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

Details

Stereochemistry ACHIRAL
Molecular Formula C24H27FN2O4
Molecular Weight 426.4815
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

Description
Curator's Comment:: 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 nM [IC50]
0.400000000000000022 nM [IC50]
210 nM [IC50]
0.400000000000000022 nM [IC50]
161 nM [IC50]
0.0109999999999999994 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

1241481600000
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
experiment_type: multiple
dose_type: MTD
co-adm with
    data_source:
    https://onlinelibrary.wiley.com/doi/epdf/10.1111/j.1527-3458.1997.tb00320.x
    https://pubmed.ncbi.nlm.nih.gov/20368905
    unhealthy, 18 - 55
    24 mg 1 times / day multiple, oral
    Highest studied dose
    dose: 24 mg 1 times / day
    route: oral
    experiment_type: multiple
    dose_type: Highest studied dose
    co-adm with
      data_source:
      https://pubmed.ncbi.nlm.nih.gov/28817490
      unhealthy, 42 (13.1)
      population: unhealthy
      age: 42 (13.1)
      sex: M+F
      food_status:
      n:
      data_source:
      https://pubmed.ncbi.nlm.nih.gov/28817490
      438 mg multiple, oral
      Overdose
      dose: 438 mg
      route: oral
      experiment_type: multiple
      dose_type: Overdose
      co-adm with
        data_source:
        https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
        unhealthy
        population: unhealthy
        age:
        sex:
        food_status:
        n:
        data_source:
        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

        data_source:
        https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
        576 mg single, oral
        Overdose
        dose: 576 mg
        route: oral
        experiment_type: single
        dose_type: Overdose
        co-adm with
          data_source:
          https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
          unhealthy
          population: unhealthy
          age:
          sex:
          food_status:
          n:
          data_source:
          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
          experiment_type: multiple
          dose_type: Recommended
          co-adm with
            data_source:
            https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
            unhealthy
            population: unhealthy
            age:
            sex:
            food_status:
            n:
            data_source:
            https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
            Other AEs: Somnolence...
            12 mg 2 times / day multiple, oral
            Recommended
            dose: 12 mg 2 times / day
            route: oral
            experiment_type: multiple
            dose_type: Recommended
            co-adm with
              data_source:
              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
              unhealthy
              population: unhealthy
              age:
              sex:
              food_status:
              n:
              data_source:
              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
              Other AEs: Neuroleptic malignant syndrome...
              Other AEs:
              Neuroleptic malignant syndrome

              data_source:
              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
              experiment_type: multiple
              dose_type: Recommended
              co-adm with
                data_source:
                https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                unhealthy
                population: unhealthy
                age:
                sex:
                food_status:
                n:
                data_source:
                https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                Other AEs: QT interval prolonged...
                12 mg 2 times / day multiple, oral
                Recommended
                dose: 12 mg 2 times / day
                route: oral
                experiment_type: multiple
                dose_type: Recommended
                co-adm with
                  data_source:
                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                  unhealthy
                  population: unhealthy
                  age:
                  sex:
                  food_status:
                  n:
                  data_source:
                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                  Other AEs: Tardive dyskinesia, Hyperglycemia...
                  Other AEs:
                  Tardive dyskinesia
                  Hyperglycemia

                  data_source:
                  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
                  experiment_type: multiple
                  dose_type: Recommended
                  co-adm with
                    data_source:
                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                    unhealthy
                    population: unhealthy
                    age:
                    sex:
                    food_status:
                    n:
                    data_source:
                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                    Other AEs: Weight gain...
                    12 mg 2 times / day multiple, oral
                    Recommended
                    dose: 12 mg 2 times / day
                    route: oral
                    experiment_type: multiple
                    dose_type: Recommended
                    co-adm with
                      data_source:
                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                      unhealthy
                      population: unhealthy
                      age:
                      sex:
                      food_status:
                      n:
                      data_source:
                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                      Other AEs: Orthostatic hypotension...
                      Other AEs:
                      Orthostatic hypotension (5%)

                      data_source:
                      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
                      experiment_type: multiple
                      dose_type: Recommended
                      co-adm with
                        data_source:
                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                        unhealthy
                        population: unhealthy
                        age:
                        sex:
                        food_status:
                        n:
                        data_source:
                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                        Other AEs: Gynecomastia, Galactorrhea...
                        Other AEs:
                        Gynecomastia (0.1%)
                        Galactorrhea (0.2%)

                        data_source:
                        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
                        experiment_type: multiple
                        dose_type: Recommended
                        co-adm with
                          data_source:
                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                          unhealthy
                          population: unhealthy
                          age:
                          sex:
                          food_status:
                          n:
                          data_source:
                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                          Other AEs: Hyperprolactinemia...
                          12 mg 2 times / day multiple, oral
                          Recommended
                          dose: 12 mg 2 times / day
                          route: oral
                          experiment_type: multiple
                          dose_type: Recommended
                          co-adm with
                            data_source:
                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                            unhealthy
                            population: unhealthy
                            age:
                            sex:
                            food_status:
                            n:
                            data_source:
                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                            Other AEs: Syncope...
                            12 mg 2 times / day multiple, oral
                            Recommended
                            dose: 12 mg 2 times / day
                            route: oral
                            experiment_type: multiple
                            dose_type: Recommended
                            co-adm with
                              data_source:
                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                              unhealthy
                              population: unhealthy
                              age:
                              sex:
                              food_status:
                              n:
                              data_source:
                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                              Other AEs: Seizures...
                              12 mg 2 times / day multiple, oral
                              Recommended
                              dose: 12 mg 2 times / day
                              route: oral
                              experiment_type: multiple
                              dose_type: Recommended
                              co-adm with
                                data_source:
                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                unhealthy
                                population: unhealthy
                                age:
                                sex:
                                food_status:
                                n:
                                data_source:
                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                Other AEs: Leukopenia, Neutropenia...
                                Other AEs:
                                Leukopenia
                                Neutropenia
                                Agranulocytosis

                                data_source:
                                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
                                experiment_type: multiple
                                dose_type: Recommended
                                co-adm with
                                  data_source:
                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                  unhealthy
                                  population: unhealthy
                                  age:
                                  sex:
                                  food_status:
                                  n:
                                  data_source:
                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                  Other AEs: Suicide attempt, Priapism...
                                  12 mg 2 times / day multiple, oral
                                  Recommended
                                  dose: 12 mg 2 times / day
                                  route: oral
                                  experiment_type: multiple
                                  dose_type: Recommended
                                  co-adm with
                                    data_source:
                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                    unhealthy
                                    population: unhealthy
                                    age:
                                    sex:
                                    food_status:
                                    n:
                                    data_source:
                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                    Other AEs: Temperature regulation disorder, Dysphagia...
                                    Other AEs:
                                    Temperature regulation disorder
                                    Dysphagia

                                    data_source:
                                    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
                                    experiment_type: multiple
                                    dose_type: Overdose
                                    co-adm with
                                      data_source:
                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                      unhealthy
                                      population:
                                      age:
                                      sex:
                                      food_status:
                                      n:
                                      data_source:
                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                      Extrapyramidal symptoms
                                      438 mg multiple, oral
                                      Overdose
                                      dose: 438 mg
                                      route: oral
                                      experiment_type: multiple
                                      dose_type: Overdose
                                      co-adm with
                                        data_source:
                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                        unhealthy
                                        population:
                                        age:
                                        sex:
                                        food_status:
                                        n:
                                        data_source:
                                        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
                                        experiment_type: multiple
                                        dose_type: Recommended
                                        co-adm with
                                          data_source:
                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                          unhealthy
                                          population:
                                          age:
                                          sex:
                                          food_status:
                                          n:
                                          data_source:
                                          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
                                          experiment_type: multiple
                                          dose_type: Recommended
                                          co-adm with
                                            data_source:
                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                            unhealthy
                                            population:
                                            age:
                                            sex:
                                            food_status:
                                            n:
                                            data_source:
                                            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
                                            experiment_type: multiple
                                            dose_type: Recommended
                                            co-adm with
                                              data_source:
                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                              unhealthy
                                              population:
                                              age:
                                              sex:
                                              food_status:
                                              n:
                                              data_source:
                                              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
                                              experiment_type: multiple
                                              dose_type: Recommended
                                              co-adm with
                                                data_source:
                                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                unhealthy
                                                population:
                                                age:
                                                sex:
                                                food_status:
                                                n:
                                                data_source:
                                                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
                                                experiment_type: multiple
                                                dose_type: Recommended
                                                co-adm with
                                                  data_source:
                                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                  unhealthy
                                                  population:
                                                  age:
                                                  sex:
                                                  food_status:
                                                  n:
                                                  data_source:
                                                  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
                                                  experiment_type: multiple
                                                  dose_type: Recommended
                                                  co-adm with
                                                    data_source:
                                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                    unhealthy
                                                    population:
                                                    age:
                                                    sex:
                                                    food_status:
                                                    n:
                                                    data_source:
                                                    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
                                                    experiment_type: multiple
                                                    dose_type: Recommended
                                                    co-adm with
                                                      data_source:
                                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                      unhealthy
                                                      population:
                                                      age:
                                                      sex:
                                                      food_status:
                                                      n:
                                                      data_source:
                                                      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
                                                      experiment_type: multiple
                                                      dose_type: Recommended
                                                      co-adm with
                                                        data_source:
                                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                        unhealthy
                                                        population:
                                                        age:
                                                        sex:
                                                        food_status:
                                                        n:
                                                        data_source:
                                                        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
                                                        experiment_type: multiple
                                                        dose_type: Recommended
                                                        co-adm with
                                                          data_source:
                                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                          unhealthy
                                                          population:
                                                          age:
                                                          sex:
                                                          food_status:
                                                          n:
                                                          data_source:
                                                          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
                                                          experiment_type: multiple
                                                          dose_type: Recommended
                                                          co-adm with
                                                            data_source:
                                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                            unhealthy
                                                            population:
                                                            age:
                                                            sex:
                                                            food_status:
                                                            n:
                                                            data_source:
                                                            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
                                                            experiment_type: multiple
                                                            dose_type: Recommended
                                                            co-adm with
                                                              data_source:
                                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                              unhealthy
                                                              population:
                                                              age:
                                                              sex:
                                                              food_status:
                                                              n:
                                                              data_source:
                                                              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
                                                              experiment_type: multiple
                                                              dose_type: Recommended
                                                              co-adm with
                                                                data_source:
                                                                https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                unhealthy
                                                                population:
                                                                age:
                                                                sex:
                                                                food_status:
                                                                n:
                                                                data_source:
                                                                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
                                                                experiment_type: multiple
                                                                dose_type: Recommended
                                                                co-adm with
                                                                  data_source:
                                                                  https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                  unhealthy
                                                                  population:
                                                                  age:
                                                                  sex:
                                                                  food_status:
                                                                  n:
                                                                  data_source:
                                                                  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
                                                                  experiment_type: multiple
                                                                  dose_type: Recommended
                                                                  co-adm with
                                                                    data_source:
                                                                    https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                    unhealthy
                                                                    population:
                                                                    age:
                                                                    sex:
                                                                    food_status:
                                                                    n:
                                                                    data_source:
                                                                    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
                                                                    experiment_type: multiple
                                                                    dose_type: Recommended
                                                                    co-adm with
                                                                      data_source:
                                                                      https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                      unhealthy
                                                                      population:
                                                                      age:
                                                                      sex:
                                                                      food_status:
                                                                      n:
                                                                      data_source:
                                                                      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
                                                                      experiment_type: multiple
                                                                      dose_type: Recommended
                                                                      co-adm with
                                                                        data_source:
                                                                        https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                        unhealthy
                                                                        population:
                                                                        age:
                                                                        sex:
                                                                        food_status:
                                                                        n:
                                                                        data_source:
                                                                        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
                                                                        experiment_type: multiple
                                                                        dose_type: Recommended
                                                                        co-adm with
                                                                          data_source:
                                                                          https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                          unhealthy
                                                                          population:
                                                                          age:
                                                                          sex:
                                                                          food_status:
                                                                          n:
                                                                          data_source:
                                                                          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
                                                                          experiment_type: multiple
                                                                          dose_type: Recommended
                                                                          co-adm with
                                                                            data_source:
                                                                            https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                            unhealthy
                                                                            population:
                                                                            age:
                                                                            sex:
                                                                            food_status:
                                                                            n:
                                                                            data_source:
                                                                            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
                                                                            experiment_type: multiple
                                                                            dose_type: Recommended
                                                                            co-adm with
                                                                              data_source:
                                                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                              unhealthy
                                                                              population:
                                                                              age:
                                                                              sex:
                                                                              food_status:
                                                                              n:
                                                                              data_source:
                                                                              https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022192lbl.pdf
                                                                              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
                                                                              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
                                                                              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
                                                                              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
                                                                              Tox targets

                                                                              Tox targets

                                                                              PubMed

                                                                              PubMed

                                                                              TitleDatePubMed
                                                                              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
                                                                              Gateways to clinical trials.
                                                                              2002 Nov
                                                                              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
                                                                              Upcoming agents for the treatment of schizophrenia: mechanism of action, efficacy and tolerability.
                                                                              2008
                                                                              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
                                                                              Pharmacogenomics: the promise of personalized medicine for CNS disorders.
                                                                              2009 Jan
                                                                              Applicability of a genetic signature for enhanced iloperidone efficacy in the treatment of schizophrenia.
                                                                              2009 Jun
                                                                              Akathisia and second-generation antipsychotic drugs.
                                                                              2009 May
                                                                              Whole genome association study identifies polymorphisms associated with QT prolongation during iloperidone treatment of schizophrenia.
                                                                              2009 Nov
                                                                              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
                                                                              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
                                                                              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.
                                                                              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