U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C25H34FN3O2
Molecular Weight 427.5557
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PIMAVANSERIN

SMILES

CC(C)COc1ccc(cc1)CN=C(N(Cc2ccc(cc2)F)C3CCN(C)CC3)O

InChI

InChIKey=RKEWSXXUOLRFBX-UHFFFAOYSA-N
InChI=1S/C25H34FN3O2/c1-19(2)18-31-24-10-6-20(7-11-24)16-27-25(30)29(23-12-14-28(3)15-13-23)17-21-4-8-22(26)9-5-21/h4-11,19,23H,12-18H2,1-3H3,(H,27,30)

HIDE SMILES / InChI

Molecular Formula C25H34FN3O2
Molecular Weight 427.5557
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: Description was created based on several sources, including http://www.acadia-pharm.com/product/

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

CNS Activity

Curator's Comment:: Pimavanserin readily crosses the blood brain barrier and acts as a CNS-active 5-HT2A inverse agonist.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Nuplazid

Approved Use

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

Launch Date

1.46180158E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
151.8 ng/mL
300 mg single, nasogastric
dose: 300 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
20.3 ng/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
92.9 ng/mL
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
49.7 ng/mL
100 mg single, nasogastric
dose: 100 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
193.4 ng/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
247.5 ng/mL
150 mg 1 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
9.2 ng/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
111.3 ng/mL
200 mg single, nasogastric
dose: 200 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
10798 ng × h/mL
300 mg single, nasogastric
dose: 300 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1315 ng × h/mL
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
1838.7 ng × h/mL
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3742 ng × h/mL
100 mg single, nasogastric
dose: 100 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3804.6 ng × h/mL
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
4680.3 ng × h/mL
150 mg 1 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
706 ng × h/mL
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7335 ng × h/mL
200 mg single, nasogastric
dose: 200 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
53.5 h
300 mg single, nasogastric
dose: 300 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
53 h
50 mg single, oral
dose: 50 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
54.6 h
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
58.3 h
100 mg single, nasogastric
dose: 100 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
60.1 h
100 mg 1 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
48 h
150 mg 1 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
57 h
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
55.4 h
200 mg single, nasogastric
dose: 200 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
3.2%
300 mg single, nasogastric
dose: 300 mg
route of administration: Nasogastric
experiment type: SINGLE
co-administered:
PIMAVANSERIN TARTRATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Disc. AE: Nausea, Vomiting...
Other AEs: Gastrointestinal disorders, Nervous system disorders...
AEs leading to
discontinuation/dose reduction:
Nausea (1 patient)
Vomiting (2 patients)
Dyspepsia (1 patient)
Other AEs:
Gastrointestinal disorders (5 patients)
Nervous system disorders (6 patients)
General system disorders NEC (3 patients)
Sources:
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (1 patient)
Vomiting (1 patient)
Sources:
300 mg single, nasogastric
Highest studied dose
Dose: 300 mg
Route: nasogastric
Route: single
Dose: 300 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Other AEs: Nervous system disorders, General system disorders NEC...
Other AEs:
Nervous system disorders (2 patients)
General system disorders NEC (1 patient)
Vascular disorders (1 patient)
Sources:
50 mg single, oral
Highest studied dose
Dose: 50 mg
Route: oral
Route: single
Dose: 50 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Other AEs: Cardiac disorders, Gastrointestinal disorders...
Other AEs:
Cardiac disorders (1 patient)
Gastrointestinal disorders (2 patients)
Nervous system disorders (2 patients)
Sources:
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Disc. AE: Confusional state, Psychotic disorder...
AEs leading to
discontinuation/dose reduction:
Confusional state (0.5%)
Psychotic disorder (1.5%)
Mental status changes (1.5%)
Headache (0.5%)
Asthenia (0.5%)
Infections and infestations (1%)
Urinary tract infection (1%)
Pollakiuria (0.5%)
Dehydration (0.5%)
Respiratory distress (0.5%)
Sources: Page: 109
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources:
unhealthy, > 40 years
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: > 40 years
Sex: M+F
Population Size: 202
Sources:
Disc. AE: Hallucination, Fatigue...
AEs leading to
discontinuation/dose reduction:
Hallucination (2%)
Fatigue (1%)
Sources:
17 mg 2 times / day multiple, oral
Recommended
Dose: 17 mg, 2 times / day
Route: oral
Route: multiple
Dose: 17 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: dementia-related psychosis
Sources:
Other AEs: Heart failure, Pneumonia...
Other AEs:
Heart failure (grade 5)
Pneumonia (grade 5)
Sources:
AEs

AEs

AESignificanceDosePopulation
Dyspepsia 1 patient
Disc. AE
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Nausea 1 patient
Disc. AE
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Vomiting 2 patients
Disc. AE
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
General system disorders NEC 3 patients
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Gastrointestinal disorders 5 patients
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Nervous system disorders 6 patients
150 mg 1 times / day multiple, oral
Highest studied dose
Dose: 150 mg, 1 times / day
Route: oral
Route: multiple
Dose: 150 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Nausea 1 patient
Disc. AE
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
Vomiting 1 patient
Disc. AE
100 mg 1 times / day multiple, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
healthy, 23.8 years (range: 19-28 years)
n = 6
Health Status: healthy
Age Group: 23.8 years (range: 19-28 years)
Sex: M
Population Size: 6
Sources:
General system disorders NEC 1 patient
300 mg single, nasogastric
Highest studied dose
Dose: 300 mg
Route: nasogastric
Route: single
Dose: 300 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Vascular disorders 1 patient
300 mg single, nasogastric
Highest studied dose
Dose: 300 mg
Route: nasogastric
Route: single
Dose: 300 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Nervous system disorders 2 patients
300 mg single, nasogastric
Highest studied dose
Dose: 300 mg
Route: nasogastric
Route: single
Dose: 300 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Cardiac disorders 1 patient
50 mg single, oral
Highest studied dose
Dose: 50 mg
Route: oral
Route: single
Dose: 50 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Gastrointestinal disorders 2 patients
50 mg single, oral
Highest studied dose
Dose: 50 mg
Route: oral
Route: single
Dose: 50 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Nervous system disorders 2 patients
50 mg single, oral
Highest studied dose
Dose: 50 mg
Route: oral
Route: single
Dose: 50 mg
Sources:
healthy, 25.8 years (range: 25-28 years)
n = 4
Health Status: healthy
Age Group: 25.8 years (range: 25-28 years)
Sex: M
Population Size: 4
Sources:
Asthenia 0.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Confusional state 0.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Dehydration 0.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Headache 0.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Pollakiuria 0.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Respiratory distress 0.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Infections and infestations 1%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Urinary tract infection 1%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Mental status changes 1.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Psychotic disorder 1.5%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources: Page: 109
unhealthy, 71 years (range: 41-85 years)
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: 71 years (range: 41-85 years)
Sex: M+F
Population Size: 202
Sources: Page: 109
Fatigue 1%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources:
unhealthy, > 40 years
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: > 40 years
Sex: M+F
Population Size: 202
Sources:
Hallucination 2%
Disc. AE
34 mg 1 times / day multiple, oral
Recommended
Dose: 34 mg, 1 times / day
Route: oral
Route: multiple
Dose: 34 mg, 1 times / day
Sources:
unhealthy, > 40 years
n = 202
Health Status: unhealthy
Condition: hallucinations and delusions associated with Parkinson’s disease psychosis
Age Group: > 40 years
Sex: M+F
Population Size: 202
Sources:
Heart failure grade 5
17 mg 2 times / day multiple, oral
Recommended
Dose: 17 mg, 2 times / day
Route: oral
Route: multiple
Dose: 17 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: dementia-related psychosis
Sources:
Pneumonia grade 5
17 mg 2 times / day multiple, oral
Recommended
Dose: 17 mg, 2 times / day
Route: oral
Route: multiple
Dose: 17 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Condition: dementia-related psychosis
Sources:
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 133 uM]
no [IC50 34.6 uM]
no [IC50 43 uM]
no [IC50 43.8 uM]
no
no
no
no
no
no
no
no
no
no
no
no
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
yes
yes (co-administration study)
Comment: Ketoconazole increased Pimavanserin Cmax and AUC by 1.5- and 3- fold, respectively
Page: 9.0
yes
yes (co-administration study)
Comment: Ketoconazole increased Pimavanserin Cmax and AUC by 1.5- and 3- fold, respectively
Page: 2.0
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
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.
2004 Sep
A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model.
2008 Oct
Parkinson's disease dementia.
2010 Jul
Serotonin 5-HT(2A) receptor antagonists in the treatment of insomnia: present status and future prospects.
2010 Mar
Pimavanserin, a serotonin(2A) receptor inverse agonist, for the treatment of parkinson's disease psychosis.
2010 Mar
Pimavanserin for the treatment of Parkinson's disease psychosis.
2013 Oct
Patents

Sample Use Guides

The recommended dose of NUPLAZID (Pimavanserin) is 34 mg, taken orally as two 17 mg strength tablets once daily, without titration. Pimavanserin can be taken with or without food.
Route of Administration: Oral
In vitro, pimavanserin acts as an inverse agonist and antagonist at serotonin 5-HT2A receptors with high binding affinity (Ki value 0.087 nM) and at serotonin 5-HT2C receptors with lower binding affinity (Ki value 0.44 nM).
Substance Class Chemical
Created
by admin
on Sat Jun 26 04:06:42 UTC 2021
Edited
by admin
on Sat Jun 26 04:06:42 UTC 2021
Record UNII
JZ963P0DIK
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PIMAVANSERIN
DASH   INN   WHO-DD  
INN  
Official Name English
PIMAVANSERIN [INN]
Common Name English
PIMAVANSERIN [MI]
Common Name English
PIMAVANSERIN [WHO-DD]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175430
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
WHO-ATC N05AX17
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
NCI_THESAURUS C66885
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
Code System Code Type Description
MERCK INDEX
M11934
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
DRUG BANK
DB05316
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
CAS
706779-91-1
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
FDA UNII
JZ963P0DIK
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
RXCUI
1791685
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
NCI_THESAURUS
C76444
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
DRUG CENTRAL
5142
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
EVMPD
SUB183869
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
INN
8877
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
PUBCHEM
10071196
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
WIKIPEDIA
PIMAVANSERIN
Created by admin on Sat Jun 26 04:06:42 UTC 2021 , Edited by admin on Sat Jun 26 04:06:42 UTC 2021
PRIMARY
Related Record Type Details
BINDER->LIGAND
BINDING
SALT/SOLVATE -> PARENT
EXCRETED UNCHANGED
FECAL
TARGET->INVERSE AGONIST
AGONIST
Ki
TARGET->INVERSE AGONIST
AGONIST
Ki
METABOLIC ENZYME -> SUBSTRATE
MINOR
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
URINE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC