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
SMILES
COC1=CC(=CC=C1OCCCN2CCC(CC2)C3=NOC4=CC(F)=CC=C34)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
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 |
DescriptionSources: http://www.drugbank.ca/drugs/DB04946Curator's Comment: Description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022192s015lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB04946
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL217 Sources: http://www.drugbank.ca/drugs/DB04946 |
110.0 nM [IC50] | ||
Target ID: CHEMBL1907610 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7562515 |
0.4 nM [IC50] | ||
Target ID: CHEMBL273 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7562515 |
210.0 nM [IC50] | ||
Target ID: CHEMBL327 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7707315 |
0.4 nM [IC50] | ||
Target ID: CHEMBL240 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22465688 |
161.0 nM [IC50] | ||
Target ID: CHEMBL224 Sources: http://www.drugbank.ca/drugs/DB04946 |
0.011 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | FANAPT Approved UseFANAPT is an atypical antipsychotic indicated for the treatment of schizophrenia in adults. Launch Date1.24148161E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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% |
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
Dose | Population | Adverse 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 Sources: Page: p.17Electrocardiogram QTc interval prolonged |
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... Other AEs: Somnolence (11.9%) Sources: Page: p.9 |
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... Other AEs: Weight gain (18%) Sources: Page: p.7 |
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%) Sources: Page: p.8Galactorrhea (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 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... Other AEs: Syncope (0.4%) 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 n = 1344 Health Status: unhealthy Condition: Schizophrenia Population Size: 1344 Sources: Page: p.7 |
Other AEs: Seizures... Other AEs: Seizures (0.1%) 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: Leukopenia, Neutropenia... Other AEs: Leukopenia Sources: Page: p.7Neutropenia 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.8 |
unhealthy Health Status: unhealthy Condition: Schizophrenia Sources: Page: p.8 |
Other AEs: Temperature regulation disorder, Dysphagia... Other AEs: Temperature regulation disorder Sources: Page: p.8Dysphagia |
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 Sources: Page: p.9Priapism |
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 Sources: Page: p.6Hyperglycemia |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 |
Overview
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
no | |||
Page: 18.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
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; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 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; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022192s018s021lbl.pdf#page=15 Page: 15.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022192s000_PharmR_P1.pdf#page=30 Page: 30.0 |
PubMed
Title | Date | PubMed |
---|---|---|
The ratios of serotonin2 and dopamine2 affinities differentiate atypical and typical antipsychotic drugs. | 1989 |
|
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873). | 1995 Mar 31 |
|
The pharmacological profile of iloperidone, a novel atypical antipsychotic agent. | 1995 Sep |
|
Iloperidone binding to human and rat dopamine and 5-HT receptors. | 1996 Dec 19 |
|
Iloperidone (Hoechst Marion Roussel Inc). | 1999 Jun |
|
Treatments for chronic psychosis. | 2001 Dec |
|
Iloperidone (Novartis). | 2002 Jan |
|
New antipsychotic agents for schizophrenia: pharmacokinetics and metabolism update. | 2002 Jul |
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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 |
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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 |
|
Differential effects of iloperidone, clozapine, and haloperidol on working memory of rats in the delayed non-matching-to-position paradigm. | 2003 Sep |
|
Atypical antipsychotics: pharmacokinetics, therapeutic drug monitoring and pharmacological interactions. | 2004 Feb |
|
Iloperidone reduces sensorimotor gating deficits in pharmacological models, but not a developmental model, of disrupted prepulse inhibition in rats. | 2006 Sep |
|
Efficacy of iloperidone in the treatment of schizophrenia: initial phase 3 studies. | 2008 Apr |
|
Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia. | 2008 Apr |
|
Four-week, double-blind, placebo- and ziprasidone-controlled trial of iloperidone in patients with acute exacerbations of schizophrenia. | 2008 Apr |
|
Safety profile of iloperidone: a pooled analysis of 6-week acute-phase pivotal trials. | 2008 Apr |
|
New advances in the treatment of schizophrenia. Introduction. | 2008 Apr |
|
Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market? | 2008 Jan |
|
Gateways to clinical trials. July-August 2008. | 2008 Jul-Aug |
|
American psychiatric association. | 2008 Jun |
|
Effect of a ciliary neurotrophic factor polymorphism on schizophrenia symptom improvement in an iloperidone clinical trial. | 2008 Mar |
|
Gateways to clinical trials. | 2008 Oct |
|
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 |
|
Genome-wide association studies in pharmacogenomics: untapped potential for translation. | 2009 Apr 28 |
|
Iloperidone for schizophrenia: a review of the efficacy and safety profile for this newly commercialised second-generation antipsychotic. | 2009 Aug |
|
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 |
|
Applicability of a genetic signature for enhanced iloperidone efficacy in the treatment of schizophrenia. | 2009 Jun |
|
Whole genome association study identifies polymorphisms associated with QT prolongation during iloperidone treatment of schizophrenia. | 2009 Nov |
|
Iloperidone: in schizophrenia. | 2009 Oct |
|
Iloperidone for the treatment of schizophrenia. | 2010 Aug |
|
Iloperidone for schizophrenia. | 2010 Aug |
|
A review of new atypical antipsychotic launches in the United States. | 2010 Dec |
|
Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion. | 2010 Dec |
|
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 |
|
Gateways to clinical trials. | 2010 Jan-Feb |
|
New drugs: asenapine, iloperidone, and bepotastine besilate. | 2010 Jan-Feb |
|
Atypical antipsychotic metabolism and excretion. | 2010 Jul |
|
Iloperidone for the treatment of schizophrenia. | 2010 May |
|
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 |
|
New antipsychotic drugs: how do their receptor-binding profiles compare? | 2010 Sep |
|
Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults. | 2013 Jan |
|
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. | 2013 Nov |
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22465688
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
Edited
Fri Dec 16 17:52:53 UTC 2022
by
admin
on
Fri Dec 16 17:52:53 UTC 2022
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Record UNII |
VPO7KJ050N
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Record Status |
Validated (UNII)
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Record Version |
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-
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NDF-RT |
N0000175430
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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LIVERTOX |
NBK548669
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WHO-VATC |
QN05AX14
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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NCI_THESAURUS |
C29710
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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WHO-ATC |
N05AX14
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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Code System | Code | Type | Description | ||
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65173
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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DB04946
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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SUB08135MIG
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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Iloperidone
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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Iloperidone
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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VPO7KJ050N
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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CHEMBL14376
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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7045
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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M6211
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | Merck Index | ||
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C83784
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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DTXSID6049060
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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71360
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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1336249
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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133454-47-4
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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8207
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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73178
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | RxNorm | ||
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C081732
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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EE-25
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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VPO7KJ050N
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY | |||
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3294
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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87
Created by
admin on Fri Dec 16 17:52:53 UTC 2022 , Edited by admin on Fri Dec 16 17:52:53 UTC 2022
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PRIMARY |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
MAJOR
Ki
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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.
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TARGET -> INHIBITOR |
MAJOR
Ki
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
MAJOR
Ki
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Related Record | Type | Details | ||
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METABOLITE -> PARENT | |||
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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
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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.
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METABOLITE -> PARENT |
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METABOLITE -> PARENT | |||
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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.
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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
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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
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
FECAL; URINE
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METABOLITE -> PARENT |
MINOR
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METABOLITE -> PARENT | |||
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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
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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HIGH-FAT MEAL |
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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