Page last updated: 2024-11-12

pimavanserin

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Description

pimavanserin: A 5-HT(2A) inverse agonist; ACP-103 is the dihydroxybutanedioate (2:1) salt. It is used to treat hallucinations and delusions associated with PARKINSON DISEASE; structure in first source. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

pimavanserin : A member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of hallucinations and delusions associated with Parkinson's disease. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID10071196
CHEMBL ID2111101
CHEBI ID133017
SCHEMBL ID675165
MeSH IDM0498685

Synonyms (51)

Synonym
AC-5273 ,
acp-103
CHEBI:133017 ,
pimavanserin
706779-91-1
n-(4-fluorophenylmethyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl) carbamide
n-[(4-fluorophenyl)methyl]-n-(1-methylpiperidin-4-yl)-n'-{[4-(2-methylpropoxy)phenyl]methyl}urea
FT-0653701
n-[(4-fluorophenyl)methyl]-n-(1-methyl-4-piperidinyl)-n'-[[4-(2-methylpropoxy)phenyl]methyl]urea;
A836958
n-(4-fluorophenylmethyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide
unii-jz963p0dik
pimavanserin [inn]
jz963p0dik ,
AKOS015902593
1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea
pimavanserin [mi]
pimavanserin [who-dd]
DB05316
CS-3378
HY-14557
SCHEMBL675165
pimanavserin
ME-0240
J-503297
bdbm139370
RKEWSXXUOLRFBX-UHFFFAOYSA-N
CHEMBL2111101
nuplazid (proposed trade name)
gtpl8423
1-[(4-fluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)-3-[[4-(2-methylpropoxy)phenyl]methyl]urea
n-[(4-fluorophenyl)methyl]-n-(1-methyl-4-piperidinyl)-n'-[[4-(2-methylpropoxy)phenyl]methyl]-urea; n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-[[4-(2-methylpropyloxy)phenyl]methyl]carbamide; pimavanserin
NCGC00390656-01
methyltrimethylacetate
pimavanserin(acp-103)
706779-91-1 (free base)
pimavanserin free base
DTXSID90990906
BCP11618
Q7194603
EX-A4895
SB16963
HMS3742A03
NCGC00390656-02
EN300-19659487
1-[(4-fluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)-3-{[4-(2-methylpropoxy)phenyl]methyl}urea
pimavanserinum
n05ax17
pimavanserina
n-((4-fluorophenyl)methyl)-n-(1-methylpiperidin-4-yl)-n'-((4-(2-methylpropoxy)phenyl)methyl)urea
pimavanserine

Research Excerpts

Overview

Pimavanserin is a 5HT2A inverse agonist that is the only Food and Drug Administration-approved treatment for Parkinson disease (PD) psychosis.

ExcerptReferenceRelevance
"Pimavanserin is a selective 5-HT"( Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
Dai, Y; Du, G; Liu, B; Liu, W; Ma, M; Tian, J; Wang, W; Xu, H; Yang, H; Yang, Y; Ye, L; Zhang, J; Zhang, R; Zheng, L; Zhu, X; Zou, F, 2022
)
2.16
"Pimavanserin is a novel agent approved for the treatment of Parkinson's disease and exerts neuroprotective properties."( The protective effects of Pimavanserin against cerebral ischemia-induced brain injury.
Li, X; Tian, X, 2021
)
1.64
"Pimavanserin is a selective serotonin 5-HT 2A receptor inverse agonist/antagonist being investigated in patients with negative symptoms of schizophrenia. "( Pimavanserin Exposure-Response Analyses in Patients With Schizophrenia: Results From the Phase 2 ADVANCE Study.
Bugarski-Kirola, D; Darwish, M; DeKarske, D; Jaworowicz, D; Owen, J; Passarell, J; Stankovic, S,
)
3.02
"Pimavanserin is a serotonin 5HT-2A receptor inverse agonist that has recently been shown to reduce psychosis related to dementia."( [Pimavanserin and trazodone combination in behavioral disorders in severe dementia with Lewy bodies].
Blanc, F; Javelot, H; Merignac, J; Moog, C; Muller, C; Schorr, B, 2023
)
2.54
"Pimavanserin is a 5-hydroxytryptamine-2A antagonist and inverse receptor agonist. "( A Phase 2, Randomized, Double-Blind, Placebo-Controlled Study of Adjunctive Pimavanserin in Patients With Major Depressive Disorder and an Inadequate Response to Therapy (CLARITY).
Dirks, B; Fava, M; Freeman, MP; Liu, K; Papakostas, GI; Shelton, RC; Stankovic, S; Thase, ME; Trivedi, MH, 2019
)
2.19
"Pimavanserin is a receptor antagonist (5-HT2A, 5-HT2C) that has been given market authorization for psychosis occurring in Parkinson's disease."( New antipsychotic drugs for the treatment of agitation and psychosis in Alzheimer's disease: focus on brexpiprazole and pimavanserin.
Cannavò, D; Caraci, F; Caruso, G; Drago, F; Leggio, GM; Salomone, S; Santagati, M, 2020
)
1.49
"Pimavanserin is a novel 5-HT"( Pimavanserin: A Novel Antipsychotic for Parkinson's Disease Psychosis.
Bozymski, KM; Crouse, EL; Gatesman, TL; Lowe, DK; Pasternak, KM, 2017
)
3.34
"Pimavanserin is an effective treatment for PDP, and, like clozapine, it has very few negative effects on motor skills."( [Pimavanserin: a new treatment for the Parkinson's disease psychosis].
Duits, JH; Martens, HJM; Ongering, MS; Schulte, PFJ,
)
1.76
"Pimavanserin is a selective 5-HT"( Evaluation of the safety, tolerability, and efficacy of pimavanserin versus placebo in patients with Alzheimer's disease psychosis: a phase 2, randomised, placebo-controlled, double-blind study.
Ballard, C; Banister, C; Coate, B; Cummings, J; Demos, G; Khan, Z; Owen, R; Stankovic, S; Youakim, JM, 2018
)
2.17
"Pimavanserin (Pim) is a 5HT2A inverse agonist that is the only Food and Drug Administration-approved treatment for Parkinson disease (PD) psychosis. "( Pimavanserin for Psychotic Symptoms in People With Parkinsonism: A Second Chart Review.
Friedman, JH,
)
3.02
"Pimavanserin is a 5-HT2A receptor inverse agonist/antagonist and is approved in the United States for the treatment of hallucinations and delusions associated with Parkinson's disease psychosis."( Pimavanserin in Alzheimer's Disease Psychosis: Efficacy in Patients with More Pronounced Psychotic Symptoms.
Ballard, C; Coate, B; Stankovic, S; Youakim, JM, 2019
)
3.4
"Pimavanserin is a first-in-class selective serotonin 5-HT2A receptor inverse agonist approved for the treatment of Parkinson disease psychosis. "( Can pimavanserin help patients with Parkinson disease psychosis?
Canal, C; de la Cruz, J, 2019
)
2.51
"Pimavanserin is a newly approved treatment for Parkinson's disease psychosis, but real-world experience with pimavanserin has been limited by small sample sizes and limited assessment of longitudinal outcomes."( Pimavanserin for Psychosis in Parkinson's Disease-Related Disorders: A Retrospective Chart Review.
Claassen, DO; Darby, RR; Farooque, A; Sellers, J, 2019
)
2.68
"Pimavanserin is a selective serotonin 2A receptor (5-HT2AR) inverse agonist that has shown promise for treatment of psychotic symptoms in patients with Parkinson's disease. "( (11)C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand.
Andersen, VL; Dyssegaard, A; Hansen, HD; Herth, MM; Knudsen, GM; Kristensen, JL, 2015
)
2.12
"Pimavanserin (ACP-103) is a selective inverse agonist of the 5-hydroxytryptamine 2A (5-HT2A) receptor intended to treat patients with Parkinson's disease psychosis (PDP). "( Pimavanserin.
Anderson, KC; Cox, A; Hunter, NS, 2015
)
3.3
"Pimavanserin is an inverse agonist at the 5HT2A receptor, with a lower binding affinity at the serotonin-2C receptor and sigma 1 receptor, but no significant binding to dopamine or other receptors."( Pimavanserin: An Inverse Agonist Antipsychotic Drug.
Howland, RH, 2016
)
2.6
"Pimavanserin (Nuplazid™) is a selective and potent serotonin 2A (5-HT2A) receptor inverse agonist and antagonist developed by ACADIA Pharmaceuticals that has been approved in the US as a treatment for patients with hallucinations and delusions associated with Parkinson's disease psychosis. "( Pimavanserin: First Global Approval.
Markham, A, 2016
)
3.32
"Pimavanserin is an antipsychotic with a unique mechanism of action (5-HT2A receptor inverse agonist) and no measurable dopaminergic activity; it has been demonstrated to be efficacious, well tolerated and safe for the treatment of PDP. "( Pimavanserin for the treatment of Parkinson's disease psychosis.
Chendo, I; Ferreira, JJ, 2016
)
3.32
"Pimavanserin is a new 5-HT2A receptor acting drug that has been given market authorization for psychosis in Parkinson׳s disease."( Inverse agonists - What do they mean for psychiatry?
Blier, P; Drago, F; Nutt, D; Stahl, S; Wilson, S; Zohar, J, 2017
)
1.18

Effects

ExcerptReferenceRelevance
"Pimavanserin has a unique mechanism of action."( A New Hope in Alzheimer's Disease Psychosis: Pimavanserin.
Akın, M; Kurhan, F, 2023
)
1.89

Actions

ExcerptReferenceRelevance
"Pimavanserin displays nanomolar potency as a 5-HT2A receptor inverse agonist, selectivity for 5-HT2A over 5-HT2C receptors, and no meaningful activity at any other G-protein coupled receptor."( On the discovery and development of pimavanserin: a novel drug candidate for Parkinson's psychosis.
Burstein, ES; Hacksell, U; McFarland, K; Mills, RG; Williams, H, 2014
)
1.4

Treatment

Pimavanserin is a selective serotonin 5-HT(2A) receptor inverse agonist. Treatment prevented 2,5-dimethoxy-4-iodoamphetamine hydrochloride-induced head twitches. It reversed the augmented locomotor response to amphetamine.

ExcerptReferenceRelevance
"Pimavanserin-treated patients with ≥50% response in psychotic symptoms (n = 44) showed a greater improvement in agitation and aggression symptoms on the NPI-NH domain C (week six, least squares mean [LSM] difference = -3.64, t = -4.69, P < .0001) and the CMAI-SF (week six, LSM difference = -3.71, t = -2.01, P = .0483) than nonresponders (n = 32). "( Evaluation of the efficacy of pimavanserin in the treatment of agitation and aggression in patients with Alzheimer's disease psychosis: A post hoc analysis.
Abler, V; Ballard, CG; Coate, B; Foff, E; Stankovic, S, 2020
)
2.29
"Treatment with pimavanserin showed an acceptable tolerability profile."( Pimavanserin in Alzheimer's Disease Psychosis: Efficacy in Patients with More Pronounced Psychotic Symptoms.
Ballard, C; Coate, B; Stankovic, S; Youakim, JM, 2019
)
2.3
"Treatment with pimavanserin, a selective serotonin 5-HT(2A) receptor inverse agonist, prevented 2,5-dimethoxy-4-iodoamphetamine hydrochloride-induced head twitches, reversed the augmented locomotor response to amphetamine, and normalized prepulse inhibition in mice with amyloid pathology."( Pimavanserin, a 5-HT2A receptor inverse agonist, reverses psychosis-like behaviors in a rodent model of Alzheimer's disease.
Bonhaus, DW; McFarland, K; Price, DL, 2012
)
2.16

Toxicity

Common adverse events were falls, urinary tract infections, and agitation. Safety, including collection of adverse events and the Mini-Mental State Examination (MMSE) and Movement Disorder Society-sponsored revision of the Unified Parkinson's Disease Rating Scale Part III (MDS-UPDRS III) was assessed.

ExcerptReferenceRelevance
"To establish the mortality risk and adverse events associated with the use of atypical antipsychotic medications in people with Parkinson disease psychosis (PDP) in a clinically defined trial cohort."( Impact of Current Antipsychotic Medications on Comparative Mortality and Adverse Events in People With Parkinson Disease Psychosis.
Ballard, C; Burn, DJ; Coate, B; Corbett, A; Isaacson, S; Mills, R; Pahwa, R; Rascol, O; Williams, H, 2015
)
0.42
"Safety assessments at 2 weeks; 1, 3, 6, 9, and 12 months; and every 6 months thereafter, including evaluation of adverse events (AEs), vital signs, weight, physical examinations, 12-lead electrocardiograms, clinical laboratory tests (serum chemistry, hematology, and urinalysis), and the Unified Parkinson's Disease Rating Scale Parts II and III (UPDRS-II+III, activities of daily living and motor impairment, respectively)."( Impact of Current Antipsychotic Medications on Comparative Mortality and Adverse Events in People With Parkinson Disease Psychosis.
Ballard, C; Burn, DJ; Coate, B; Corbett, A; Isaacson, S; Mills, R; Pahwa, R; Rascol, O; Williams, H, 2015
)
0.42
" Common adverse events were falls (21 [23%] of 90 participants in the pimavanserin group vs 21 [23%] of 91 in the placebo group), urinary tract infections (20 [22%] vs 25 [28%]), and agitation (19 [21%] vs 13 [14%])."( Evaluation of the safety, tolerability, and efficacy of pimavanserin versus placebo in patients with Alzheimer's disease psychosis: a phase 2, randomised, placebo-controlled, double-blind study.
Ballard, C; Banister, C; Coate, B; Cummings, J; Demos, G; Khan, Z; Owen, R; Stankovic, S; Youakim, JM, 2018
)
0.96
" Safety was evaluated from adverse events (AEs), clinical laboratory results, motor symptoms, electrocardiograms (ECG), and mortality."( Long-term evaluation of open-label pimavanserin safety and tolerability in Parkinson's disease psychosis.
Abler, V; Azulay, JP; Ballard, CG; Demos, G; Fernandez, HH; Ferreira, JJ; Ilic, TV; Isaacson, S; Kreitzman, DL; Liu, IY; Norton, JC; Stankovic, S, 2020
)
0.84
" Safety, including collection of adverse events and the Mini-Mental State Examination (MMSE) and Movement Disorder Society-sponsored revision of the Unified Parkinson's Disease Rating Scale Part III (MDS-UPDRS III) scores, was assessed in patients who received ≥1 pimavanserin dose."( An Open-Label, 8-Week Study of Safety and Efficacy of Pimavanserin Treatment in Adults with Parkinson's Disease and Depression.
Abler, V; Aldred, JL; Alva, G; Cantillon, M; Coate, B; DeKarske, D; Jacobi, L; Norton, JC; Nunez, R, 2020
)
0.99
" Twenty-one of 47 patients experienced 42 treatment-emergent adverse events; the most common by system organ class were gastrointestinal (n = 7; 14."( An Open-Label, 8-Week Study of Safety and Efficacy of Pimavanserin Treatment in Adults with Parkinson's Disease and Depression.
Abler, V; Aldred, JL; Alva, G; Cantillon, M; Coate, B; DeKarske, D; Jacobi, L; Norton, JC; Nunez, R, 2020
)
0.81

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic sampling was measured up to 216 hours after single oral/nasogastric doses of ACP-103 and after the last dose of once-daily oral administration of ACP-103 for 14 days."( Pharmacokinetics, tolerability, and safety of ACP-103 following single or multiple oral dose administration in healthy volunteers.
Davis, RE; Mant, TG; Robbins-Weilert, D; van Kammen, DP; Vanover, KE; Weiner, DM; Wilbraham, DG, 2007
)
0.34
" This methodology was effectively used to estimate Pimavanserin in vivo human (K2EDTA) plasma concentration for a clinical pharmacokinetic study."( A Fully Validated UHPLC-MS/MS Method for the Estimation of Pimavanserin in Human (K2EDTA) Plasma and its Application to a Clinical Pharmacokinetic Study.
Aalapati, KK; Patnaik, RS; Singh, A, 2022
)
1.22

Bioavailability

ExcerptReferenceRelevance
" Limited oral bioavailability of AC-90179 likely reflects rapid metabolism rather than poor absorption."( Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
Andersson, CM; Bradley, SR; Brann, MR; Davis, RE; Hacksell, U; Harvey, SC; Kold, H; Makhay, M; Son, T; Spalding, TA; Tolf, BR; Vanover, KE; Veinbergs, I; Weiner, DM, 2004
)
0.32
"6% oral bioavailability in rats."( Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.
Andersson, CM; Brann, MR; Burstein, ES; Davis, RE; Del Tredici, AL; Gardell, LR; Geyer, MA; Harvey, SC; Lameh, J; Makhay, M; Ott, TR; Piu, F; Powell, SB; Schiffer, HH; Schlienger, N; Son, TY; Thygesen, MB; Tolf, BR; Uldam, AK; Vanover, KE; Veinbergs, I; Weiner, DM, 2006
)
0.33
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Further study is needed to determine whether these results concerning mechanism and dosage can be the basis for prevention of the development of CIS in at risk populations."( Prevention of the phencyclidine-induced impairment in novel object recognition in female rats by co-administration of lurasidone or tandospirone, a 5-HT(1A) partial agonist.
Adelekun, AE; Hannaway, KE; Horiguchi, M; Jayathilake, K; Meltzer, HY, 2012
)
0.38
" The starting dosage of 20 mg of pimavanserin or placebo could be adjusted to 34 mg or 10 mg within the first 8 weeks of the study, after which dosage remained stable until the end of the study."( Pimavanserin for negative symptoms of schizophrenia: results from the ADVANCE phase 2 randomised, placebo-controlled trial in North America and Europe.
Abbs, B; Arango, C; Bugarski-Kirola, D; Fava, M; Liu, IY; Nasrallah, H; Stankovic, S, 2022
)
2.45
" However, given the small effect size, further investigation with optimised dosing is warranted to determine the clinical significance of this effect."( Pimavanserin for negative symptoms of schizophrenia: results from the ADVANCE phase 2 randomised, placebo-controlled trial in North America and Europe.
Abbs, B; Arango, C; Bugarski-Kirola, D; Fava, M; Liu, IY; Nasrallah, H; Stankovic, S, 2022
)
2.16
", dysphagia) occur in up to 40% of the adult general population, particularly among the elderly prescribed solid oral dosage forms."( In Vitro Stability and Recovery Studies of Pimavanserin in Water and in Different Vehicles Orally Administered.
Adegbenle, YH; Bokser, AD; Norton, JC; Stoisavljevic, V, 2022
)
0.98
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antipsychotic agentAntipsychotic drugs are agents that control agitated psychotic behaviour, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect.
5-hydroxytryptamine 2A receptor inverse agonistAn inverse agonist that binds to the same receptor as a 5-hydroxytryptamine 2A receptor agonist, but which induces a pharmacological response opposite to that agonist.
serotonergic antagonistDrugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
ureas
piperidines
monofluorobenzenesAny member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency37.90830.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency5.35470.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency37.90830.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency37.90830.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)52.00000.00011.774010.0000AID1879795
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)100.00000.00011.753610.0000AID1879798
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)100.00000.00002.015110.0000AID1879760
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)100.00000.00002.800510.0000AID1879796
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.03350.00010.88018.8500AID1380714; AID1654710; AID1800764; AID1879757; AID1879782
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.00090.00000.385510.0000AID1800763; AID1855112
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.04640.00011.03029.0000AID1800764
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.00120.00010.954910.0000AID1800763; AID1855113
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)49.80000.00002.398310.0000AID1879797
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.04640.00011.18738.9125AID1800764
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)0.41000.00091.901410.0000AID1879765
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2AHomo sapiens (human)Kb0.00060.00060.16891.1000AID1380714
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (181)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (72)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (42)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (65)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1879817Drug distribution in Sprague-Dawley rat brain at 6 micromol/kg administered via gavage measured after 2 hrs by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879795Inhibition of CYP1A2 (unknown origin)2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879775Drug metabolism in rat assessed as AUC(0 to 24 hrs) for AC- 423 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1823828Antagonist activity at human 5-HT2A receptor expressed in human recombinant CHO-K1 cells co-expressing G protein alpha16 incubated for 1 hr by cellular aequorin-based functional assay
AID1823849Antipsychotic activity in ip dosed Wistar rat assessed as induction of MK801-induced hyperlocomotor activity by measuring minimum effective dose measured for 15 mins
AID1879768AUC(0 to 24 hrs) in monkey at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879778Drug metabolism in mouse assessed as AUC(0 to 24 hrs) for AC- 527 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1654750Drug level in ICR mouse brain at 10 mg/kg, iv measured after 0.5 hrs by LC-MS/MS analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT
AID1380714Antagonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 30 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminesc
AID1879785Metabolic stability in Sprague-Dawley rat liver microsomes assessed as intrinsic clearance at 100 uM preincubated for 10 mins followed by NADPH addition by LC/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879777Drug metabolism in human assessed as AUC(0 to 24 hrs) for AC- 423 metabolite at 80 mg/kg/day by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1654710Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT
AID1879786Metabolic stability in human liver microsomes assessed as intrinsic clearance at 100 uM preincubated for 10 mins followed by NADPH addition by LC/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879793Kinetic solubility of compound2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879797Inhibition of CYP2C19 (unknown origin)2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879794Metabolic stability in dog liver microsomes assessed as compound remaining at 100 uM preincubated for 60 mins followed by NADPH addition by LC/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879759Plasma protein binding in human at 10 uM2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879816Drug distribution in Sprague-Dawley rat brain at 6 micromol/kg administered via gavage measured after 0.5 hr by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879767AUC(0 to 24 hrs) in rat at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879780Drug metabolism in monkey assessed as AUC(0 to 24 hrs) for AC- 527 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879772Drug metabolism in monkey assessed as AUC(0 to 24 hrs) for AC-279 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1855112Inverse agonist activity at 5-HT2A receptor (unknown origin)2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1879792Aqueous solubility of compound at pH 7.42022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1654749Plasma concentration in ICR mouse at 10 mg/kg, iv measured after 0.5 hrs by LC-MS/MS analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT
AID1879781Drug metabolism in human assessed as AUC(0 to 24 hrs) for AC- 527 metabolite at 80 mg/kg/day by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879757Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879784Metabolic stability in human liver microsomes assessed as half life at 100 uM preincubated for 10 mins followed by NADPH addition by LC/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879769AUC(0 to 24 hrs) in human at 80 mg/kg/day by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879761Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 100 uM preincubated for 60 mins followed by NADPH addition by LC/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879782Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1823851Sedative activity in ip dosed Wistar rat assessed as effect on spontaneous locomotor activity measured for 10 mins by social interaction test
AID1879796Inhibition of CYP2C9 (unknown origin)2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879758Plasma protein binding in monkey at 10 uM2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879776Drug metabolism in monkey assessed as AUC(0 to 24 hrs) for AC- 423 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879820Antiparkinson's activity in rat assessed as reduction of DOI-induced head-twitching at 6 micromol/kg, IG measured after 1 hr2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879787Metabolic stability in human liver microsomes assessed as compound remaining at 100 uM preincubated for 60 mins followed by NADPH addition by LC/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1380711Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay relative to alpha-methylserotonin
AID1879818Drug distribution in Sprague-Dawley rat brain at 6 micromol/kg administered via gavage measured after 6 hrs by LC-MS/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879771Drug metabolism in rat assessed as AUC(0 to 24 hrs) for AC-279 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879764Plasma protein binding in rat at 10 uM2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879765Inhibition of hERG potassium channel expressed in CHO cells at -80 mV holding potential by whole cell patch clamp assay2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1855113Inverse agonist activity at 5-HT2C receptor (unknown origin)2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1690398Antagonist activity at recombinant human Ga16-coupled 5HT2A receptor expressed in CHO-K1 cells assessed as inhibition of alpha-methylserotonin-induced calcium mobilization preincubated for 15 to 30 mins followed by alpha-methylserotonin addition and measu2020European journal of medicinal chemistry, Apr-01, Volume: 191Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).
AID1879770Drug metabolism in mouse assessed as AUC(0 to 24 hrs) for AC-279 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879779Drug metabolism in rat assessed as AUC(0 to 24 hrs) for AC- 527 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879766AUC(0 to 24 hrs) in mouse at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879773Drug metabolism in human assessed as AUC(0 to 24 hrs) for AC-279 metabolite at 80 mg/kg/day by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879783Metabolic stability in Sprague-Dawley rat liver microsomes assessed as half life at 100 uM preincubated for 10 mins followed by NADPH addition by LC/MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879760Inhibition of CYP2D6 (unknown origin)2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1654709Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux at 1 uM preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT
AID1879763Dissociation constant, pKa of the compound2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1654751Ratio of drug level in brain to plasma of ICR mouse at 10 mg/kg, iv measured after 0.5 hrs by LC-MS/MS analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT
AID1380713Antagonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin-induced calcium mobilization preincubated for 30 mins followed by serotonin challenge measured for 30 secs by aequorin-derived
AID1879791Lipophilicity, logD of the compound at pH 7.42022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879798Inhibition of CYP3A4 (unknown origin)2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1879774Drug metabolism in mouse assessed as AUC(0 to 24 hrs) for AC- 423 metabolite at 100 mg/kg by UHPLC/FT-ICR-MS analysis2022European journal of medicinal chemistry, Apr-15, Volume: 234Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
AID1800763Radioligand Binding Assay from Article 10.1124/jpet.105.097006: \\Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-102006The Journal of pharmacology and experimental therapeutics, May, Volume: 317, Issue:2
Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.
AID1800764Receptor Selection and Amplification Technology from Article 10.1124/jpet.105.097006: \\Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybuta2006The Journal of pharmacology and experimental therapeutics, May, Volume: 317, Issue:2
Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2007The Journal of pharmacology and experimental therapeutics, Aug, Volume: 322, Issue:2
ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental models.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2004The Journal of pharmacology and experimental therapeutics, Sep, Volume: 310, Issue:3
Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (149)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (6.71)29.6817
2010's79 (53.02)24.3611
2020's60 (40.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 75.14

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index75.14 (24.57)
Research Supply Index5.21 (2.92)
Research Growth Index5.51 (4.65)
Search Engine Demand Index128.22 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (75.14)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials23 (14.47%)5.53%
Reviews38 (23.90%)6.00%
Case Studies5 (3.14%)4.05%
Observational1 (0.63%)0.25%
Other92 (57.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (40)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A 52-Week Open-label Extension Study of Pimavanserin in Adult and Elderly Subjects With Neuropsychiatric Symptoms Related to Neurodegenerative Disease [NCT03623321]Phase 3597 participants (Actual)Interventional2018-07-17Active, not recruiting
A 52-Week Open-Label Extension Study of Pimavanserin in Children and Adolescents With Irritability Associated With Autism Spectrum Disorder (ASD) [NCT05555615]Phase 2/Phase 3228 participants (Anticipated)Interventional2022-11-02Recruiting
A Pilot Randomized, Double-blind, Placebo-controlled Study to Evaluate Safety and Daytime Sedation in Subjects With Parkinson's Disease With Neuropsychiatric Symptoms Treated With Pimavanserin or Low-Dose Quetiapine [NCT04164758]Phase 211 participants (Actual)Interventional2019-10-23Terminated(stopped due to Study enrollment impacted by COVID-19 pandemic and Sponsor terminated for business reasons)
A Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled, Study to Evaluate the Efficacy and Safety of Adjunctive Pimavanserin in Major Depressive Disorder [NCT03018340]Phase 2207 participants (Actual)Interventional2016-12-31Completed
A Double-Blind, Placebo-Controlled Study to Examine the Safety and Efficacy of Pimavanserin for the Treatment of Agitation and Aggression in Alzheimer's Disease [NCT02992132]Phase 2111 participants (Actual)Interventional2016-11-30Terminated
A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Adjunctive Pimavanserin for the Treatment of Schizophrenia [NCT02970292]Phase 3396 participants (Actual)Interventional2016-10-26Completed
An Open-label, 8-Week Study of Safety and Efficacy of Pimavanserin Treatment in Adults With Parkinson's Disease and Depression [NCT03482882]Phase 247 participants (Actual)Interventional2018-03-09Completed
A Double-blind, Placebo-controlled, Relapse Prevention Study of Pimavanserin for the Treatment of Hallucinations and Delusions Associated With Dementia-related Psychosis [NCT03325556]Phase 3392 participants (Actual)Interventional2017-09-27Completed
A 52-Week Open-Label Extension Study of Pimavanserin for the Treatment of Agitation and Aggression in Subjects With Alzheimer's Disease [NCT03118947]Phase 279 participants (Actual)Interventional2017-02-23Completed
Does Pimavanserin (Nuplazid) Improve Sleep in Patients With Parkinson Disease Psychosis? A Pilot Study [NCT05796167]Early Phase 110 participants (Anticipated)Interventional2024-01-09Not yet recruiting
A Phase 2, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Pimavanserin as Adjunctive Treatment for the Negative Symptoms of Schizophrenia [NCT02970305]Phase 2403 participants (Actual)Interventional2016-11-04Completed
[NCT00658567]Phase 3123 participants (Actual)Interventional2008-03-31Completed
Open-label Pimavanserin 34mg at Bedtime for 6 Weeks for Insomnia in Veterans With Post-traumatic Stress Disorder: Proof of Concept Study [NCT04809116]Phase 40 participants (Actual)Interventional2022-12-15Withdrawn(stopped due to Received alternative sources of funding.)
A 52-Week Open-Label Extension Study of Pimavanserin in Subjects With Major Depressive Disorder and Inadequate Response to Antidepressant Treatment [NCT04000009]Phase 3235 participants (Actual)Interventional2019-06-06Terminated(stopped due to The study was terminated for business reasons and not due to safety concerns.)
Study of Pimavanserin Efficacy for the Treatment of Impulse Control Disorders in Parkinson's Disease [NCT03947216]Phase 2130 participants (Anticipated)Interventional2020-10-23Recruiting
Characterization of the Serotonin 2A Receptor Selective PET Tracer [18F]MH.MZ in Patients With Neurodegenerative Diseases [NCT05357612]Phase 475 participants (Anticipated)Interventional2023-01-23Recruiting
A Multi-Center, Open-Label Extension Study to Examine the Safety and Tolerability of ACP-103 in the Treatment of Psychosis in Parkinson's Disease [NCT00550238]Phase 3459 participants (Actual)Interventional2007-07-31Completed
Expanded Access Program of Pimavanserin in Patients With Parkinson's Disease Psychosis [NCT02762591]0 participants Expanded AccessApproved for marketing
Identification of a Serotonin 2A Receptor Subtype of Schizophrenia Spectrum Disorders With Pimavanserin: The Sub-Sero Proof-of-principle Study [NCT03994965]Phase 20 participants (Actual)Interventional2020-01-31Withdrawn(stopped due to Drug supply withdrawn)
Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of Adjunctive Pimavanserin in Subjects With Major Depressive Disorder and Inadequate Response to Antidepressant Treatment (ACP-103-054/059) [NCT03968159]Phase 3298 participants (Actual)Interventional2019-04-25Completed
A Multi-Center, Placebo-Controlled, Double-Blind Trial to Examine the Safety and Efficacy of ACP-103 in the Treatment of Psychosis in Parkinson's Disease [NCT00477672]Phase 3298 participants (Actual)Interventional2007-06-30Completed
A Multi-Center, Placebo-Controlled, Double-Blind Trial to Examine the Safety and Efficacy of Pimavanserin in the Treatment of Psychosis in Parkinson's Disease [NCT01174004]Phase 3199 participants (Actual)Interventional2010-07-31Completed
Effect of Pimavanserin on Aggression and Social Cognition. [NCT05895513]Phase 235 participants (Anticipated)Interventional2024-01-31Not yet recruiting
A 52-Week, Open-Label, Extension Study of Pimavanserin for the Adjunctive Treatment of Schizophrenia [NCT03121586]Phase 3500 participants (Anticipated)Interventional2017-01-31Recruiting
5HT2A/C Serotonin Blockade in Parkinson's Disease [NCT00086294]Phase 240 participants Interventional2004-06-25Completed
[NCT00087542]Phase 260 participants Interventional2004-03-31Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Pimavanserin as Adjunctive Treatment for the Negative Symptoms of Schizophrenia [NCT04531982]Phase 3454 participants (Actual)Interventional2020-08-05Active, not recruiting
A Multi-Center, Placebo-Controlled, Double-Blind Trial to Examine the Safety and Efficacy of Pimavanserin in the Treatment of Psychosis in Parkinson's Disease [NCT06068465]Phase 3248 participants (Anticipated)Interventional2023-09-27Recruiting
An Open-Label Safety Study of Pimavanserin in Parkinson's Disease Patients [NCT01518309]Phase 239 participants (Actual)Interventional2004-11-17Completed
A Single Center, Double-Blind, Placebo-Controlled Study to Examine the Safety and Efficacy of Pimavanserin for the Treatment of Psychosis in Alzheimer's Disease [NCT02035553]Phase 2181 participants (Actual)Interventional2013-11-30Completed
Pilot Feasibility Study of Pimavanserin for Insomnia in Veterans With Posttraumatic Stress Disorder [NCT04188392]Phase 46 participants (Actual)Interventional2020-01-06Completed
CSP #2015 - Multicenter, Randomized, Double-blind Comparator Study of Antipsychotics Pimavanserin and Quetiapine for Parkinson''s Disease Psychosis (C-SAPP) [NCT04373317]Phase 4358 participants (Anticipated)Interventional2022-10-24Recruiting
A Randomized, Double Blind, Multi-Center Study to Assess the Antipsychotic and Motor Effects of ACP-103 When Administered in Combination With Haloperidol or Risperidone to Schizophrenic Subjects [NCT00361166]Phase 2400 participants Interventional2005-08-31Completed
A Pragmatic Randomized Trial Comparing Antipsychotics in Lewy Body Disease [NCT05590637]Phase 494 participants (Anticipated)Interventional2022-04-22Recruiting
A 16-Week Open-Label Study of the Effects of Treatment With Pimavanserin on Activities of Daily Living in Subjects With Parkinson's Disease Psychosis [NCT04292223]Phase 429 participants (Actual)Interventional2020-02-10Completed
A Phase 2, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Efficacy and Safety of Pimavanserin for the Treatment of Irritability Associated With Autism Spectrum Disorder [NCT05523895]Phase 2/Phase 3228 participants (Anticipated)Interventional2022-08-09Recruiting
Pimavanserin for Insomnia in Veterans With Post-traumatic Stress Disorder [NCT05441280]Phase 260 participants (Anticipated)Interventional2023-06-26Recruiting
A Phase 3b, Multicenter, Randomized, Double-blind, Placebo-controlled, Safety Study of Pimavanserin Therapy in Adult and Elderly Subjects Experiencing Neuropsychiatric Symptoms Related to Neurodegenerative Disease [NCT03575052]Phase 3784 participants (Actual)Interventional2018-05-21Completed
An Open Label, Proof-of-Principle, Pilot Study to Evaluate Pimavanserin for the Treatment of Motor and Behavioral Symptoms of Tourette Syndrome [NCT04794413]Early Phase 110 participants (Actual)Interventional2018-11-12Completed
A Target Engagement Study of Pimavanserin for Behavioral Inflexibility With Open Label Trial for Rigid Rigid-compulsive Behavior in Adolescents and Adults With Autism [NCT05999240]Phase 230 participants (Anticipated)Interventional2023-12-01Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00477672 (2) [back to overview]Antipsychotic Efficacy
NCT00477672 (2) [back to overview]Motor Symptoms Change From Baseline (Negative = Improvement)
NCT00550238 (1) [back to overview]Safety: Number (%) of Patients With Drug-related Treatment-emergent Adverse Events (AEs)
NCT00658567 (2) [back to overview]Antipsychotic Efficacy
NCT00658567 (2) [back to overview]Motor Symptoms Change From Baseline (Negative = Improvement)
NCT01174004 (2) [back to overview]Motor Symptoms Change From Baseline (Negative = Improvement)
NCT01174004 (2) [back to overview]Antipsychotic Efficacy
NCT01518309 (1) [back to overview]Number (%) of Patients With Drug-related Treatment-emergent Adverse Events (AEs)
NCT02035553 (1) [back to overview]Antipsychotic Efficacy
NCT02970292 (9) [back to overview]Change From Baseline to Week 6 in the Positive and Negative Syndrome Scale (PANSS) Total Score
NCT02970292 (9) [back to overview]Clinical Global Impression-Improvement (CGI-I) Response
NCT02970292 (9) [back to overview]Drug Attitude Inventory (DAI-10)
NCT02970292 (9) [back to overview]PANSS Responders
NCT02970292 (9) [back to overview]Change From Baseline to Week 6 in Karolinska Sleepiness Scale (KSS) Score
NCT02970292 (9) [back to overview]Clinical Global Impression-Improvement (CGI-I) Score at Week 6
NCT02970292 (9) [back to overview]Change From Baseline (CFBL) to Week 6 in PANSS Subscale Scores, i.e. PANSS Positive Subscale Score, PANSS Negative Subscale Score and PANSS General Psychopathological Scale Score
NCT02970292 (9) [back to overview]Change From Baseline to Week 6 in the Clinical Global Impression-Severity (CGI-S) Score
NCT02970292 (9) [back to overview]Change From Baseline to Week 6 in Personal and Social Performance (PSP) Scale Score
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in the Negative Symptom Assessment-16 (NSA-16) Total Score
NCT02970305 (13) [back to overview]Change From Baseline (CFB) to Week 26 in NSA-16 Domain Scores
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in the Clinical Global Impression of Schizophrenia Scale-Severity (CGI-SCH-S) of Negative Symptoms Score
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in NSA-16 Global Negative Symptoms Rating
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in Karolinska Sleepiness Scale (KSS) Score
NCT02970305 (13) [back to overview]Proportion of Negative Symptom Assessment-16 (NSA-16) Responders at Week 26
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in the Personal and Social Performance Scale (PSP) Score
NCT02970305 (13) [back to overview]Proportion of CGI-SCH-I Responders (CGI-SCH-I Score of 1 or 2) at Week 26; Observed Cases
NCT02970305 (13) [back to overview]Clinical Global Impression of Schizophrenia Scale-Improvement (CGI-SCH-I) of Negative Symptoms Score at Week 26
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in the Positive and Negative Syndrome Scale (PANSS) Total Score
NCT02970305 (13) [back to overview]Change From Baseline (CFB) to Week 26 in PANSS Subscale Scores
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in 10-item Drug Attitude Inventory (DAI-10) Score
NCT02970305 (13) [back to overview]Change From Baseline to Week 26 in Brief Assessment of Cognition in Schizophrenia (BACS) Composite Score
NCT02992132 (2) [back to overview]Cohen-Mansfield Agitation Inventory (CMAI)
NCT02992132 (2) [back to overview]Zarit Burden Interview
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in SIS Score
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in the SDS Total Score
NCT03018340 (11) [back to overview]Treatment Response and Remission Rates at the End of 5-week Treatment Period
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in the HAMD-17 Total Score
NCT03018340 (11) [back to overview]CGI-I Score at Week 5
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in BIS-11 Score
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in CGI-S Total Score
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in DAI-10 Score
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in KSS Score
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in MGH-SFI Score
NCT03018340 (11) [back to overview]Change From Baseline to Week 5 in SF-12 Score
NCT03118947 (1) [back to overview]Treatment Emergent Adverse Events (TEAEs)
NCT03325556 (2) [back to overview]Time From Randomization to Relapse in the Double-blind (DB) Period
NCT03325556 (2) [back to overview]Time From Randomization to Discontinuation From the DB Period for Any Reason
NCT03482882 (8) [back to overview]Change From Baseline (CFB) in Clinical Global Impression-Severity (CGI-S)
NCT03482882 (8) [back to overview]Change From Baseline (CFB) in Scale of Outcomes in PD-Sleep Scale (SCOPA) Nighttime Sleep (NS)Score
NCT03482882 (8) [back to overview]The Number (or Percentage) of Responders
NCT03482882 (8) [back to overview]Clinical Global Impression-Improvement (CGI-I)
NCT03482882 (8) [back to overview]Change From Baseline to Week 8 in HAMD-17 (Hamilton Depression Scale -17 Items) Total Score
NCT03482882 (8) [back to overview]Change From Baseline in EuroQol-5 Dimensions-5 Levels (EQ-5D-5L)
NCT03482882 (8) [back to overview]Change From Baseline (CFB) in SCOPA Daytime Sleepiness (DS) Score
NCT03482882 (8) [back to overview]Change From Baseline (CFB) in HAMD-17 Total Score at Weeks 2, 4, and 6
NCT03968159 (10) [back to overview]Change From Baseline to Week 1 in the HAMD-17 Total Score
NCT03968159 (10) [back to overview]Change From Baseline to Week 5 in Clinical Global Impression-Severity (CGI-S) Score for Depressive Symptoms
NCT03968159 (10) [back to overview]Change From Baseline to Week 5 in Karolinska Sleepiness Scale (KSS) Score
NCT03968159 (10) [back to overview]Change From Baseline to Week 5 in Sheehan Disability Scale (SDS) Score
NCT03968159 (10) [back to overview]Change From Baseline to Week 5 in the Barratt Impulsiveness Scale (BIS-11)
NCT03968159 (10) [back to overview]Change From Baseline to Week 5 in the Changes in Sexual Functioning Questionnaire Short Form
NCT03968159 (10) [back to overview]Change From Baseline to Week 5 in the Hamilton Depression (HAMD) Anxiety/Somatization Factor Score
NCT03968159 (10) [back to overview]Clinical Global Impression-Improvement (CGI-I) Score for Depressive Symptoms at Week 5
NCT03968159 (10) [back to overview]Treatment Responder and Treatment Remission Rates at Week 5
NCT03968159 (10) [back to overview]Change From Baseline to Week 5 in Hamilton Depression Scale (17 Items) (HAMD-17) Total Score
NCT04000009 (1) [back to overview]Treatment-emergent Adverse Events (TEAEs)
NCT04164758 (1) [back to overview]Treatment-emergent Adverse Events (TEAEs)
NCT04188392 (5) [back to overview]Discontinuation Rates Due to Adverse Effects
NCT04188392 (5) [back to overview]Mean Change in Duration of Stage N3 Sleep Pre- and Post-treatment
NCT04188392 (5) [back to overview]Recruitment Rates
NCT04188392 (5) [back to overview]Retention Rates
NCT04188392 (5) [back to overview]Completion Rates of Key Outcome Measures

Antipsychotic Efficacy

"Antipsychotic Efficacy was defined as a decrease in the severity and/or frequency of hallucinations and/or delusions. This is measured as the change from baseline (Day 1) to Day 42 in the Scale for the Assessment of Positive Symptoms - Hallucinations and Delusions scales (SAPS-H+D) score for the ITT Analysis Set. The possible total score is 0 to 100 and a negative change in score indicates improvement.~Analysis Method: Analysis of Covariance (ANCOVA) and missing data was imputed using Last Observation Carried Forward (LOCF) method." (NCT00477672)
Timeframe: Each study visit (i.e. Days 1, 8, 15, 29 and 42)

,,
InterventionScore on the SAPS H+D scale (Least Squares Mean)
Change from BaselineDifference of Least Squares Mean versus Placebo
Pimavanserin 10 mg-5.80.1
Pimavanserin 40 mg-6.7-0.8
Placebo-5.9NA

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Motor Symptoms Change From Baseline (Negative = Improvement)

"Motor symptoms were measured using the change from baseline (Day 1) to Day 42 in the combined score of the Unified Parkinson's Disease Rating Scale (UPDRS) Part II (Activities of Daily Living) and Part III (Motor Examination) using the per-protocol (PP) analysis set. The possible total score is 0 to 160 and a negative change in score indicates improvement.~Analysis Method: ANCOVA, and missing data was imputed using LOCF. The UPDRS Parts II+III score was analyzed by constructing 2-sided 95% confidence intervals (CIs) on the difference between each pimavanserin dose group and placebo mean change from baseline. Non-inferiority was concluded if the upper limit of the CI was less than or equal to 5." (NCT00477672)
Timeframe: Each study visit (i.e. Days 1, 8, 15, 29 and 42)

,,
InterventionScore on UPDRS-II+III (Least Squares Mean)
Change from BaselineDifference of Least Square Mean versus Placebo
Pimavanserin 10 mg-1.411.53
Pimavanserin 40 mg-3.13-0.19
Placebo-2.94NA

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Antipsychotic Efficacy

"Antipsychotic efficacy was defined as a decrease in the severity and/or frequency of hallucinations and/or delusions. This is measured as the change from baseline (Day 1) to Day 42 in the Scale for the Assessment of Positive Symptoms - Hallucinations and Delusions scales (SAPS-H+D) score for the ITT Analysis Set. The possible total score is 1 to 100 and a negative change in score indicates improvement.~Analysis Method: Analysis of Covariance (ANCOVA) and missing data was imputed using Last Observation Carried Forward (LOCF) method." (NCT00658567)
Timeframe: Each study visit (i.e. Days 1, 8, 15, 29 and 42)

,,
InterventionScores on the SAPS H+D scale (Least Squares Mean)
Change from BaselineDifference of Least Squares Mean versus Placebo
Pimavanserin 10 mgNANA
Pimavanserin 20 mg-6.5-2.1
Placebo-4.4NA

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Motor Symptoms Change From Baseline (Negative = Improvement)

"Motor symptoms were measured using the change from baseline (Day 1) to Day 42 in the combined score of the Unified Parkinson's Disease Rating Scale (UPDRS) Part II (Activities of Daily Living) and Part III (Motor Examination). The total possible score is 0 to 160 and a negative change in score indicates improvement.~Analysis Method: ANCOVA, and missing data was imputed using LOCF method. The UPDRS Parts II+III score was analyzed by constructing 2-sided 95% confidence intervals (CIs) on the difference between each pimavanserin dose group and placebo mean change from baseline. Non-inferiority was concluded if the upper limit of the CI was less than or equal to 5." (NCT00658567)
Timeframe: Each study visit (i.e. Days 1, 8, 15, 29 and 42)

,,
InterventionScore on UPDRS-II+III scale. (Least Squares Mean)
Change from BaselineDifference of Least Squares Mean versus Placebo
Pimavanserin 10 mgNANA
Pimavanserin 20 mg-3.9-2.1
Placebo-1.8NA

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Motor Symptoms Change From Baseline (Negative = Improvement)

"Motor symptoms were measured using the change from baseline to Day 43 in the combined score of the Unified Parkinson's Disease Rating Scale (UPDRS) Part II (Activities of Daily Living) and Part III (Motor Examination). The possible total score is 0 to 160 and a negative change in score indicates improvement.~Analysis Method: Analysis of Covariance (ANCOVA). The UPDRS Parts II+III score was analyzed by constructing 2-sided 95% confidence intervals (CIs) on the difference between the pimavanserin dose group and placebo mean change from baseline. Non-inferiority was concluded if the upper limit of the CI was less than or equal to 5." (NCT01174004)
Timeframe: Study Days 1 and 43

,
InterventionScore on the UPDRS-II+III (Least Squares Mean)
Change from BaselineDifference of Least Squares Mean versus Placebo
Pimavanserin 40 mg-1.400.29
Placebo-1.69NA

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Antipsychotic Efficacy

"Antipsychotic Efficacy was defined as a decrease in the severity and/or frequency of hallucinations and/or delusions. This is measured as the change from baseline (Day 1) to Day 43 in the Scale for the Assessment of Positive Symptoms 9-item sum score for Parkinson's Disease (SAPS-PD). The possible total score is 0 to 45 and a negative change in score indicates improvement.~Analysis Method: Mixed Model Repeated Measures (MMRM)" (NCT01174004)
Timeframe: Each study visit (i.e. Days 1, 15, 29 and 43)

,
InterventionScore on the SAPS-PD scale (Least Squares Mean)
Change from BaselineDifference of Least Squares Mean versus Placebo
Pimavanserin 40 mg-5.79-3.06
Placebo-2.73NA

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Antipsychotic Efficacy

Change from Baseline to Day 43 in the Neuropsychiatric Inventory-Nursing Home Version (NPI-NH) psychosis score (Delusions [Domain A]+Hallucinations [Domain B]) in the Full Analysis Set (FAS). The NPI-NH is a questionnaire that quantifies behavioral changes in dementia in nursing home patients and evaluates 12 behavioral domains. For each of the 12 behavioral domains the Frequency (scale:1=occasionally to 4=very frequently) is multiplied by the Severity (scale:1=Mild to 3=Severe) to obtain a domain score (frequency x severity), The NPI-NH Psychosis Subscale consists of the two domains of Delusions and Hallucinations, calculated by adding the Individual domain scores, to yield a possible total score of 0 to 24. Lower scores correspond to less severity. A negative change score from baseline indicates improvement. (NCT02035553)
Timeframe: Day 43

InterventionScore on the NPI-NH scale (Least Squares Mean)
Placebo-1.93
Pimavanserin 40 mg-3.76

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Change From Baseline to Week 6 in the Positive and Negative Syndrome Scale (PANSS) Total Score

The PANSS is a 30-item scale used to evaluate the presence, absence, and severity of schizophrenia symptoms. The 30 items are arranged as 7 positive symptom items (P1 to P7), 7 negative symptom items (N1 to N7), and 16 general psychopathology symptom items (G1 to G16). Items are scored over the past week (7 days) on a 7-point scale ranging from 1 (absent) to 7 (extreme). The PANSS total score can range from a minimum of 30 to a maximum of 210, where a higher score signifies greater severity of schizophrenia symptoms. (NCT02970292)
Timeframe: From baseline to Week 6

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 6
Pimavanserin88.3-15.3
Placebo88.1-13.4

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Clinical Global Impression-Improvement (CGI-I) Response

"The CGI-I is a 1-item scale, used to rate the improvement from 1 (very much improved) to 7 (very much worse). Higher scores denote less improvement.~A CGI-I score of 1 or 2 was counted as response. The Analysis was performed twice; once including missing values as non-responders (MN) and once including only observed cases (OC)." (NCT02970292)
Timeframe: From baseline to Week 6

,
InterventionParticipants (Count of Participants)
CGI-I response (MN)CGI-I response (OC)
Pimavanserin6868
Placebo6565

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Drug Attitude Inventory (DAI-10)

"The DAI-10 contains 6 items (1, 3, 4, 7, 9, and 10) that a patient who is fully adherent to study medication would answer as True and 4 items (2, 5, 6, and 8) that a patient who is fully adherent to study medication would answer as False. A correct answer is scored +1 and an incorrect answer is scored -1; the total score is derived as overall sum. The score can range from -10 to 10. Positive total scores indicate adherence and negative total scores indicate non-adherence. Higher scores denote better adherence." (NCT02970292)
Timeframe: From baseline to Week 6

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 6
Pimavanserin5.60.4
Placebo5.80.4

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PANSS Responders

Porportion of patients showing a PANSS response of >=20% or >=30% reduction in PANSS total score PANSS total score reduction signifies improvement. (NCT02970292)
Timeframe: From baseline to Week 6

,
InterventionParticipants (Count of Participants)
PANSS total score reduction >=20%PANSS total score reduction >=30%
Pimavanserin10971
Placebo9967

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Change From Baseline to Week 6 in Karolinska Sleepiness Scale (KSS) Score

The KSS is a self-reported measure of a patient's level of drowsiness. In this study, drowsiness was to be rated during the last week (7 days). Scoring is based on a 9-point verbally anchored scale ranging from 1 (extremely alert) to 9 (very sleepy, great effort to keep awake, fighting sleep). The maximum score is 9. Higher scores denote more drowsiness. (NCT02970292)
Timeframe: From baseline to Week 6

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 6
Pimavanserin4.6-0.5
Placebo4.7-0.2

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Clinical Global Impression-Improvement (CGI-I) Score at Week 6

The CGI-I is a 1-item scale, used to rate the improvement from 1 (very much improved) to 7 (very much worse). Higher scores denote less improvement. (NCT02970292)
Timeframe: From baseline to Week 6

Interventionscore on a scale (Mean)
Pimavanserin2.8
Placebo3.0

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Change From Baseline (CFBL) to Week 6 in PANSS Subscale Scores, i.e. PANSS Positive Subscale Score, PANSS Negative Subscale Score and PANSS General Psychopathological Scale Score

"The PANSS is a 30-item scale used to evaluate the presence, absence, and severity of schizophrenia symptoms. The 30 items are arranged as 7 positive symptom items (P1 to P7), 7 negative symptom items (N1 to N7), and 16 general psychopathology symptom items (G1 to G16). Items are scored over the past week (7 days) on a 7-point scale ranging from 1 (absent) to 7 (extreme).~The PANSS positive subscale score can range from 7 to 49; the PANSS negative subscale score can range from 7 to 49; the PANSS general psychopathology scale score can range from 16 to 112.~For each of the subscale scores, a higher score signifies greater severity of schizophrenia symptoms." (NCT02970292)
Timeframe: From baseline to Week 6

,
Interventionscore on a scale (Mean)
PANSS positive scale BLPANSS positive scale CFBL to 6 weeksPANSS negative scale BLPANSS negative scale CFBL to 6 weeksPANSS general psychopatholigy scale BLPANSS gen. psychopath. scale CFBL to 6 w
Pimavanserin23.0-5.423.0-2.842.4-7.2
Placebo22.8-4.923.1-2.142.2-6.4

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Change From Baseline to Week 6 in the Clinical Global Impression-Severity (CGI-S) Score

The CGI-S is a 1-item scale, used to rate the severity of the disorder from 0 (not assessed) to 7 (among the most extremely ill patients). A higher CGI-S score denotes greater severity of the disorder. (NCT02970292)
Timeframe: From baseline to Week 6

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 6
Pimavanserin4.6-0.8
Placebo4.6-0.7

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Change From Baseline to Week 6 in Personal and Social Performance (PSP) Scale Score

The PSP is a validated 100-point (1 to100) single-item rating scale to assess the psychosocial functioning of patients with schizophrenia. The maximum score is 100. Higher scores denote better psychosocial functioning. (NCT02970292)
Timeframe: From baseline to Week 6

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 6
Pimavanserin51.86.8
Placebo51.65.7

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Change From Baseline to Week 26 in the Negative Symptom Assessment-16 (NSA-16) Total Score

The NSA-16 is a semi-structured interview and a validated scale containing 16 items for evaluating negative symptoms of schizophrenia, i.e. the reduction or absence of emotional expression and volitional behaviors normally present in a healthy person. Items are scored based on behaviors during the interview (items 1-4, 6, 7, 9, 11, 15, 16) or previous 7 days (items 5, 8, 10, 12-14) on a 6-point scale from 1 to 6. The NSA-16 total score is the sum of item scores. It can range from 16 to a maximum of 96, with higher scores denoting more severe negative symptoms in schizophrenia. (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin61.8-10.5
Placebo61.0-8.8

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Change From Baseline (CFB) to Week 26 in NSA-16 Domain Scores

The NSA-16 is a semi-structured interview and a validated scale containing 16 items for evaluating negative symptoms of schizophrenia, i.e. the reduction or absence of emotional expression and volitional behaviors normally present in a healthy person. Items are scored based on behaviors during the interview (items 1-4, 6, 7, 9, 11, 15, 16) or previous 7 days (items 5, 8, 10, 12-14) on a 6-point scale from 1 to 6. The NSA-16 domain scores are the sum of item scores in each domain i.e. communication (min score 4, max score 24), emotion/affect (min 3, max 18), social involvement (min 3, max 18), motivation (min 4, max 24), and retardation (min 2, max 12); with higher scores denoting more severe negative symptoms in schizophrenia. (NCT02970305)
Timeframe: From baseline (BL) to Week 26

,
Interventionscore on a scale (Mean)
Communication, BLCommunication, CFB to Week 26Emotion/affect, BLEmotion/affect, CFB to Week 26Social Involvement, BLSocial Involvement, CFB to Week 26Motivation, BLMotivation, CFB to Week 26Retardation, BLRetardation, CFB to Week 26
Pimavanserin12.3-2.412.7-1.913.1-2.016.7-2.67.0-1.7
Placebo12.3-2.012.5-1.612.6-1.416.6-2.27.0-1.5

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Change From Baseline to Week 26 in the Clinical Global Impression of Schizophrenia Scale-Severity (CGI-SCH-S) of Negative Symptoms Score

The CGI-SCH-S is a clinician-rated, 7-point scale to evaluate positive, negative, depressive, cognitive symptoms and overall severity in schizophrenia. For the purpose of this study, only the negative symptoms were evaluated. The score could range from 1 (normal, not ill) to 7 (among the most severely ill). (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin4.6-0.6
Placebo4.7-0.6

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Change From Baseline to Week 26 in NSA-16 Global Negative Symptoms Rating

The global negative symptoms rating of the NSA-16 assesses overall severity on a 7-point scale from 1 to 7, with higher scores denoting more severe negative symptoms in schizophrenia. (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin4.7-0.7
Placebo4.8-0.7

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Change From Baseline to Week 26 in Karolinska Sleepiness Scale (KSS) Score

The KSS is a self-reported subjective measure of a subject's level of drowsiness. Respondents must choose statements that most accurately describe their level of sleepiness over the past 7 days. Scoring was based on a 9-point verbally anchored scale ranging from 1 (extremely alert) to 9 (very sleepy, great effort to keep awake, fighting sleep). Higher scores denoted more drowsiness. (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin4.6-0.3
Placebo4.8-0.6

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Proportion of Negative Symptom Assessment-16 (NSA-16) Responders at Week 26

"The NSA-16 is a semi-structured interview and a validated scale containing 16 items for evaluating negative symptoms of schizophrenia, i.e. the reduction or absence of emotional expression and volitional behaviors normally present in a healthy person. Items are scored based on behaviors during the interview (items 1-4, 6, 7, 9, 11, 15, 16) or previous 7 days (items 5, 8, 10, 12-14) on a 6-point scale from 1 to 6. The NSA-16 total score is the sum of item scores. It can range from 16 to a maximum of 96, with higher scores denoting more severe negative symptoms in schizophrenia.~NSA-16 responders were defined as patients with at least 20, 30, 50, or 75% percentage improvement in NSA-16 total score from baseline." (NCT02970305)
Timeframe: From baseline to Week 26

,
InterventionParticipants (Count of Participants)
At least 20% improvementAt least 30% improvementAt least 50% improvementAt least 75% improvement
Pimavanserin9356214
Placebo8451162

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Change From Baseline to Week 26 in the Personal and Social Performance Scale (PSP) Score

"The PSP is a validated 100-point (1 to100) single-item rating scale to assess the psychosocial functioning of subjects with schizophrenia. Ratings are based on 4 main areas i.e. (a) socially useful activities, including work and study; (2) personal and social relationships, (3) self-care; and (4) disturbing and aggressive behaviors. The time period assessed is past month. Higher scores denote better psychosocial functioning" (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin47.28.1
Placebo46.78.4

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Proportion of CGI-SCH-I Responders (CGI-SCH-I Score of 1 or 2) at Week 26; Observed Cases

"The CGI-SCH-I is a clinician-rated, 7-point scale that is designed to evaluate change from baseline in positive, negative, depressive, cognitive symptoms and overall severity in schizophrenia. For the purpose of this study, only the changes in negative symptoms from baseline were evaluated. The 7-point scores range from 1 (very much improved) to 7 (very much worse); responders were defined as those with CGI-SCH-I of 1 or 2.~The analysis includes observed cases; missing cases were not imputed." (NCT02970305)
Timeframe: From baseline to Week 26

InterventionParticipants (Count of Participants)
Pimavanserin47
Placebo40

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Clinical Global Impression of Schizophrenia Scale-Improvement (CGI-SCH-I) of Negative Symptoms Score at Week 26

The CGI-SCH-I is a clinician-rated, 7-point scale to evaluate change from baseline in positive, negative, depressive, cognitive symptoms and overall severity in schizophrenia. For the purpose of this study, only the changes in negative symptoms from baseline were evaluated. The score could range from 1 (very much improved) to 7 (very much worse). (NCT02970305)
Timeframe: From baseline to Week 26

Interventionscore on a scale (Mean)
Pimavanserin3.1
Placebo3.1

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Change From Baseline to Week 26 in the Positive and Negative Syndrome Scale (PANSS) Total Score

The PANSS is a 30-item scale to evaluate the presence, absence, and severity of schizophrenia symptoms. Items are scored over the past week (7 days) on a 7-point scale from 1 (absent) to 7 (extreme). The PANSS total score is the sum of scores and ranges from a minimum of 30 to a maximum of 210. Higher scores denote more severe symptoms. (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin77.2-8.7
Placebo79.4-8.6

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Change From Baseline (CFB) to Week 26 in PANSS Subscale Scores

The PANSS is a 30-item scale to evaluate the presence, absence, and severity of schizophrenia symptoms. Items are scored over the past week (7 days) on a 7-point scale from 1 (absent) to 7 (extreme). The PANSS has 3 subscales that are the sums of the respective item scores, including the positive scale (min 7, max 49), negative scale (min 7, max 49), and general psychopathology scale (min 16, max 112). Higher scores denote more severe symptoms. (NCT02970305)
Timeframe: From baseline (BL) to Week 26

,
Interventionscore on a scale (Mean)
Positive subscale, BLPositive subscale, CFB to Week 26Negative subscale, BLNegative subscale, CFB to Week 26General psychopathology subscale, BLGeneral psychopathology subscale, CFB to Week 26
Pimavanserin13.1-0.627.5-4.036.6-4.1
Placebo13.7-0.827.5-3.838.2-4.0

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Change From Baseline to Week 26 in 10-item Drug Attitude Inventory (DAI-10) Score

"The DAI-10 contains 6 items (1, 3, 4, 7, 9, and 10) that a subject who is fully adherent to the prescribed medication would answer as True and 4 items (2, 5, 6, and 8) that a subject who is fully adherent to the prescribed medication would answer as False. A correct answer is scored +1 and an incorrect answer is scored -1. The total score is the sum of pluses and minuses, which can range from -10 to 10 in increments of 2. A positive total score indicates a positive subjective response (adherent) and a negative total score indicates a negative subjective response (non-adherent). Higher scores denote better adherence." (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin5.70.2
Placebo5.70.2

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Change From Baseline to Week 26 in Brief Assessment of Cognition in Schizophrenia (BACS) Composite Score

The BACS is a performance-based assessment of treatment-related changes in cognition, assessing 6 domains of verbal memory and learning; working memory; motor function; verbal fluency; attention and speed of processing; and executive function. The 6 domains with their raw scores are: verbal memory 0-75; digit sequencing 0-28; token motor 0-100; verbal fluency 0-225; symbol coding 0-110; Tower of London 0-22. For each domain, higher scores reflect better cognition. Raw scores are converted to age and sex-corrected normalized scores. The BACS composite score is calculated as the mean of the normalized scores from the 6 subscale scores, standardized so that the mean of the BACS composite score in the healthy normative sample is 50 and the standard deviation is 10. (NCT02970305)
Timeframe: From baseline to Week 26

,
Interventionscore on a scale (Mean)
BaselineChange from baseline to Week 26
Pimavanserin22.943.33
Placebo20.994.16

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Cohen-Mansfield Agitation Inventory (CMAI)

The Cohen-Mansfield Agitation Inventory (CMAI) is a 29-item scale to assess agitation. Each item is rated on a 7-point scale of frequency, from least (1) to most frequent (7). Items are summed to calculate the CMAI total score. The CMAI total score has a range of 29-203 points; higher scores indicate more severe agitation (NCT02992132)
Timeframe: Baseline to 12 weeks

,,
Interventionscore on a scale (Mean)
BaselineWeek 12Week 12 change from baseline
Pimavanserin 20 mg56.952.5-3.7
Pimavanserin 34 mg68.053.7-12.3
Placebo70.354.3-16.8

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Zarit Burden Interview

The Zarit Burden Interview (ZBI) assess the stresses experienced by caregivers of patients with dementia. It assesses 22 questions about the impact of the patient's disabilities on the caregiver's life, each rated from least (0) to most (4) frequent. Items are summed to calculate the ZBI total score. The ZBI total score ranges from 0 to 88; higher scores denoting more stresses experienced by caregivers. (NCT02992132)
Timeframe: Baseline to 12 weeks

,,
Interventionscore on a scale (Mean)
BaselineWeek 12Week 12 change from baseline
Pimavanserin 20 mg40.836.8-4.9
Pimavanserin 34 mg41.735.7-5.5
Placebo41.537.0-6.5

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Change From Baseline to Week 5 in SIS Score

The Sheehan Irritability Scale is a 7-item patient-reported outcome measure to measure the frequency, severity, and impairment associated with irritability in psychiatric patients. It includes items on: irritability, frustration, edginess/ impatience/ overreaction, moodiness, anger with self, anger with others, and temper. Items are answered on an 11-point rating scale where higher scores indicated greater severity (0=not at all, 10=extremely). Item responses are summed into a total score (range=0-70). Higher scores mean higher irritability. (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Baseline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 138.9-19.4
Pimavanserin 34 mg + SSRI/SNRI, Stage 235.2-4.8
Placebo + SSRI/SNRI, Stage 138.8-10.8
Placebo + SSRI/SNRI, Stage 236.6-6.6

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Change From Baseline to Week 5 in the SDS Total Score

The Sheehan Disability Scale is a 3-item patient-facing questionnaire used to evaluate impairments in the domains of work, social life/leisure, and family life/home responsibility. All items are rated on an 11-point scale from 0 (no impairment) to 10 (most severe). The total SDS score ranges from 0 to 10. It is calculated as the arithmetic mean of the scores for all 3 items. A higher score indicates greater disability. (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Basline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 16.365-3.229
Pimavanserin 34 mg + SSRI/SNRI, Stage 25.753-0.890
Placebo + SSRI/SNRI, Stage 16.519-2.026
Placebo + SSRI/SNRI, Stage 25.747-0.507

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Treatment Response and Remission Rates at the End of 5-week Treatment Period

"The Hamilton Rating Scale for Depression (HAMD-17) is a 17-item scale to assess depression. Each item is rated from least (0) to most frequent or most severe, as applicable, with highest scores of 2 to 4 depending on the item. Items are summed up to calculate the HAMD-17 total score. A higher total score indicates more severe depression.~Treatment response was defined as a reduction from Baseline in HAMD-17 total score of >=50%.~Remission was defined as a HAMD-17 total score <=7." (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
InterventionParticipants (Count of Participants)
Treatment responders Week 5Remission rate Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 12712
Pimavanserin 34 mg + SSRI/SNRI, Stage 221
Placebo + SSRI/SNRI, Stage 13817
Placebo + SSRI/SNRI, Stage 221

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Change From Baseline to Week 5 in the HAMD-17 Total Score

The Hamilton Rating Scale for Depression (HAMD-17) is a 17-item scale to assess depression. The HAMD-17 consists of 8 items with a score on a 3 point scale and 9 items with a score on a 5 point scale. Each item is rated from least (0) to most frequent or most severe, as applicable, with highest scores of 2 to 4, depending on the item. Items are summed up to calculate the HAMD-17 total score. The total score ranges from 0 to 52. A higher total score indicates more severe depression. (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Baseline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 122.9-11.9
Pimavanserin 34 mg + SSRI/SNRI, Stage 220.3-2.8
Placebo + SSRI/SNRI, Stage 122.0-7.1
Placebo + SSRI/SNRI, Stage 220.4-3.2

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CGI-I Score at Week 5

The Clinical Global Impression- Improvement scale is a 1-item scale, used to rate the global improvement of the patient since beginning of the study from 0 (not assessed) to 7 (very much worse). A higher CGI-I score denotes less improvement in depression. (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

Interventionscore on a scale (Least Squares Mean)
Pimavanserin 34 mg + SSRI/SNRI, Stage 12.2
Placebo + SSRI/SNRI, Stage 12.8
Pimavanserin 34 mg + SSRI/SNRI, Stage 23.0
Placebo + SSRI/SNRI, Stage 23.1

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Change From Baseline to Week 5 in BIS-11 Score

The Barratt Impulsiveness Scale-11 is a questionnaire for assessment of the personality/behavioral construct of impulsiveness. It is composed of 30 items describing common impulsive or non-impulsive (for reverse scored items) behaviors and preferences. Items are scored on a 4-point scale from Rarely/Never (1) to Almost Always/Always (4). Items are summed up to calculate the total score. The BIS-11 total score ranges from 30 to 120. Higher scores denotes more impulsiveness. (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Baseline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 172.5-4.2
Pimavanserin 34 mg + SSRI/SNRI, Stage 265.9-1.4
Placebo + SSRI/SNRI, Stage 170.0-2.8
Placebo + SSRI/SNRI, Stage 270.31.7

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Change From Baseline to Week 5 in CGI-S Total Score

The Clinical Global Impression-Severity Scale is a 1-item scale, used to rate the severity of the disorder from 0 (not assessed) to 7 (among the most extremely ill patients). A higher CGI-I score denotes more severe depression. (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Baseline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 14.6-2.0
Pimavanserin 34 mg + SSRI/SNRI, Stage 24.1-0.5
Placebo + SSRI/SNRI, Stage 14.4-1.1
Placebo + SSRI/SNRI, Stage 24.1-0.5

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Change From Baseline to Week 5 in DAI-10 Score

"The Drug Attitude Inventory-10 is a 6-item patient-facing questionnaire to evaluate a patient's perceptions and experiences of treatment. It contains 6 items that a patient who is fully adherent to prescribed medication would answer as True, and 4 items that a patient who is fully adherent would rate as False. Scores are allocated to each answer and the total score is calculated as the sum. A correct answer is scored +1 and an incorrect answer is scored -1. The total score ranges from -10 to 10 and is the sum of pluses and minuses. A positive total score indicates a positive subjective response (adherent) and a negative total score indicates a negative subjective response (nonadherent). Higher scores denoted better adherence." (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Baseline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 14.21.4
Pimavanserin 34 mg + SSRI/SNRI, Stage 25.10.6
Placebo + SSRI/SNRI, Stage 14.40.5
Placebo + SSRI/SNRI, Stage 24.80.3

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Change From Baseline to Week 5 in KSS Score

"The Karolinska Sleepiness Scale is a patient-facing 1-item scale that measures the patient's drowsiness. Scoring is based on a 9-point verbally anchored scale ranging from extremely alert (1) to very sleepy, great effort to keep awake, fighting sleep (9). Higher scores denote more drowsiness." (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Baseline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 16.7-1.9
Pimavanserin 34 mg + SSRI/SNRI, Stage 26.7-0.5
Placebo + SSRI/SNRI, Stage 16.6-0.4
Placebo + SSRI/SNRI, Stage 26.1-0.2

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Change From Baseline to Week 5 in MGH-SFI Score

"The Massachusetts General Hospital Sexual Functioning Index is a patient-facing questionnaire that quantifies sexual dysfunction into 5 functional domains (interest in sex, sexual arousal, ability to achieve orgasm, ability to maintain erection [males only], and sexual satisfaction). Patients rate each item using a 6-point scale ranging from 1 (good function) to 6 (poor function). The MGH-SFI score is calculated as the arithmetic mean of the item scores for the 5 domains. The mean MGH-SFI score ranges from a minimum value of 1 to a maximum value of 6. Higher scores denotes worse sexual dysfunction." (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
Baseline (BL)Change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 14.642-0.830
Pimavanserin 34 mg + SSRI/SNRI, Stage 24.678-0.472
Placebo + SSRI/SNRI, Stage 14.457-0.155
Placebo + SSRI/SNRI, Stage 24.264-0.183

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Change From Baseline to Week 5 in SF-12 Score

The 12-Item Short Form Health Survey is a patient-reported outcome measure that addresses 8 domains of physical functioning, role - physical, bodily pain, general health perceptions, vitality, social functioning, role - emotional, and mental health. Composite scores were obtained representing physical health and mental health composite summaries, Physical Component Summary (PCS) and Mental Component Summary (MCS), respectively. An algorithm was used to generate PCS and MCS for comparison to normative data. In normative data, the mean score was set to 50; thus, scores >50 indicate better physical or mental health than the mean and scores <50 indicate worse health. A higher score is indicative of a better health state. (NCT03018340)
Timeframe: Baseline, 5 weeks and 10 weeks during Stage 1 and Stage 2, respectively

,,,
Interventionscore on a scale (Mean)
PCS baseline (BL)PCS change from BL to Week 5MCS baseline (BL)MCS change from BL to Week 5
Pimavanserin 34 mg + SSRI/SNRI, Stage 149.587-0.98123.11316.146
Pimavanserin 34 mg + SSRI/SNRI, Stage 246.945-0.54627.5573.566
Placebo + SSRI/SNRI, Stage 148.783-0.72624.0047.989
Placebo + SSRI/SNRI, Stage 248.9941.81128.5240.578

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Treatment Emergent Adverse Events (TEAEs)

Safety and tolerability of pimavanserin after 52 weeks of treatment in patients with probable Alzheimer's disease who have symptoms of agitation and Aggression, in terms of occurrence of TEAEs (NCT03118947)
Timeframe: 52 weeks

InterventionParticipants (Count of Participants)
All Patients53

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Time From Randomization to Relapse in the Double-blind (DB) Period

"The time from randomization to relapse in the DB period was compared between treatment groups using a Cox regression model. The treatment effect was measured by the hazard ratio (HR).~Relapse was defined as (1) ≥30% increase in SAPS-H+D total score from DB baseline (BL) and CGI-I score ≥6 relative to DB BL, (2) treatment with antipsychotic for dementia-related delusions/hallucinations, (3) treatment/study discontinuation due to lack of efficacy, and/or (4) hospitalization for worsening dementia-related psychosis.~SAPS-H+D is a 20-item scale; the total score is the sum of the 20 item scores (range 0-100); higher scores denote more severe symptoms. CGI-I is a clinician-rated 7-point scale to rate improvement in hallucinations/delusions relative to BL (range 1-7); higher scores denote less improvement or worsening.~A pre-specified IA was conducted after accrual of 40 adjudicated relapse events. The prespecified stopping criterion was met; the study was stopped for efficacy." (NCT03325556)
Timeframe: From randomization in the DB period through 26 weeks

Interventiondays (Median)
Pimavanserin Double-Blind PeriodNA
Placebo Double-Blind PeriodNA

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Time From Randomization to Discontinuation From the DB Period for Any Reason

The endpoint of time from randomization to discontinuation from the DB period for any reason (other than termination of the study by the sponsor) was compared between treatment groups using a Cox regression model. The treatment effect was measured by the HR. (NCT03325556)
Timeframe: From randomization in the DB period through 26 weeks

Interventiondays (Median)
Pimavanserin Double-Blind PeriodNA
Placebo Double-Blind PeriodNA

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Change From Baseline (CFB) in Clinical Global Impression-Severity (CGI-S)

The CGI-S is a clinician-rated 7-point scale to rate the severity of the patient's depression at the time of assessment. The CGI-S ranges from 1 (normal) to 7 (patient is among the most severely ill). (NCT03482882)
Timeframe: From baseline to Week 8

Interventionscore on a scale (Mean)
Baseline CGI-S8 Week CGI-S CFB
Pimavanserin Full Analysis Set4.1-1.8

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Change From Baseline (CFB) in Scale of Outcomes in PD-Sleep Scale (SCOPA) Nighttime Sleep (NS)Score

The SCOPA-NS subscale addresses problems in nighttime sleep and consists of 5 items (sleep initiation, sleep fragmentation, sleep efficiency, sleep duration, early wakening). Each item has 4 response options (ranging from 0=not at all to 3=a lot). The SCOPA-NS score ranges from 0 to 15, with a higher score indicating more severe nighttime sleep problems. (NCT03482882)
Timeframe: From baseline to Week 8

Interventionscore on a scale (Mean)
Baseline SCOPA-NSWeek 8 SCOPA-NS CFB
Pimavanserin Full Analysis Set6.1-2.1

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The Number (or Percentage) of Responders

"The HAMD-17 is a multiple-item questionnaire to assess the severity of depression, including items of mood, feelings of guilt, suicide ideation, insomnia, agitation or retardation, anxiety, weight loss, and somatic symptoms. Each of the 17 items is scored on a 3- or 5-point scale (depending on the item). The minimum total score is 0; the maximum total score is 52. A higher total score signifies more severe Depression.~Response was defined as ≥50% reduction from baseline in HAMD-17 total score. Patients without Week-8 score were counted as nonresponders." (NCT03482882)
Timeframe: From baseline to Week 8

InterventionParticipants (Count of Participants)
Pimavanserin Full Analysis Set27

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Clinical Global Impression-Improvement (CGI-I)

The CGI-I is a clinician-rated 7-point scale to rate the improvement in the patient's depression at the time of assessment relative baseline. The CGI-I ranges from 1 (very much improved) to 7 (very much worse) (NCT03482882)
Timeframe: At Week 8

Interventionscore on a scale (Mean)
Pimavanserin Full Analysis Set2.0

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Change From Baseline to Week 8 in HAMD-17 (Hamilton Depression Scale -17 Items) Total Score

The HAMD-17 is a multiple-item questionnaire to assess the severity of depression, including items of mood, feelings of guilt, suicide ideation, insomnia, agitation or retardation, anxiety, weight loss, and somatic symptoms. Each of the 17 items is scored on a 3- or 5-point scale (depending on the item). The minimum total score is 0; the maximum total score is 52. A higher total score signifies more severe depression. (NCT03482882)
Timeframe: From baseline to Week 8

Interventionscore on a scale (Mean)
Baseline HAMD-17 total scoreWeek 8 HAMD-17 total score
Pimavanserin Full Analysis Set19.28.1

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Change From Baseline in EuroQol-5 Dimensions-5 Levels (EQ-5D-5L)

"The EQ-5D-5L is a standardized measure of health status. The questionnaire consists of 2 components: the EQ-5D-5L descriptive system and the EQ-5D-5L Visual Analogue scale (EQ-5D-5L VAS). The descriptive system consists of 5 dimensions (mobility, self-care, usual activities, pain/discomfort, anxiety/depression). Each dimension has 5 levels (from 1=no problem to 5=extreme Problems). The digits for the 5 dimensions are combined into a 5-digit code that describes the patient's health state, which is then converted into a single summary index value. Health state index scores generally range from less than 0 (where 0 is the value of a health state equivalent to dead; negative values representing values as worse than dead) to 1 (the value of full health), with higher scores indicating higher health utility.~The EQ-5D-5L VAS records the patient's health on a vertical visual analogue scale, ranging from 100 (=the best health you can imagine) to 0 (=the worst health you can imagine)." (NCT03482882)
Timeframe: From baseline to Week 8

Interventionscore on a scale (Mean)
Baseline EQ-5D-5L index score8 Week EQ-5D-5L index score CFBBaseline EQ-5D-5L VAS8 Week EQ-5D-5L VAS CFB
Pimavanserin Full Analysis Set0.67500.071263.96.7

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Change From Baseline (CFB) in SCOPA Daytime Sleepiness (DS) Score

The SCOPA-DS subscale addresses problems in daytime sleepiness and consists of 6 items (falling asleep unexpectedly, falling asleep peacefully, falling asleep watching TV/reading, falling asleep while talking to someone, having difficulty staying awake, whether falling asleep in the daytime is considered a Problem). Each item has 4 response options (from 0=never to 3=often). The SCOPA-DS subscale score ranges from 0 to 18, with a higher score indicating more severe DS problems. (NCT03482882)
Timeframe: From baseline to Week 8

Interventionscore on a scale (Mean)
Baseline SCOPA-DS8 Week SCOPA-DS CFB
Pimavanserin Full Analysis Set5.2-2.2

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Change From Baseline (CFB) in HAMD-17 Total Score at Weeks 2, 4, and 6

The HAMD-17 is a multiple-item questionnaire to assess the severity of depression, including items of mood, feelings of guilt, suicide ideation, insomnia, agitation or retardation, anxiety, weight loss, and somatic symptoms. Each of the 17 items is scored on a 3- or 5-point scale (depending on the item). The minimum total score is 0; the maximum total score is 52. A higher total score signifies more severe depression. (NCT03482882)
Timeframe: 2, 4, and 6 weeks from baseline

Interventionscore on a scale (Mean)
Baseline HAMD-17 total scoreWeek 2 HAMD-17 total score CFBWeek 4 HAMD-17 total score CFBWeek 6 HAMD-17 total score CFB
Pimavanserin Full Analysis Set19.2-7.5-9.7-9.6

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Change From Baseline to Week 1 in the HAMD-17 Total Score

The HAMD-17 consists of 8 items with a score on a 3 point scale and 9 items with a score on a 5 point scale. The total score ranging from 0 to 52 will be calculated as the sum of the scores for all 17 items. Higher total scores denote more severe depression. (NCT03968159)
Timeframe: Baseline, 1 week

Interventionscore on a scale (Least Squares Mean)
Pimavanserin-3.8
Placebo-3.2

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Change From Baseline to Week 5 in Clinical Global Impression-Severity (CGI-S) Score for Depressive Symptoms

The CGI-S rates the severity of a subject's depression over the past 7 days and the score ranges from 1 to 7. Higher CGI-S scores denote more severe depression. (NCT03968159)
Timeframe: Baseline, 5 weeks

Interventionscore on a scale (Least Squares Mean)
Pimavanserin-1.4
Placebo-1.1

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Change From Baseline to Week 5 in Karolinska Sleepiness Scale (KSS) Score

"The KSS is a scale that measures the subject's drowsiness and is frequently used in studies measuring subjective sleepiness. Scoring is based on a 9-point verbally anchored scale going from 1 = extremely alert to 9 = very sleepy, great effort to keep awake, fighting sleep. Higher scores denote more drowsiness." (NCT03968159)
Timeframe: Baseline, 5 weeks

Interventionscore on a scale (Least Squares Mean)
Pimavanserin-1.4
Placebo-0.8

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Change From Baseline to Week 5 in Sheehan Disability Scale (SDS) Score

The SDS is a 3-item subject-facing questionnaire used to evaluate impairments in the domains of work, social life/leisure, and family life/home responsibility. Subjects rate each item using an 11-point scale ranging from 0 (not at all) to 10 (extremely). Higher scores denote greater disability. (NCT03968159)
Timeframe: Baseline, 5 weeks

Interventionscore on a scale (Least Squares Mean)
Pimavanserin-2.5
Placebo-2.1

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Change From Baseline to Week 5 in the Barratt Impulsiveness Scale (BIS-11)

The BIS-11 is a questionnaire designed to assess the personality/behavioral construct of impulsiveness. It is composed of 30 items describing common impulsive or non-impulsive (reverse scored items: 1, 7, 8, 9, 10, 12, 13, 15, 20, 29, and 30) behaviors and preferences. Items are scored on the following 4-point scale: Rarely/Never = 1; Occasionally = 2; Often = 3; Almost Always/Always = 4. For reverse scored items, a response of 1 is recoded to 4; 2 is recoded to 3; 3 is recoded to 2; and 4 is recoded to 1. The BIS-11 score ranging from 30 to 120 will be calculated as the sum of the scores for all 30 items. Higher scores denote more impulsiveness. (NCT03968159)
Timeframe: Baseline, 5 weeks

Interventionscore on a scale (Least Squares Mean)
Pimavanserin-3.0
Placebo-2.5

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Change From Baseline to Week 5 in the Changes in Sexual Functioning Questionnaire Short Form

The CSFQ-14 is a 14-item version of the CSFQ. This is a patient-facing questionnaire, with a male version and a female version. The total score ranging from 14 to 70 will be calculated as the sum of the scores for all 14 items. Higher total scores denote better sexual functioning. (NCT03968159)
Timeframe: Baseline, 5 weeks

Interventionscore on a scale (Least Squares Mean)
Pimavanserin3.4
Placebo2.5

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Change From Baseline to Week 5 in the Hamilton Depression (HAMD) Anxiety/Somatization Factor Score

The Anxiety/Somatization factor of the HAMD-17 includes 6 items: psychic anxiety, somatic anxiety, gastrointestinal somatic symptoms, general somatic symptoms, hypochondriasis, and insight. The HAMD-17 Anxiety/Somatization factor score ranging from 0 to 18 will be calculated as the sum of the scores for the 6 items. Higher scores denote more severe anxiety/somatization condition. (NCT03968159)
Timeframe: Baseline, 5 weeks

Interventionscore on a scale (Least Squares Mean)
Pimavanserin-2.5
Placebo-2.5

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Clinical Global Impression-Improvement (CGI-I) Score for Depressive Symptoms at Week 5

The CGI-I rates the change in a subject's depression over the past 7 days relative to the subject's symptoms at Baseline and the score ranges from 1 to 7. Higher CGI-I scores denote less improvement in Depression. (NCT03968159)
Timeframe: Baseline, 5 weeks

Interventionscore on a scale (Least Squares Mean)
Pimavanserin2.7
Placebo2.9

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Treatment Responder and Treatment Remission Rates at Week 5

The HAMD-17 consists of 8 items with a score on a 3 point scale and 9 items with a score on a 5 point scale. The total score ranging from 0 to 52 will be calculated as the sum of the scores for all 17 items. Treatment response is defined as a reduction from Baseline in HAMD-17 total score of 50% or more. Treatment remission is defined as a HAMD-17 total score ≤7. (NCT03968159)
Timeframe: Baseline, 5 weeks

,
InterventionParticipants (Count of Participants)
ResponderRemitter
Pimavanserin4627
Placebo4625

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Change From Baseline to Week 5 in Hamilton Depression Scale (17 Items) (HAMD-17) Total Score

The HAMD-17 consists of 8 items with a score on a 3 point scale and 9 items with a score on a 5 point scale. The total score ranging from 0 to 52 will be calculated as the sum of the scores for all 17 items. Higher total scores denote more severe depression. (NCT03968159)
Timeframe: Baseline, Week 5

Interventionscore on a scale (Least Squares Mean)
Pimavanserin-9.0
Placebo-8.1

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Treatment-emergent Adverse Events (TEAEs)

Number of patients with treatment emergent AEs (NCT04000009)
Timeframe: 52 weeks

InterventionParticipants (Count of Participants)
Pimavanserin137

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Treatment-emergent Adverse Events (TEAEs)

Assess the safety and tolerability of pimavanserin in patients with PD in terms of treatment-emergent adverse events. (NCT04164758)
Timeframe: 4-week treatment duration, plus 30 days treatment-free safety follow-up

InterventionParticipants (Count of Participants)
Placebo1
Quetiapine3
Pimavanserin 34 mg1

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Discontinuation Rates Due to Adverse Effects

The number of subjects who discontinue the protocol due to adverse effects (from either protocol or medication) (NCT04188392)
Timeframe: 10 weeks (overall study duration)

InterventionParticipants (Count of Participants)
Open-label Treatment0

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Mean Change in Duration of Stage N3 Sleep Pre- and Post-treatment

The mean difference in duration of stage N3 sleep from baseline polysomnogram to week-6 polysomnogram ([Time in N3 post-treatment] - [Time in N3 at baseline polysomnogram]) (NCT04188392)
Timeframe: 6 weeks (time between baseline and closeout polysomnogram)

Interventionminutes (Mean)
Open-label Treatment21.7

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Recruitment Rates

The rate of enrollment per month; goal of 6 subjects total (NCT04188392)
Timeframe: Total duration of recruitment time (5.8 months)

Interventionparticipants enrolled per month (Mean)
Open-label Treatment1.03

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Retention Rates

The number of subjects who complete the protocol in its entirety; goal of 75% of subjects enrolled into treatment (NCT04188392)
Timeframe: 10 weeks (overall study)

InterventionParticipants (Count of Participants)
Open-label Treatment6

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Completion Rates of Key Outcome Measures

The percentage of participants who complete subject and objective measures of insomnia, including sleep diaries, actigraphy, and attended polysomnography (NCT04188392)
Timeframe: 10 weeks (overall study duration)

InterventionParticipants (Count of Participants)
Completed sleep study 1Completed sleep study 2Completed sleep study 3At least 4 days of actigraphy pre-treatmentAt least 4 days of actigraphy post-treatmentAt least 4 days of sleep diary pre-treatmentAt least 4 days of sleep diary post-treatment
Open-label Treatment6656666

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