only medication approved by the U.S. Food and Drug Administration (FDA) for the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis. The mechanism of action of pimavanserin in the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis is unknown. However, the effect of pimavanserin could be mediated through a combination of inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at serotonin 5-HT2C receptors. In vitro, pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A receptors with high binding affinity (Ki value 0.087 nM) and at serotonin 5-HT2C receptors with lower binding affinity (Ki value 0.44 nM). Pimavanserin shows low binding to sigma 1 receptors (Ki value 120 nM) and has no appreciable affinity (Ki value >300 nM), to serotonin 5-HT2B, dopaminergic (including D2), muscarinic, histaminergic, or adrenergic receptors, or to calcium channels. Pimavanserin was approved by the FDA to treat hallucinations and delusions associated with psychosis experienced by some people with Parkinson's disease on April 29, 2016.   NCATS

Chemistry

  • SMILES: CC(C)COc1ccc(CNC(=O)N(Cc2ccc(F)cc2)C2CCN(C)CC2)cc1
  • InChIKey: RKEWSXXUOLRFBX-UHFFFAOYSA-N
  • Mol. Mass: 427.56
  • ALogP: 4.67
  • ChEMBL Molecules:
    pimavanserin  
    pimavanserin tartrate  
More Chemistry

Pharmacology

  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: Yes
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$70.8527 - $100.6690
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

acp103 | acp 103 | acp-103 | bis(1-(4-fluorobenzyl)-1-(1-methylpiperidin-4-yl)-3-(4-(2-methylpropoxy)benzyl)urea) (2r,3r)-2,3-dihydroxybutanedioate | n-(4-fluorophenylmethyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide | nuplazid | pimavanserin | pimavanserin tartrate | urea, n-((4-fluorophenyl)methyl)-n-(1-methyl-4-piperidinyl)-n'-((4-(2-methylpropoxy)phenyl)methyl)-, (2r,3r)-2,3-dihydroxybutanedioate (2:1)

Organizations (20)

Research & Development (16)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (5)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (16)

Approved Indications (3)


 

Hallucinations

Parkinson Disease

Psychotic Disorders

Experimental Indications - Clinical Trial Phases 1-4 (16)


 

Alzheimer Disease (Phase 2)

Autism Spectrum Disorder (Phase 2/Phase 3)

Dementia (Phase 3)

Depression (Phase 3)

Disruptive, Impulse Control, and Conduct Disorders (Phase 2)

Dyskinesias (Phase 2)

Hallucinations (Phase 2)

Lewy Body Disease (Phase 4)

Neurodegenerative Diseases (Phase 4)

Parkinson Disease ()

Psychotic Disorders (Phase 2)

Schizophrenia (Phase 3)

Sleep Initiation and Maintenance Disorders (Phase 4)

Stress Disorders, Post-Traumatic (Phase 4)

Tardive Dyskinesia (Early Phase 1)

Tourette Syndrome (Early Phase 1)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 40
  • # of Trial Organizations: 16

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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