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Details

Stereochemistry ACHIRAL
Molecular Formula C24H27FN2O4
Molecular Weight 426.4815
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ILOPERIDONE

SMILES

CC(=O)c1ccc(c(c1)OC)OCCCN2CCC(CC2)c3c4ccc(cc4on3)F

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 426.4815
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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
110.0 nM [IC50]
0.4 nM [IC50]
210.0 nM [IC50]
0.4 nM [IC50]
161.0 nM [IC50]
0.011 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
FANAPT

Approved Use

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

Launch Date

1.24148161E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.79 ng/mL
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
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
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
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%
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%
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:
unhealthy, 18 - 55
n = 24
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 18 - 55
Population Size: 24
Sources:
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: Page: p.3
unhealthy, 42 (13.1)
n = 31
Health Status: unhealthy
Condition: Bipolar Disorder
Age Group: 42 (13.1)
Sex: M+F
Population Size: 31
Sources: Page: p.3
438 mg multiple, oral (total)
Overdose
Dose: 438 mg
Route: oral
Route: multiple
Dose: 438 mg
Sources: Page: p.17
unhealthy
n = 1
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1
Sources: Page: p.17
Other AEs: Extrapyramidal symptoms, Electrocardiogram QTc interval prolonged...
Other AEs:
Extrapyramidal symptoms
Electrocardiogram QTc interval prolonged
Sources: Page: p.17
576 mg single, oral
Overdose
Dose: 576 mg
Route: oral
Route: single
Dose: 576 mg
Sources: Page: p.17
unhealthy
n = 1
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1
Sources: Page: p.17
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: Page: p.9
unhealthy
n = 874
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 874
Sources: Page: p.9
Other AEs: Somnolence...
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
Other AEs: Orthostatic hypotension...
Other AEs:
Orthostatic hypotension (5%)
Sources: Page: p.7
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
Other AEs: Weight gain...
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: Page: p.8
unhealthy
n = 3210
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 3210
Sources: Page: p.8
Other AEs: Gynecomastia, Galactorrhea...
Other AEs:
Gynecomastia (0.1%)
Galactorrhea (0.2%)
Sources: Page: p.8
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: Page: p.8
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.8
Other AEs: Hyperprolactinemia...
Other AEs:
Hyperprolactinemia (26%)
Sources: Page: p.8
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
n = 1344
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1344
Sources: Page: p.7
Other AEs: Syncope...
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
n = 1344
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1344
Sources: Page: p.7
Other AEs: Seizures...
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
Other AEs: Leukopenia, Neutropenia...
Other AEs:
Leukopenia
Neutropenia
Agranulocytosis
Sources: Page: p.7
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.8
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.8
Other AEs: Temperature regulation disorder, Dysphagia...
Other AEs:
Temperature regulation disorder
Dysphagia
Sources: Page: p.8
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.9
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.9
Other AEs: Suicide attempt, Priapism...
Other AEs:
Suicide attempt
Priapism
Sources: Page: p.9
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: Page: p.4
unhealthy
n = 160
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 160
Sources: Page: p.4
Other AEs: QT interval prolonged...
Other AEs:
QT interval prolonged
Sources: Page: p.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: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.5
Other AEs: Neuroleptic malignant syndrome...
Other AEs:
Neuroleptic malignant syndrome
Sources: Page: p.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: Page: p.6
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.6
Other AEs: Tardive dyskinesia, Hyperglycemia...
Other AEs:
Tardive dyskinesia
Hyperglycemia
Sources: Page: p.6
AEs

AEs

AESignificanceDosePopulation
Electrocardiogram QTc interval prolonged
438 mg multiple, oral (total)
Overdose
Dose: 438 mg
Route: oral
Route: multiple
Dose: 438 mg
Sources: Page: p.17
unhealthy
n = 1
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1
Sources: Page: p.17
Extrapyramidal symptoms
438 mg multiple, oral (total)
Overdose
Dose: 438 mg
Route: oral
Route: multiple
Dose: 438 mg
Sources: Page: p.17
unhealthy
n = 1
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1
Sources: Page: p.17
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: Page: p.9
unhealthy
n = 874
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 874
Sources: Page: p.9
Orthostatic hypotension 5%
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
Weight gain 18%
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
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: Page: p.8
unhealthy
n = 3210
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 3210
Sources: Page: p.8
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: Page: p.8
unhealthy
n = 3210
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 3210
Sources: Page: p.8
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: Page: p.8
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.8
Syncope 0.4%
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
n = 1344
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1344
Sources: Page: p.7
Seizures 0.1%
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
n = 1344
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 1344
Sources: Page: p.7
Agranulocytosis
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
Leukopenia
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
Neutropenia
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.7
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.7
Dysphagia
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.8
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.8
Temperature regulation disorder
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.8
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.8
Priapism
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.9
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.9
Suicide attempt
12 mg 2 times / day multiple, oral (max)
Recommended
Dose: 12 mg, 2 times / day
Route: oral
Route: multiple
Dose: 12 mg, 2 times / day
Sources: Page: p.9
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.9
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: Page: p.4
unhealthy
n = 160
Health Status: unhealthy
Condition: Schizophrenia
Population Size: 160
Sources: Page: p.4
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: Page: p.5
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.5
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: Page: p.6
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.6
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: Page: p.6
unhealthy
Health Status: unhealthy
Condition: Schizophrenia
Sources: Page: p.6
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
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
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
weak
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
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
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
PubMed

PubMed

TitleDatePubMed
The pharmacological profile of iloperidone, a novel atypical antipsychotic agent.
1995 Sep
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
2001 Dec
Advances in atypical antipsychotics for the treatment of schizophrenia: new formulations and new agents.
2002
Receptor profile of P88-8991 and P95-12113, metabolites of the novel antipsychotic iloperidone.
2002 Apr
New antipsychotic agents for schizophrenia: pharmacokinetics and metabolism update.
2002 Jul
Gateways to clinical trials.
2002 Nov
Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism.
2002 Nov 29
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
alpha2C-Adrenoceptor blockade by clozapine and other antipsychotic drugs.
2003 Feb 21
Functional characterization of the novel antipsychotic iloperidone at human D2, D3, alpha 2C, 5-HT6, and 5-HT1A receptors.
2003 Jul 18
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 Apr
Association of the NPAS3 gene and five other loci with response to the antipsychotic iloperidone identified in a whole genome association study.
2009 Aug
Iloperidone: a new option for the treatment of schizophrenia.
2009 Dec
Iloperidone: in schizophrenia.
2009 Oct
New atypical antipsychotics for schizophrenia: iloperidone.
2010 Feb 18
Iloperidone (Fanapt)--another second-generation antipsychotic.
2010 Feb 22
Absence of weight gain association with the HTR2C -759C/T polymorphism in patients with schizophrenia treated with iloperidone.
2010 Feb 28
New drugs: asenapine, iloperidone, and bepotastine besilate.
2010 Jan-Feb
Atypical antipsychotic metabolism and excretion.
2010 Jul
Iloperidone redux: a dissection of the Drug Approval Package for this newly commercialised second-generation antipsychotic.
2010 May
The effect of metformin on anthropometrics and insulin resistance in patients receiving atypical antipsychotic agents: a meta-analysis.
2010 Oct
Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults.
2013 Jan
Patents

Sample Use Guides

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
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 Sat Jun 26 00:04:24 UTC 2021
Edited
by admin
on Sat Jun 26 00:04:24 UTC 2021
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
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
FANAPT
Brand Name English
ILOPERIDONE [MI]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175430
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
LIVERTOX 498
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
WHO-VATC QN05AX14
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
NCI_THESAURUS C29710
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
WHO-ATC N05AX14
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
Code System Code Type Description
DRUG BANK
DB04946
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
EVMPD
SUB08135MIG
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
WIKIPEDIA
Iloperidone
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
LACTMED
Iloperidone
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
ChEMBL
CHEMBL14376
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
INN
7045
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
MERCK INDEX
M6211
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY Merck Index
USP_CATALOG
1336249
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY USP-RS
NCI_THESAURUS
C83784
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
EPA CompTox
133454-47-4
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
PUBCHEM
71360
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
CAS
133454-47-4
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
HSDB
8207
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
RXCUI
73178
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY RxNorm
MESH
C081732
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
FDA UNII
VPO7KJ050N
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
DRUG CENTRAL
3294
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
IUPHAR
87
Created by admin on Sat Jun 26 00:04:24 UTC 2021 , Edited by admin on Sat Jun 26 00:04:24 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
MAJOR
Ki
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.
TARGET -> INHIBITOR
MAJOR
Ki
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
MAJOR
Ki
Related Record Type Details
METABOLITE -> PARENT
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
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.
METABOLITE -> PARENT
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
METABOLITE -> PARENT
METABOLITE -> PARENT
FECAL; URINE
METABOLITE -> PARENT
MINOR
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
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