NAV

Pimavanserin

Identification

Summary

Pimavanserin is a second generation atypical antipsychotic used for the treatment of hallucinations and delusions caused by Parkinson's Disease.

Brand Names
Nuplazid
Generic Name
Pimavanserin
DrugBank Accession Number
DB05316
Background

Pimavanserin is an atypical antipsychotic indicated for the treatment of psychiatric disorders.19 Although the exact mechanism of action is unknown, it is thought that pimavanserin interacts with the serotonin receptors, particularly the 5-HT2A and HT2C receptors.19 Unlike other atypical antipsychotics, pimavanserin lacks inherent dopaminergic activity. In fact, pimavanserin is the first antipsychotic drug without D2 blocking activity. Therefore, pimavanserin can be used to treat psychotic symptoms without causing extrapyramidal or worsening motor symptoms.6,3

Pimavanserin is marketed under the trade name NUPLAZID and developed by Acadia Pharmaceuticals.11 It was approved by the FDA in April 2016 for the treatment of hallucinations and delusions associated with Parkinson's disease psychosis thanks to favorable results from a pivotal six-week, randomized, placebo-controlled, parallel-group study.20,3 Pimavanserin was also under review as a potential treatment for dementia-related psychosis; however, as of April 2021, FDA approval has not been granted for this indication despite previous breakthrough designation.18

Type
Small Molecule
Groups
Approved, Investigational
Structure
3D
Similar Structures
Weight
Average: 427.564
Monoisotopic: 427.26350551
Chemical Formula
C25H34FN3O2
Synonyms
  • Pimavanserin
External IDs
  • ACP 103
  • ACP-103
  • ACP103
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Pharmacology

Indication

Pimavanserin is indicated for the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis.14

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofDelusions•••••••••••••••••••• ••••••
Management ofHallucinations•••••••••••••••••••• ••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Pimavanserin's unique actions on serotonin receptors improve symptoms of hallucinations and delusions associated with Parkinson's disease.2 In clinical studies, 80.5% of individuals treated with pimavanserin reported improvement in symptoms. Pimavanserin does not worsen motor functioning in patients with Parkinson's disease psychosis.9

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.19

The effect of pimavanserin on the QTc interval was evaluated in a randomized placebo- and positive-controlled double-blind, multiple-dose parallel thorough QTc study in 252 healthy subjects. A central tendency analysis of the QTc data at steady-state demonstrated that the maximum mean change from baseline (upper bound of the two-sided 90% CI) was 13.5 (16.6) msec at a dose of twice the therapeutic dose. A pharmacokinetic/pharmacodynamic analysis with pimavanserin suggested a concentration-dependent QTc interval prolongation in the therapeutic range.19

In the 6-week, placebo-controlled effectiveness studies, mean increases in QTc interval of ~5-8 msec were observed in patients receiving once-daily doses of pimavanserin 34 mg. These data are consistent with the profile observed in a thorough QT study in healthy subjects. Sporadic QTcF values ≥500 msec and change from baseline values ≥60 msec were observed in subjects treated with pimavanserin 34 mg; although the incidence was generally similar for pimavanserin and placebo groups. There were no reports of torsade de pointes or any differences from placebo in the incidence of other adverse reactions associated with delayed ventricular repolarization in studies of pimavanserin, including those patients with hallucinations and delusions associated with Parkinson’s disease psychosis.19

Mechanism of action

Parkinson's disease psychosis (PDP) is an imbalance of serotonin and dopamine from disruption of the normal balance between the serotonergic and dopaminergic receptors and neurotransmitters in the brain.10

The mechanism by which pimavanserin treats hallucinations and delusions associated with Parkinson’s disease psychosis is not fully established. It is possible that pimavanserin acts via inverse agonist and antagonist activity at serotonin 5-HT2A receptors with limited effects on serotonin 5-HT2C receptors. Pimavanserin is an inverse agonist and antagonist of serotonin 5-HT2A receptors with high binding affinity, demonstrating low binding affinity to serotonin 5-HT2C receptors. In addition, this drug exhibits low affinity binding to sigma 1 receptors.14 Pimavanserin lacks activity at muscarinic, dopaminergic, adrenergic, and histaminergic receptors, preventing various undesirable effects typically associated with antipsychotics.9

TargetActionsOrganism
A5-hydroxytryptamine receptor 2A
inverse agonist
Humans
U5-hydroxytryptamine receptor 2C
inverse agonist
Humans
USigma non-opioid intracellular receptor 1
binder
Humans
Absorption

The median Tmax of pimavanserin in clinical studies was 6 hours, regardless of the dose. The bioavailability of an oral tablet of pimavanserin and a solution were almost identical.20 Ingestion of a high-fat meal had no significant effect on the rate (Cmax) and extent (AUC) of pimavanserin exposure. Cmax decreased by about 9% while AUC increased by about 8% with a high-fat meal.

The major active circulating N-desmethylated metabolite, AC-279, has a median Tmax of 6 hours.20

Volume of distribution

Following administration of a single dose of 34 mg, the average apparent volume of distribution was 2173 L in clinical studies.20

Protein binding

Pimavanserin is highly protein-bound (~95%) in human plasma. Protein binding appeared to be dose-independent and did not change significantly over dosing time from Day 1 to Day 14.20

Metabolism

Pimavanserin is mainly metabolized CYP3A4 and CYP3A5 hepatic cytochrome enzymes, and to a lesser extent by CYP2J2, CYP2D6, and other cytochrome and flavin-containing monooxygenase enzymes. CYP3A4 metabolizes pimavanserin to its major active metabolite, AC-279.14

Route of elimination

Approximately 0.55% of the 34 mg oral dose of 14C-pimavanserin was eliminated as unchanged drug in urine and 1.53% was eliminated in feces after 10 days. Less than 1% of the administered dose of pimavanserin and its active metabolite AC-279 were recovered in urine.20

Half-life

The average plasma half-lives for pimavanserin and its active metabolite (AC-279) are estimated at 57 hours and 200 hours, respectively.14

Clearance

Not Available

Adverse Effects
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Toxicity

LD50 information for pimavanserin is not readily available in the literature. Pre-marketing clinical trials involving pimavanserin in approximately 1200 subjects and patients do not report symptoms of overdose. In healthy subject studies, nausea and vomiting were reported. There are no known antidotes for an overdose with this drug. Cardiovascular monitoring should begin immediately in the case of an overdose and continuous ECG monitoring is recommended. If antiarrhythmic drugs are administered in an overdose of pimavanserin, disopyramide, procainamide, and quinidine should not be used due to their potential for QT-prolonging effects. In the case of an overdose, consider the 57 hour plasma half-life of pimavanserin and the possibility of multiple drug involvement.14

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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interactions in your software
AbametapirThe serum concentration of Pimavanserin can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Pimavanserin can be increased when combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Pimavanserin.
AcalabrutinibThe metabolism of Acalabrutinib can be decreased when combined with Pimavanserin.
AcebutololThe risk or severity of QTc prolongation can be increased when Acebutolol is combined with Pimavanserin.
Food Interactions
  • Avoid grapefruit products. Dose adjustment may be necessary if taking grapefruit products or other CYP3A4 inhibitors.
  • Avoid St. John's Wort. This may induce the CYP3A4 metabolism of pimavanserin, which may cause reduced efficacy.
  • Take with or without food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Pimavanserin tartrateNA83F1SJSR706782-28-7RGSULKHNAKTFIZ-CEAXSRTFSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
NuplazidTablet, coated17 mg/1OralACADIA Pharmaceuticals Inc2016-04-292022-04-30US flag
NuplazidCapsule34 mg/1OralAcadia Pharmaceuticals Inc.2018-06-28Not applicableUS flag
NuplazidTablet, coated10 mg/1OralAcadia Pharmaceuticals Inc.2018-06-28Not applicableUS flag

Categories

ATC Codes
N05AX17 — Pimavanserin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenol ethers
Sub Class
Not Available
Direct Parent
Phenol ethers
Alternative Parents
Phenoxy compounds / Fluorobenzenes / Alkyl aryl ethers / Piperidines / Aryl fluorides / Ureas / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organofluorides
show 3 more
Substituents
Alkyl aryl ether / Amine / Aromatic heteromonocyclic compound / Aryl fluoride / Aryl halide / Azacycle / Carbonic acid derivative / Carbonyl group / Ether / Fluorobenzene
show 18 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
JZ963P0DIK
CAS number
706779-91-1
InChI Key
RKEWSXXUOLRFBX-UHFFFAOYSA-N
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)
IUPAC Name
1-[(4-fluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)-3-{[4-(2-methylpropoxy)phenyl]methyl}urea
SMILES
CC(C)COC1=CC=C(CNC(=O)N(CC2=CC=C(F)C=C2)C2CCN(C)CC2)C=C1

References

Synthesis Reference

A Novel Synthesis of Pimavanserin: A Selective Serotonin 5-HT2A Receptor Inverse Agonist. (2020). Kun Hu, Meiju Zhang, Dongdong Wu, Yuxuan Xie & Jie Ren. The New Journal for Organic Synthesis Volume 52, 2020 - Issue 1. https://doi.org/10.1080/00304948.2019.1697613

General References
  1. Nordstrom AL, Mansson M, Jovanovic H, Karlsson P, Halldin C, Farde L, Vanover KE, Hacksell U, Brann MR, Davis RE, Weiner DM: PET analysis of the 5-HT2A receptor inverse agonist ACP-103 in human brain. Int J Neuropsychopharmacol. 2008 Mar;11(2):163-71. Epub 2007 Aug 21. [Article]
  2. Kianirad Y, Simuni T: Pimavanserin, a novel antipsychotic for management of Parkinson's disease psychosis. Expert Rev Clin Pharmacol. 2017 Nov;10(11):1161-1168. doi: 10.1080/17512433.2017.1369405. Epub 2017 Oct 17. [Article]
  3. Cruz MP: Pimavanserin (Nuplazid): A Treatment for Hallucinations and Delusions Associated With Parkinson's Disease. P T. 2017 Jun;42(6):368-371. [Article]
  4. Hunter NS, Anderson KC, Cox A: Pimavanserin. Drugs Today (Barc). 2015 Nov;51(11):645-52. doi: 10.1358/dot.2015.51.11.2404001. [Article]
  5. Markham A: Pimavanserin: First Global Approval. Drugs. 2016 Jul;76(10):1053-7. doi: 10.1007/s40265-016-0597-9. [Article]
  6. D'Souza RS, Hooten WM: Extrapyramidal Symptoms . [Article]
  7. Cummings JL, Devanand DP, Stahl SM: Dementia-related psychosis and the potential role for pimavanserin. CNS Spectr. 2020 Aug 19:1-9. doi: 10.1017/S1092852920001765. [Article]
  8. Stahl SM: Mechanism of action of pimavanserin in Parkinson's disease psychosis: targeting serotonin 5HT2A and 5HT2C receptors. CNS Spectr. 2016 Aug;21(4):271-5. doi: 10.1017/S1092852916000407. [Article]
  9. Tampi RR, Tampi DJ, Young JJ, Balachandran S, Hoq RA, Manikkara G: Evidence for using pimavanserin for the treatment of Parkinson's disease psychosis. World J Psychiatry. 2019 Jun 10;9(3):47-54. doi: 10.5498/wjp.v9.i3.47. eCollection 2019 Jun 10. [Article]
  10. Stahl SM: Parkinson's disease psychosis as a serotonin-dopamine imbalance syndrome. CNS Spectr. 2016 Oct;21(5):355-359. doi: 10.1017/S1092852916000602. [Article]
  11. Zahodne LB, Fernandez HH: Pathophysiology and treatment of psychosis in Parkinson's disease: a review. Drugs Aging. 2008;25(8):665-82. doi: 10.2165/00002512-200825080-00004. [Article]
  12. Yunusa I, El Helou ML, Alsahali S: Pimavanserin: A Novel Antipsychotic With Potentials to Address an Unmet Need of Older Adults With Dementia-Related Psychosis. Front Pharmacol. 2020 Feb 26;11:87. doi: 10.3389/fphar.2020.00087. eCollection 2020. [Article]
  13. Acadia pharmaceuticals pipeline [Link]
  14. FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
  15. Acadia Pharmaceuticals: Pimavanserin – Dementia-Related Psychosis [Link]
  16. Spectrum Chemical: Pimavanserin MSDS [Link]
  17. DailyMed Label: Nuplazid (pimavanserin tartrate) capsule [Link]
  18. BusinessWire: Acadia Pharmaceuticals Receives Complete Response Letter from U.S. FDA for Supplemental New Drug Application for Pimavanserin for the Treatment of Hallucinations and Delusions Associated with Dementia-Related Psychosis [Link]
  19. FDA Approved Drug Products: NUPLAZID® (pimavanserin) capsules/tablets, for oral use (September 2023) [Link]
  20. Acadia Pharmaceuticals Announces Label Update for NUPLAZID® (pimavanserin) [Link]
Human Metabolome Database
HMDB0256551
PubChem Compound
10071196
PubChem Substance
175426976
ChemSpider
8246736
BindingDB
139370
RxNav
1791685
ChEBI
133017
ChEMBL
CHEMBL2111101
ZINC
ZINC000016159083
Wikipedia
Pimavanserin

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4CompletedTreatmentInsomnia / Post Traumatic Stress Disorder (PTSD)1
4CompletedTreatmentParkinson's Disease Psychosis1
4RecruitingBasic ScienceNeurodegenerative Disorders / Parkinson's Disease (PD) / Parkinson's Disease Psychosis1
4RecruitingTreatmentDementia With Lewy Body Disease / Parkinson's Disease Psychosis1
4RecruitingTreatmentParkinson's Disease Psychosis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral34 mg/1
Tablet, coatedOral10 mg/1
Tablet, coatedOral17 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9296694No2016-03-292021-03-06US flag
US8110574No2012-02-072020-12-13US flag
US7601740No2009-10-132027-06-17US flag
US7732615No2010-06-082028-06-03US flag
US7923564No2011-04-122025-09-26US flag
US6756393No2004-06-292021-03-06US flag
US7858789No2010-12-282020-12-13US flag
US7115634No2006-10-032021-10-06US flag
US7659285No2010-02-092026-08-24US flag
US6815458No2004-11-092021-03-06US flag
US8618130No2013-12-312024-01-15US flag
US8921393No2014-12-302024-01-15US flag
US9566271No2017-02-142024-01-15US flag
US9765053No2017-09-192022-07-27US flag
US10028944No2018-07-242024-01-15US flag
US10449185No2019-10-222038-08-27US flag
US10517860No2019-12-312037-03-23US flag
US10646480No2020-05-122038-08-27US flag
US10849891No2020-12-012038-08-27US flag
US10953000No2021-03-232037-03-23US flag
US11452721No2018-08-272038-08-27US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)117-119http://www.chemspider.com/Chemical-Structure.8246736.html
boiling point (°C)604.2±55.0https://www.chemicalbook.com/ProductChemicalPropertiesCB8966229_EN.htm
pKa13.52±0.46https://www.chemicalbook.com/ProductChemicalPropertiesCB8966229_EN.htm
Predicted Properties
PropertyValueSource
Water Solubility0.00748 mg/mLALOGPS
logP4.19ALOGPS
logP4.01Chemaxon
logS-4.8ALOGPS
pKa (Strongest Acidic)15.06Chemaxon
pKa (Strongest Basic)8.44Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count3Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area44.81 Å2Chemaxon
Rotatable Bond Count8Chemaxon
Refractivity122.93 m3·mol-1Chemaxon
Polarizability47.76 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption-0.696
Blood Brain Barrier-0.8018
Caco-2 permeable-0.6395
P-glycoprotein substrateSubstrate0.8782
P-glycoprotein inhibitor INon-inhibitor0.685
P-glycoprotein inhibitor IINon-inhibitor0.8743
Renal organic cation transporterNon-inhibitor0.799
CYP450 2C9 substrateNon-substrate0.7844
CYP450 2D6 substrateNon-substrate0.8342
CYP450 3A4 substrateSubstrate0.5769
CYP450 1A2 substrateNon-inhibitor0.8285
CYP450 2C9 inhibitorNon-inhibitor0.7474
CYP450 2D6 inhibitorNon-inhibitor0.8458
CYP450 2C19 inhibitorNon-inhibitor0.8247
CYP450 3A4 inhibitorNon-inhibitor0.9552
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8855
Ames testNon AMES toxic0.6638
CarcinogenicityNon-carcinogens0.8967
BiodegradationNot ready biodegradable0.9775
Rat acute toxicity2.4414 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8668
hERG inhibition (predictor II)Inhibitor0.7703
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-004i-0040900000-edef98113b8bec750243
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-2360900000-1cd0e7867c168061641c
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-05i4-9662600000-d4777bde0cb19ebc76a5
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-00di-1390000000-a7660fb9aa7240c7c911
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0fdk-4912000000-55c0175992a03a5fdede
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-06r7-4941100000-0b8e0194706876ebbded
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-206.90457
predicted
DeepCCS 1.0 (2019)
[M+H]+209.26257
predicted
DeepCCS 1.0 (2019)
[M+Na]+216.14374
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Details1. 5-hydroxytryptamine receptor 2A
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inverse agonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Friedman JH: Pimavanserin for the treatment of Parkinson's disease psychosis. Expert Opin Pharmacother. 2013 Oct;14(14):1969-75. doi: 10.1517/14656566.2013.819345. [Article]
  2. Nordstrom AL, Mansson M, Jovanovic H, Karlsson P, Halldin C, Farde L, Vanover KE, Hacksell U, Brann MR, Davis RE, Weiner DM: PET analysis of the 5-HT2A receptor inverse agonist ACP-103 in human brain. Int J Neuropsychopharmacol. 2008 Mar;11(2):163-71. Epub 2007 Aug 21. [Article]
  3. Hunter NS, Anderson KC, Cox A: Pimavanserin. Drugs Today (Barc). 2015 Nov;51(11):645-52. doi: 10.1358/dot.2015.51.11.2404001. [Article]
  4. Hawkins T, Berman BD: Pimavanserin: A novel therapeutic option for Parkinson disease psychosis. Neurol Clin Pract. 2017 Apr;7(2):157-162. doi: 10.1212/CPJ.0000000000000342. [Article]
  5. FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
Details2. 5-hydroxytryptamine receptor 2C
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inverse agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Stahl SM: Mechanism of action of pimavanserin in Parkinson's disease psychosis: targeting serotonin 5HT2A and 5HT2C receptors. CNS Spectr. 2016 Aug;21(4):271-5. doi: 10.1017/S1092852916000407. [Article]
Details3. Sigma non-opioid intracellular receptor 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Opioid receptor activity
Specific Function
Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma m...
Gene Name
SIGMAR1
Uniprot ID
Q99720
Uniprot Name
Sigma non-opioid intracellular receptor 1
Molecular Weight
25127.52 Da
References
  1. Howland RH: Pimavanserin: An Inverse Agonist Antipsychotic Drug. J Psychosoc Nurs Ment Health Serv. 2016 Jun 1;54(6):21-4. doi: 10.3928/02793695-20160523-01. [Article]

Enzymes

Details1. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Kitten AK, Hallowell SA, Saklad SR, Evoy KE: Pimavanserin: A Novel Drug Approved to Treat Parkinson's Disease Psychosis. Innov Clin Neurosci. 2018 Feb 1;15(1-2):16-22. [Article]
  2. Tampi RR, Tampi DJ, Young JJ, Balachandran S, Hoq RA, Manikkara G: Evidence for using pimavanserin for the treatment of Parkinson's disease psychosis. World J Psychiatry. 2019 Jun 10;9(3):47-54. doi: 10.5498/wjp.v9.i3.47. eCollection 2019 Jun 10. [Article]
  3. FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
Details2. Cytochrome P450 3A5
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Kitten AK, Hallowell SA, Saklad SR, Evoy KE: Pimavanserin: A Novel Drug Approved to Treat Parkinson's Disease Psychosis. Innov Clin Neurosci. 2018 Feb 1;15(1-2):16-22. [Article]
  2. Tampi RR, Tampi DJ, Young JJ, Balachandran S, Hoq RA, Manikkara G: Evidence for using pimavanserin for the treatment of Parkinson's disease psychosis. World J Psychiatry. 2019 Jun 10;9(3):47-54. doi: 10.5498/wjp.v9.i3.47. eCollection 2019 Jun 10. [Article]
  3. FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
Details3. Cytochrome P450 2J2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
This enzyme metabolizes arachidonic acid predominantly via a NADPH-dependent olefin epoxidation to all four regioisomeric cis-epoxyeicosatrienoic acids. One of the predominant enzymes responsible f...
Gene Name
CYP2J2
Uniprot ID
P51589
Uniprot Name
Cytochrome P450 2J2
Molecular Weight
57610.165 Da
References
  1. Kitten AK, Hallowell SA, Saklad SR, Evoy KE: Pimavanserin: A Novel Drug Approved to Treat Parkinson's Disease Psychosis. Innov Clin Neurosci. 2018 Feb 1;15(1-2):16-22. [Article]
  2. FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
Details4. Cytochrome P450 2D6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Kitten AK, Hallowell SA, Saklad SR, Evoy KE: Pimavanserin: A Novel Drug Approved to Treat Parkinson's Disease Psychosis. Innov Clin Neurosci. 2018 Feb 1;15(1-2):16-22. [Article]
  2. FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]

Drug created at November 18, 2007 18:23 / Updated at February 02, 2024 22:52