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

Details

Stereochemistry ACHIRAL
Molecular Formula C24H27FN2O4
Molecular Weight 426.4806
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ILOPERIDONE

SMILES

COC1=CC(=CC=C1OCCCN2CCC(CC2)C3=NOC4=C3C=CC(F)=C4)C(C)=O

InChI

InChIKey=XMXHEBAFVSFQEX-UHFFFAOYSA-N
InChI=1S/C24H27FN2O4/c1-16(28)18-4-7-21(23(14-18)29-2)30-13-3-10-27-11-8-17(9-12-27)24-20-6-5-19(25)15-22(20)31-26-24/h4-7,14-15,17H,3,8-13H2,1-2H3

HIDE SMILES / InChI
Molecular Formula C24H27FN2O4
Molecular Weight 426.4806
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.accessdata.fda.gov/drugsatfda_docs/label/2016/022192s015lbl.pdf

Iloperidone, also known as Fanapt, Fanapta, and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia. Iloperidone shows high affinity and maximal receptor occupancy for dopamine D2 receptors in the caudate nucleus and putamen of the brains of schizophrenic patients. The improvement in cognition is attributed to iloperidone's high affinity for α adrenergic receptors. Iloperidone also binds with high affinity to serotonin 5-HT2a and dopamine 3 receptors. Iloperidone binds with moderate affinity to dopamine D4, serotonin 5-HT6 and 5-HT7, and norepinephrine NEα1 receptors. Furthermore, iloperidone binds with weak affinity to serotonin 5-HT1A, dopamine D1, and histamine H1 receptors. Iloperidone is indicated for the treatment of acute schizophrenia.

CNS Activity

Originator

Approval Year

2009
364
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
 110.0 nM [IC50]
Antagonist
2849
 0.4 nM [IC50]
Antagonist
2849
 210.0 nM [IC50]
Antagonist
2849
 0.4 nM [IC50]
Inhibitor
8504
 161.0 nM [IC50]
Antagonist
2849
 0.011 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
FANAPT

Approved Use

FANAPT is an atypical antipsychotic indicated for the treatment of schizophrenia in adults.

Launch Date

2009
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.79 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21034370/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ILOPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
29.4 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21034370/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ILOPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
17.6 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21034370/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ILOPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
18 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ILOPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/21034370/
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ILOPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf
3 mg single, oral
dose: 3 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ILOPERIDONE plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
32 mg 1 times / day multiple, oral
MTD
Dose: 32 mg, 1 times / day
Route: oral
Route: multiple
Dose: 32 mg, 1 times / day
Sources:
https://onlinelibrary.wiley.com/doi/epdf/10.1111/j.1527-3458.1997.tb00320.x
https://pubmed.ncbi.nlm.nih.gov/20368905
unhealthy, 18 - 55
Health Status: unhealthy
Age Group: 18 - 55
Sources:
https://onlinelibrary.wiley.com/doi/epdf/10.1111/j.1527-3458.1997.tb00320.x
https://pubmed.ncbi.nlm.nih.gov/20368905
Sources:
https://onlinelibrary.wiley.com/doi/epdf/10.1111/j.1527-3458.1997.tb00320.x
https://pubmed.ncbi.nlm.nih.gov/20368905
24 mg 1 times / day multiple, oral
Highest studied dose
Dose: 24 mg, 1 times / day
Route: oral
Route: multiple
Dose: 24 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/28817490
unhealthy, 42 (13.1)
Health Status: unhealthy
Age Group: 42 (13.1)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28817490
Sources:
https://pubmed.ncbi.nlm.nih.gov/28817490
438 mg multiple, oral
Overdose
Dose: 438 mg
Route: oral
Route: multiple
Dose: 438 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Extrapyramidal symptoms, Electrocardiogram QTc interval prolonged...
Other AEs:
Extrapyramidal symptoms
Electrocardiogram QTc interval prolonged
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
576 mg single, oral
Overdose
Dose: 576 mg
Route: oral
Route: single
Dose: 576 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
10 mg 2 times / day multiple, oral
Recommended
Dose: 10 mg, 2 times / day
Route: oral
Route: multiple
Dose: 10 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Somnolence...
Other AEs:
Somnolence (11.9%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: QT interval prolonged...
Other AEs:
QT interval prolonged
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Neuroleptic malignant syndrome...
Other AEs:
Neuroleptic malignant syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Tardive dyskinesia, Hyperglycemia...
Other AEs:
Tardive dyskinesia
Hyperglycemia
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Weight gain...
Other AEs:
Weight gain (18%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Orthostatic hypotension...
Other AEs:
Orthostatic hypotension (5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Hyperprolactinemia...
Other AEs:
Hyperprolactinemia (26%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Gynecomastia, Galactorrhea...
Other AEs:
Gynecomastia (0.1%)
Galactorrhea (0.2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Syncope...
Other AEs:
Syncope (0.4%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Seizures...
Other AEs:
Seizures (0.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Leukopenia, Neutropenia...
Other AEs:
Leukopenia
Neutropenia
Agranulocytosis
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Temperature regulation disorder, Dysphagia...
Other AEs:
Temperature regulation disorder
Dysphagia
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Other AEs: Suicide attempt, Priapism...
Other AEs:
Suicide attempt
Priapism
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Electrocardiogram QTc interval prolonged
438 mg multiple, oral
Overdose
Dose: 438 mg
Route: oral
Route: multiple
Dose: 438 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Extrapyramidal symptoms
438 mg multiple, oral
Overdose
Dose: 438 mg
Route: oral
Route: multiple
Dose: 438 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Somnolence 11.9%
10 mg 2 times / day multiple, oral
Recommended
Dose: 10 mg, 2 times / day
Route: oral
Route: multiple
Dose: 10 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
QT interval prolonged
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Neuroleptic malignant syndrome
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Hyperglycemia
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Tardive dyskinesia
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Weight gain 18%
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Orthostatic hypotension 5%
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Hyperprolactinemia 26%
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Gynecomastia 0.1%
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Galactorrhea 0.2%
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Syncope 0.4%
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Seizures 0.1%
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Agranulocytosis
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Leukopenia
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Neutropenia
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Dysphagia
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Temperature regulation disorder
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Priapism
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Suicide attempt
12 mg 2 times / day multiple, oral
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inducer
1087

inhibitor
2252
substrate
1193

inhibitor
2438

inducer
440
substrate
1388

inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A1
132

CYP1A2
2153

CYP2A6
879

CYP2B6
926

CYP2C8
1057

CYP2E1
1060

P-gp
1741
CYP1A1
389

CYP1A2
1197

CYP2A6
626

CYP2B6
776

CYP2C8
810

CYP2C19
1119

CYP2E1
729

P-gp
2052
CYP1A2
832

CYP2C8
198

CYP2C19
329

CYP3A5
92
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A1
272
 no
CYP1A2
2333
 no
CYP1A2
2333
 no
CYP2A6
911
 no
CYP2B6
1160
 no
CYP2C19
2141
 no
CYP2C8
1117
 no
CYP2C8
1117
 no
CYP2C9
2497
 no
CYP2C9
2497
 no
CYP2E1
1146
 no
CYP3A4
2633
 no
CYP3A5
201
 no
CYP2D6
2546
 unlikely
weak (co-administration study)
Comment: 17% increase in total exposure and a 26% increase in the maximum plasma concentrations Cmax of dextromethorphan;
Page: 16.0
CYP3A4
2633
 unlikely
weak (co-administration study)
Comment: a less than 50% increase in midazolam total exposure at iloperidone steady state (14 days of oral dosing at up to 10 mg iloperidone twice daily) and no effect on midazolam Cmax;
Page: 16.0
P-gp
1932
 weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A1
389
 no
CYP1A2
1197
 no
CYP2A6
626
 no
CYP2B6
776
 no
CYP2C19
1119
 no
CYP2C8
810
 no
CYP2C9
1193
 no
CYP2E1
729
 no
P-gp
2052
 no
CYP3A4
1946
 yes
yes (co-administration study)
Comment: administration of ketoconazole (CYP3A4 inhibitor) increased AUC of iloperidone by 57%; administration with paroxetine AND ketoconazole resulted in a 1.4 fold increase in steady-state concentration of iloperidone;
Page: 15.0
CYP2D6
1388
 yes
yes (pharmacogenomic study)
Comment: pharmacogenic study?; administration of fluoxetine (potent inhibitor of CYP2D6) increased AUC of iloperidone by about 2- to 3-fold; administration of paroxetine (potent inhibitor of CYP2D6) increased mean steady-state peak concentrations of iloperidone by about 1.6 fold; administration with paroxetine AND ketoconazole resulted in a 1.4 fold increase in steady-state concentration of iloperidone;
Page: 15.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:65173
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:65173
ChemicalBook
CB4772066
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB4772066
eMolecules
2726053
https://www.emolecules.com/cgi-bin/more?vid=2726053
MolPort
MolPort-005-934-272
https://www.molport.com/shop/molecule-link/MolPort-005-934-272
Selleck Chemicals
Iloperidone(Fanapt)
http://www.selleckchem.com/products/Iloperidone(Fanapt).html
ZINC
ZINC000001548097
http://zinc15.docking.org/substances/ZINC000001548097
PubMed

PubMed

TitleDatePubMed
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
2013-11
Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults.
2013-01
A review of new atypical antipsychotic launches in the United States.
2010-12
Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion.
2010-12
The effect of metformin on anthropometrics and insulin resistance in patients receiving atypical antipsychotic agents: a meta-analysis.
2010-10
New antipsychotic drugs: how do their receptor-binding profiles compare?
2010-09
Iloperidone for the treatment of schizophrenia.
2010-08
Iloperidone for schizophrenia.
2010-08
Atypical antipsychotic metabolism and excretion.
2010-07
Iloperidone for the treatment of schizophrenia.
2010-05
Iloperidone redux: a dissection of the Drug Approval Package for this newly commercialised second-generation antipsychotic.
2010-05
Gateways to clinical trials.
2010-04-13
Absence of weight gain association with the HTR2C -759C/T polymorphism in patients with schizophrenia treated with iloperidone.
2010-02-28
Iloperidone (Fanapt)--another second-generation antipsychotic.
2010-02-22
New atypical antipsychotics for schizophrenia: iloperidone.
2010-02-18
New drugs: asenapine, iloperidone, and bepotastine besilate.
2010-01-26
Iloperidone: a new option for the treatment of schizophrenia.
2009-12
Whole genome association study identifies polymorphisms associated with QT prolongation during iloperidone treatment of schizophrenia.
2009-11
Iloperidone: in schizophrenia.
2009-10
Iloperidone for schizophrenia: a review of the efficacy and safety profile for this newly commercialised second-generation antipsychotic.
2009-08
Association of the NPAS3 gene and five other loci with response to the antipsychotic iloperidone identified in a whole genome association study.
2009-08
Applicability of a genetic signature for enhanced iloperidone efficacy in the treatment of schizophrenia.
2009-06
Akathisia and second-generation antipsychotic drugs.
2009-05
Genome-wide association studies in pharmacogenomics: untapped potential for translation.
2009-04-28
Further characterization of the discriminative stimulus properties of the atypical antipsychotic drug clozapine in C57BL/6 mice: role of 5-HT(2A) serotonergic and alpha (1) adrenergic antagonism.
2009-04
Pharmacogenomics: the promise of personalized medicine for CNS disorders.
2009-01
Gateways to clinical trials. July-August 2008.
2008-10-14
Gateways to clinical trials.
2008-10
American psychiatric association.
2008-06
Efficacy of iloperidone in the treatment of schizophrenia: initial phase 3 studies.
2008-04
Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia.
2008-04
Four-week, double-blind, placebo- and ziprasidone-controlled trial of iloperidone in patients with acute exacerbations of schizophrenia.
2008-04
Safety profile of iloperidone: a pooled analysis of 6-week acute-phase pivotal trials.
2008-04
New advances in the treatment of schizophrenia. Introduction.
2008-04
Effect of a ciliary neurotrophic factor polymorphism on schizophrenia symptom improvement in an iloperidone clinical trial.
2008-03
Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market?
2008-01
Upcoming agents for the treatment of schizophrenia: mechanism of action, efficacy and tolerability.
2008
Iloperidone reduces sensorimotor gating deficits in pharmacological models, but not a developmental model, of disrupted prepulse inhibition in rats.
2006-09
Atypical antipsychotics: pharmacokinetics, therapeutic drug monitoring and pharmacological interactions.
2004-02
Differential effects of iloperidone, clozapine, and haloperidol on working memory of rats in the delayed non-matching-to-position paradigm.
2003-09
Functional characterization of the novel antipsychotic iloperidone at human D2, D3, alpha 2C, 5-HT6, and 5-HT1A receptors.
2003-07-18
Effects of clozapine, haloperidol and iloperidone on neurotransmission and synaptic plasticity in prefrontal cortex and their accumulation in brain tissue: an in vitro study.
2003
Gateways to clinical trials.
2002-11
Iloperidone (Novartis).
2002-01
Treatments for chronic psychosis.
2001-12
Iloperidone (Hoechst Marion Roussel Inc).
1999-06
Iloperidone binding to human and rat dopamine and 5-HT receptors.
1996-12-19
The pharmacological profile of iloperidone, a novel atypical antipsychotic agent.
1995-09
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
1995-03-31
The ratios of serotonin2 and dopamine2 affinities differentiate atypical and typical antipsychotic drugs.
1989
Patents

Patents

05571814
10
05580875
7
05580890
9
05580891
6
JP2011508765A
9

Sample Use Guides

In Vivo Use Guide
The recommended target dosage is 12 to 24 mg/day administered twice daily. This target dosage range is achieved by daily dosage adjustments, alerting patients to symptoms of orthostatic hypotension, starting at a dose of 1 mg twice daily, then moving to 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, and 12 mg twice daily on Days 2, 3, 4, 5, 6, and 7 respectively, to reach the 12 mg/day to 24 mg/day dose range.
Route of Administration: Oral
In Vitro Use Guide
While pacing the hearts at stimulation cycle lengths of 200 or 250 ms, or during natural sinus rhythm (no external pacing), iloperidone 100 nmol/L prolonged MAPD(90) by respectively 9.2 ± 0.9, 11.2 ± 1.6 and 21.4 ± 2.3 ms.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:05:45 GMT 2025
Edited
by admin
on Mon Mar 31 18:05:45 GMT 2025
Record UNII
VPO7KJ050N
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ILOPERIDONE
DASH   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
FANAPT
Preferred Name English
ILOPERIDONE [VANDF]
Common Name English
HP-873
Code English
ILOPERIDONE [USAN]
Common Name English
4'-(3-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)PIPERIDINO)PROPOXY)-3'-METHOXYACETOPHENONE
Systematic Name English
ILOPERIDONE [ORANGE BOOK]
Common Name English
Iloperidone [WHO-DD]
Common Name English
ILOPERIDONE [MART.]
Common Name English
HP 873
Code English
ETHANONE, 1-(4-(3-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)PROPOXY)-3-METHOXYPHENYL)-
Systematic Name English
iloperidone [INN]
Common Name English
ILOPERIDONE [USP-RS]
Common Name English
ILOPERIDONE [MI]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175430
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
LIVERTOX NBK548669
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
WHO-VATC QN05AX14
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
NCI_THESAURUS C29710
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
WHO-ATC N05AX14
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
Code System Code Type Description
CHEBI
65173
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
DRUG BANK
DB04946
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
EVMPD
SUB08135MIG
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
WIKIPEDIA
Iloperidone
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
LACTMED
Iloperidone
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
DAILYMED
VPO7KJ050N
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
ChEMBL
CHEMBL14376
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
INN
7045
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
MERCK INDEX
m6211
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY Merck Index
NCI_THESAURUS
C83784
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
EPA CompTox
DTXSID6049060
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
PUBCHEM
71360
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
RS_ITEM_NUM
1336249
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
SMS_ID
100000083913
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
CAS
133454-47-4
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
HSDB
8207
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
RXCUI
73178
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY RxNorm
MESH
C081732
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
USAN
EE-25
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
FDA UNII
VPO7KJ050N
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
DRUG CENTRAL
3294
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
IUPHAR
87
Created by admin on Mon Mar 31 18:05:45 GMT 2025 , Edited by admin on Mon Mar 31 18:05:45 GMT 2025
PRIMARY
Related Record Type Details
5-HYDROXYTRYPTAMINE RECEPTOR 2A
TARGET -> INHIBITOR
MAJOR
Ki
Structure of ILOPERIDONE
EXCRETED UNCHANGED
Iloperidone counted 0.7 % of dose in excreta from all six human subjects following a single oral dose of 3 mg 14C ILO522.
D(3) DOPAMINE RECEPTOR
TARGET -> INHIBITOR
MAJOR
Ki
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 2D6
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
D(2) DOPAMINE RECEPTOR
TARGET -> INHIBITOR
MAJOR
Ki
Related Record Type Details
Structure of 1-(4-(3-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)PROPOXY)-3-METHOXYPHENYL)-2-HYDROXYETHANONE
METABOLITE -> PARENT
Structure of 1-(4-(3-(4-(6-FLUORO-1,2-BENZOXAZOL-3-YL)-1-PIPERIDYL)PROPOXY)-3-METHOXY-PHENYL)ETHANE-1,2-DIOL
METABOLITE -> PARENT
This metabolite counted 4.8 % of dose in excreta from all six human subjects following a single oral dose of 3 mg 14C ILO522.
MINOR
Structure of 3-(4-ACETYL-2-METHOXYPHENOXY)PROPANOIC ACID
METABOLITE -> PARENT
This metabolite counted 6.5 % of dose in excreta from all six human subjects following a single oral dose of 3 mg 14C ILO522.
Structure of P-88-8991, (-)-
METABOLITE -> PARENT
Structure of PHENOL, 4-(3-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)PROPOXY)-3-METHOXY-
METABOLITE -> PARENT
Structure of (2S,3S,4S,5R,6R)-6-(1-(4-(3-(4-(6-FLUORO-1,2-BENZOXAZOL-3-YL)-1-PIPERIDYL)PROPOXY)-3-METHOXY-PHENYL)ETHOXY)-3,4,5-TRIHYDROXY-TETRAHYDROPYRAN-2-CARBOXYLIC ACID
METABOLITE -> PARENT
This metabolite counted 1.5 % of dose in excreta from all six human subjects following a single oral dose of 3 mg 14C IL0522.
Structure of 1-(4-(3-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-OXIDO-1-PIPERIDINYL)PROPOXY)-3-METHOXYPHENYL)ETHANONE
METABOLITE -> PARENT
This metabolite counted 0.4 % of dose in excreta from all six human subjects following a single oral dose of 3 mg 14C ILO522.
MINOR
Structure of 2-(4-(3-(4-(6-FLUORO-1,2-BENZOXAZOL-3-YL)-1-PIPERIDYL)PROPOXY)-3-METHOXY-PHENYL)-2-HYDROXY-ACETIC ACID
METABOLITE -> PARENT
This metabolite counted <3.1 % of dose in excreta from all six human subjects following a single oral dose of 3 mg 14C ILO522.
MINOR
Structure of (2S,3S,4S,5R,6S)-6-(4-(3-(4-(6-FLUORO-1,2-BENZOXAZOL-3-YL)-1-PIPERIDYL)PROPOXY)-3-METHOXY-PHENOXY)-3,4,5-TRIHYDROXY-TETRAHYDROPYRAN-2-CARBOXYLIC ACID
METABOLITE -> PARENT
Structure of 4-(3-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)PROPOXY)-3-METHOXYBENZOIC ACID
METABOLITE -> PARENT
Structure of 1-(4-(3-(4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)PROPOXY)-3-HYDROXYPHENYL)ETHANONE
METABOLITE -> PARENT
MINOR
Structure of (4-FLUORO-2-HYDROXY-PHENYL)-(1-(3-(4-HYDROXY-2-METHOXY-PHENOXY)PROPYL)-4-PIPERIDYL)METHANONE
METABOLITE -> PARENT
Structure of P-88-8991
METABOLITE ACTIVE -> PARENT
The active metabolite P88 accounts for 19.5% and 34.0% of total plasma exposure in EM and PM, respectively.
MAJOR
PLASMA; URINE
Related Record Type Details
Structure of 4-(3-CHLOROPROPOXY)-3-METHOXYACETOPHENONE
IMPURITY -> PARENT
Related Record Type Details
Structure of ILOPERIDONE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC HIGH-FAT MEAL

FED CONDITION

ORAL ADMINISTRATION

Tmax PHARMACOKINETIC ORAL ADMINISTRATION

NIH
NCATS
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