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
- Weight
- Average: 427.564
Monoisotopic: 427.26350551 - Chemical Formula
- C25H34FN3O2
- Synonyms
- Pimavanserin
- External IDs
- ACP 103
- ACP-103
- ACP103
Pharmacology
- Indication
Pimavanserin is indicated for the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis.14
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Delusions •••••••••••• •••••••• •••••• Management of Hallucinations •••••••••••• •••••••• •••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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
Target Actions Organism A5-hydroxytryptamine receptor 2A inverse agonistHumans U5-hydroxytryptamine receptor 2C inverse agonistHumans USigma non-opioid intracellular receptor 1 binderHumans - 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Pimavanserin can be increased when it is combined with Abametapir. Abatacept The metabolism of Pimavanserin can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Pimavanserin. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Pimavanserin. Acebutolol The 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
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Pimavanserin tartrate NA83F1SJSR 706782-28-7 RGSULKHNAKTFIZ-CEAXSRTFSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nuplazid Tablet, coated 17 mg/1 Oral ACADIA Pharmaceuticals Inc 2016-04-29 2022-04-30 US Nuplazid Capsule 34 mg/1 Oral Acadia Pharmaceuticals Inc. 2018-06-28 Not applicable US Nuplazid Tablet, coated 10 mg/1 Oral Acadia Pharmaceuticals Inc. 2018-06-28 Not applicable US
Categories
- ATC Codes
- N05AX17 — Pimavanserin
- Drug Categories
- Amides
- Antidepressive Agents
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Substrates
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- Psycholeptics
- Serotonin 5-HT2 Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- 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
- 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]
- 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]
- Cruz MP: Pimavanserin (Nuplazid): A Treatment for Hallucinations and Delusions Associated With Parkinson's Disease. P T. 2017 Jun;42(6):368-371. [Article]
- 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]
- Markham A: Pimavanserin: First Global Approval. Drugs. 2016 Jul;76(10):1053-7. doi: 10.1007/s40265-016-0597-9. [Article]
- D'Souza RS, Hooten WM: Extrapyramidal Symptoms . [Article]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- Acadia pharmaceuticals pipeline [Link]
- FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
- Acadia Pharmaceuticals: Pimavanserin – Dementia-Related Psychosis [Link]
- Spectrum Chemical: Pimavanserin MSDS [Link]
- DailyMed Label: Nuplazid (pimavanserin tartrate) capsule [Link]
- 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]
- FDA Approved Drug Products: NUPLAZID® (pimavanserin) capsules/tablets, for oral use (September 2023) [Link]
- Acadia Pharmaceuticals Announces Label Update for NUPLAZID® (pimavanserin) [Link]
- External Links
- Human Metabolome Database
- HMDB0256551
- PubChem Compound
- 10071196
- PubChem Substance
- 175426976
- ChemSpider
- 8246736
- BindingDB
- 139370
- 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);">
Phase Status Purpose Conditions Count 4 Completed Treatment Insomnia / Post Traumatic Stress Disorder (PTSD) 1 4 Completed Treatment Parkinson's Disease Psychosis 1 4 Recruiting Basic Science Neurodegenerative Disorders / Parkinson's Disease (PD) / Parkinson's Disease Psychosis 1 4 Recruiting Treatment Dementia With Lewy Body Disease / Parkinson's Disease Psychosis 1 4 Recruiting Treatment Parkinson's Disease Psychosis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 34 mg/1 Tablet, coated Oral 10 mg/1 Tablet, coated Oral 17 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9296694 No 2016-03-29 2021-03-06 US US8110574 No 2012-02-07 2020-12-13 US US7601740 No 2009-10-13 2027-06-17 US US7732615 No 2010-06-08 2028-06-03 US US7923564 No 2011-04-12 2025-09-26 US US6756393 No 2004-06-29 2021-03-06 US US7858789 No 2010-12-28 2020-12-13 US US7115634 No 2006-10-03 2021-10-06 US US7659285 No 2010-02-09 2026-08-24 US US6815458 No 2004-11-09 2021-03-06 US US8618130 No 2013-12-31 2024-01-15 US US8921393 No 2014-12-30 2024-01-15 US US9566271 No 2017-02-14 2024-01-15 US US9765053 No 2017-09-19 2022-07-27 US US10028944 No 2018-07-24 2024-01-15 US US10449185 No 2019-10-22 2038-08-27 US US10517860 No 2019-12-31 2037-03-23 US US10646480 No 2020-05-12 2038-08-27 US US10849891 No 2020-12-01 2038-08-27 US US10953000 No 2021-03-23 2037-03-23 US US11452721 No 2018-08-27 2038-08-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 117-119 http://www.chemspider.com/Chemical-Structure.8246736.html boiling point (°C) 604.2±55.0 https://www.chemicalbook.com/ProductChemicalPropertiesCB8966229_EN.htm pKa 13.52±0.46 https://www.chemicalbook.com/ProductChemicalPropertiesCB8966229_EN.htm - Predicted Properties
Property Value Source Water Solubility 0.00748 mg/mL ALOGPS logP 4.19 ALOGPS logP 4.01 Chemaxon logS -4.8 ALOGPS pKa (Strongest Acidic) 15.06 Chemaxon pKa (Strongest Basic) 8.44 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 44.81 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 122.93 m3·mol-1 Chemaxon Polarizability 47.76 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.696 Blood Brain Barrier - 0.8018 Caco-2 permeable - 0.6395 P-glycoprotein substrate Substrate 0.8782 P-glycoprotein inhibitor I Non-inhibitor 0.685 P-glycoprotein inhibitor II Non-inhibitor 0.8743 Renal organic cation transporter Non-inhibitor 0.799 CYP450 2C9 substrate Non-substrate 0.7844 CYP450 2D6 substrate Non-substrate 0.8342 CYP450 3A4 substrate Substrate 0.5769 CYP450 1A2 substrate Non-inhibitor 0.8285 CYP450 2C9 inhibitor Non-inhibitor 0.7474 CYP450 2D6 inhibitor Non-inhibitor 0.8458 CYP450 2C19 inhibitor Non-inhibitor 0.8247 CYP450 3A4 inhibitor Non-inhibitor 0.9552 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8855 Ames test Non AMES toxic 0.6638 Carcinogenicity Non-carcinogens 0.8967 Biodegradation Not ready biodegradable 0.9775 Rat acute toxicity 2.4414 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8668 hERG inhibition (predictor II) Inhibitor 0.7703
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-004i-0040900000-edef98113b8bec750243 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-004i-2360900000-1cd0e7867c168061641c Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-05i4-9662600000-d4777bde0cb19ebc76a5 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-00di-1390000000-a7660fb9aa7240c7c911 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0fdk-4912000000-55c0175992a03a5fdede Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-06r7-4941100000-0b8e0194706876ebbded Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 206.90457 predictedDeepCCS 1.0 (2019) [M+H]+ 209.26257 predictedDeepCCS 1.0 (2019) [M+Na]+ 216.14374 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- 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
- 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]
- 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]
- 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]
- 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]
- FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
- 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
- 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]
- 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
- 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
- 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
- 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]
- 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]
- FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
- 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
- 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]
- 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]
- FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use [Link]
- 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
- 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
Drug created at November 18, 2007 18:23 / Updated at February 02, 2024 22:52