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Details

Stereochemistry ABSOLUTE
Molecular Formula C24H28FN3O.C7H8O3S
Molecular Weight 565.7009
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LUMATEPERONE TOSYLATE

SMILES

CN1CCN2[C@@]3([H])CCN(CCCC(=O)c4ccc(cc4)F)C[C@@]3([H])c5cccc1c52.Cc1ccc(cc1)S(=O)(=O)O

InChI

InChIKey=LHAPOGAFBLSJJQ-GUTACTQSSA-N
InChI=1S/C24H28FN3O.C7H8O3S/c1-26-14-15-28-21-11-13-27(16-20(21)19-4-2-5-22(26)24(19)28)12-3-6-23(29)17-7-9-18(25)10-8-17;1-6-2-4-7(5-3-6)11(8,9)10/h2,4-5,7-10,20-21H,3,6,11-16H2,1H3;2-5H,1H3,(H,8,9,10)/t20-,21-;/m0./s1

HIDE SMILES / InChI

Molecular Formula C7H8O3S
Molecular Weight 172.203
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C24H28FN3O
Molecular Weight 393.4979
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Lumateperone (ITI-722/ITI-007) is a dual 5HT2A receptor antagonist/dopamine phosphoprotein modulator (DPPM) for the treatment of schizophrenia. It is an orally available compound which combines potent 5HT2A receptor antagonism with cell-type-specific modulation of phosphoprotein pathways downstream of dopamine receptors. Lumateperone was developed by Intra-Cellular Therapies, Inc., and is being evaluated for the treatment of schizophrenia and bipolar depression. In 3 efficacy studies in patients with acute schizophrenia, lumateperone was well-tolerated with a favorable safety profile, and in 2 studies of 3 demonstrated significantly superior efficacy over placebo.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.54 nM [Ki]
32.0 nM [Ki]
61.0 nM [Ki]
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
19.7 ng/mL
42 mg 1 times / day steady-state, oral
dose: 42 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUMATEPERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
64.2 ng × h/mL
42 mg 1 times / day steady-state, oral
dose: 42 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUMATEPERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.1 h
42 mg 1 times / day steady-state, oral
dose: 42 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUMATEPERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
4.4%
42 mg 1 times / day steady-state, oral
dose: 42 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUMATEPERONE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Other AEs: Somnolence, Nausea...
Other AEs:
Somnolence (24%)
Nausea (9%)
Dry mouth (6%)
Dizziness (5%)
Creatine phosphokinase increased (4%)
Fatigue (3%)
Vomiting (3%)
Transaminases increased (2%)
Decreased appetite (2%)
Spasm of muscle
Swallowing difficult
Difficulty breathing
Protrusion tongue
Extrapyramidal symptoms (6.7%)
Akathisia
Extrapyramidal disorder
Muscle spasms
Restlessness
Musculoskeletal stiffness
Dyskinesia
Dystonia
Muscle twitching
Tardive dyskinesia
Tremor
Drooling
Muscle contractions involuntary
Sources:
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 26 to 57 years
n = 10
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 26 to 57 years
Sex: M+F
Population Size: 10
Sources:
Other AEs: Headache, Sedation...
Other AEs:
Headache (grade 1-2, 40%)
Sedation (grade 1, 40%)
Sources:
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, mean 38.3 years
n = 84
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 38.3 years
Sex: M+F
Population Size: 84
Sources:
Other AEs: Somnolence, Dry mouth...
Other AEs:
Somnolence (16.7%)
Dry mouth (4.8%)
Nausea (6%)
Dizziness (4.8%)
Akathisia (1.2%)
Tachycardia (1.2%)
Sources:
90 mg 1 times / day steady, oral (mean)
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: steady
Dose: 90 mg, 1 times / day
Sources:
unhealthy, mean 39.7 years
n = 167
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 39.7 years
Sex: M+F
Population Size: 167
Sources:
Disc. AE: Dry mouth, Schizophrenia aggravated...
AEs leading to
discontinuation/dose reduction:
Dry mouth (0.6%)
Schizophrenia aggravated (0.6%)
Sources:
120 mg 1 times / day steady, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, mean 41.1 years
n = 83
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 41.1 years
Sex: M+F
Population Size: 83
Sources:
Other AEs: Somnolence, Dry mouth...
Other AEs:
Somnolence (32.5%)
Dry mouth (8.4%)
Nausea (4.8%)
Dizziness (8.4%)
Akathisia (2.4%)
Sources:
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Disc. AE: Headache, Orthostatic hypotension...
Other AEs: Headache, Somnolence...
AEs leading to
discontinuation/dose reduction:
Headache (1.3%)
Orthostatic hypotension (grade 3, 0.7%)
Other AEs:
Headache (grade 1-2, 19.3%)
Somnolence (grade 1-2, 17.3%)
Sedation (grade 1-2, 12.7%)
Nausea (grade 1-2, 10.7%)
Dry mouth (grade 1-2, 7.3%)
Dizziness (grade 1-2, 6.7%)
Constipation (grade 1-2, 6.7%)
Fatigue (grade 1-2, 5.3%)
Sources:
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Disc. AE: Convulsions...
Other AEs: Akathisia, Headache...
AEs leading to
discontinuation/dose reduction:
Convulsions (grade 3, 0.7%)
Other AEs:
Akathisia (grade 1-2, 4%)
Headache (grade 1-2, 16%)
Somnolence (grade 1-2, 11.3%)
Sedation (grade 1-2, 9.3%)
Nausea (grade 1-2, 4.7%)
Dry mouth (grade 1-2, 6%)
Dizziness (grade 1-2, 4.7%)
Constipation (grade 1-2, 4%)
Fatigue (grade 1-2, 4.7%)
Akathisia (grade 1-2, 1.3%)
Dyskinesia (grade 1-2, 1.3%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Akathisia
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Difficulty breathing
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Drooling
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Dyskinesia
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Dystonia
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Extrapyramidal disorder
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Muscle contractions involuntary
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Muscle spasms
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Muscle twitching
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Musculoskeletal stiffness
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Protrusion tongue
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Restlessness
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Spasm of muscle
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Swallowing difficult
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Tardive dyskinesia
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Tremor
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Decreased appetite 2%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Transaminases increased 2%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Somnolence 24%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Fatigue 3%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Vomiting 3%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Creatine phosphokinase increased 4%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Dizziness 5%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Dry mouth 6%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Extrapyramidal symptoms 6.7%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Nausea 9%
42 mg 1 times / day steady, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: steady
Dose: 42 mg, 1 times / day
Sources:
unhealthy, 19 to 60 years
n = 406
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 19 to 60 years
Sex: M+F
Population Size: 406
Sources:
Sedation grade 1, 40%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 26 to 57 years
n = 10
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 26 to 57 years
Sex: M+F
Population Size: 10
Sources:
Headache grade 1-2, 40%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, 26 to 57 years
n = 10
Health Status: unhealthy
Condition: Schizophrenia
Age Group: 26 to 57 years
Sex: M+F
Population Size: 10
Sources:
Akathisia 1.2%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, mean 38.3 years
n = 84
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 38.3 years
Sex: M+F
Population Size: 84
Sources:
Tachycardia 1.2%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, mean 38.3 years
n = 84
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 38.3 years
Sex: M+F
Population Size: 84
Sources:
Somnolence 16.7%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, mean 38.3 years
n = 84
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 38.3 years
Sex: M+F
Population Size: 84
Sources:
Dizziness 4.8%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, mean 38.3 years
n = 84
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 38.3 years
Sex: M+F
Population Size: 84
Sources:
Dry mouth 4.8%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, mean 38.3 years
n = 84
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 38.3 years
Sex: M+F
Population Size: 84
Sources:
Nausea 6%
60 mg 1 times / day steady, oral
Studied dose
Dose: 60 mg, 1 times / day
Route: oral
Route: steady
Dose: 60 mg, 1 times / day
Sources:
unhealthy, mean 38.3 years
n = 84
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 38.3 years
Sex: M+F
Population Size: 84
Sources:
Dry mouth 0.6%
Disc. AE
90 mg 1 times / day steady, oral (mean)
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: steady
Dose: 90 mg, 1 times / day
Sources:
unhealthy, mean 39.7 years
n = 167
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 39.7 years
Sex: M+F
Population Size: 167
Sources:
Schizophrenia aggravated 0.6%
Disc. AE
90 mg 1 times / day steady, oral (mean)
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: steady
Dose: 90 mg, 1 times / day
Sources:
unhealthy, mean 39.7 years
n = 167
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 39.7 years
Sex: M+F
Population Size: 167
Sources:
Akathisia 2.4%
120 mg 1 times / day steady, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, mean 41.1 years
n = 83
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 41.1 years
Sex: M+F
Population Size: 83
Sources:
Somnolence 32.5%
120 mg 1 times / day steady, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, mean 41.1 years
n = 83
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 41.1 years
Sex: M+F
Population Size: 83
Sources:
Nausea 4.8%
120 mg 1 times / day steady, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, mean 41.1 years
n = 83
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 41.1 years
Sex: M+F
Population Size: 83
Sources:
Dizziness 8.4%
120 mg 1 times / day steady, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, mean 41.1 years
n = 83
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 41.1 years
Sex: M+F
Population Size: 83
Sources:
Dry mouth 8.4%
120 mg 1 times / day steady, oral
Highest studied dose
Dose: 120 mg, 1 times / day
Route: oral
Route: steady
Dose: 120 mg, 1 times / day
Sources:
unhealthy, mean 41.1 years
n = 83
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 41.1 years
Sex: M+F
Population Size: 83
Sources:
Headache 1.3%
Disc. AE
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Nausea grade 1-2, 10.7%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Sedation grade 1-2, 12.7%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Somnolence grade 1-2, 17.3%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Headache grade 1-2, 19.3%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Fatigue grade 1-2, 5.3%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Constipation grade 1-2, 6.7%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Dizziness grade 1-2, 6.7%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Dry mouth grade 1-2, 7.3%
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Orthostatic hypotension grade 3, 0.7%
Disc. AE
42 mg 1 times / day multiple, oral
Recommended
Dose: 42 mg, 1 times / day
Route: oral
Route: multiple
Dose: 42 mg, 1 times / day
Sources:
unhealthy, mean 42.4 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 42.4 years
Sex: M+F
Population Size: 150
Sources:
Akathisia grade 1-2, 1.3%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Dyskinesia grade 1-2, 1.3%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Somnolence grade 1-2, 11.3%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Headache grade 1-2, 16%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Akathisia grade 1-2, 4%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Constipation grade 1-2, 4%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Dizziness grade 1-2, 4.7%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Fatigue grade 1-2, 4.7%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Nausea grade 1-2, 4.7%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Dry mouth grade 1-2, 6%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Sedation grade 1-2, 9.3%
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
Convulsions grade 3, 0.7%
Disc. AE
28 mg 1 times / day multiple, oral
Studied dose
Dose: 28 mg, 1 times / day
Route: oral
Route: multiple
Dose: 28 mg, 1 times / day
Sources:
unhealthy, mean 43.5 years
n = 150
Health Status: unhealthy
Condition: Schizophrenia
Age Group: mean 43.5 years
Sex: M+F
Population Size: 150
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
yes
yes
yes
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: Coadministration of lumateperone 14 mg with itraconazole 200 mg (strong CYP3A4 inhibitor) increased lumateperone exposure approximately 4-fold in patients with schizophrenia.
Page: 127.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Dopamine D2 receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia.
2019 Feb
Patents

Patents

Substance Class Chemical
Created
by admin
on Sat Jun 26 09:00:26 UTC 2021
Edited
by admin
on Sat Jun 26 09:00:26 UTC 2021
Record UNII
JIE88N006O
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LUMATEPERONE TOSYLATE
USAN  
USAN  
Official Name English
LUMATEPERONE TOSYLATE [WHO-DD]
Common Name English
1-BUTANONE, 1-(4-FLUOROPHENYL)-4-((6BR,10AS)-2,3,6B,9,10,10A-HEXAHYDRO-3-METHYL-1H-PYRIDO(3',4':4,5)PYRROLO(1,2,3-DE)QUINOXALIN-8(7H)-YL)-, 4-METHYLBENZENESULFONATE (1:1)
Systematic Name English
1-(4-FLUOROPHENYL)-4-((6BR,10AS)-3-METHYL-2,3,6B,9,10,10A-HEXAHYDRO-1H-PYRIDO(3',4':4,5)PYRROLO(1,2,3-DE)QUINOXALIN-8(7H)-YL)BUTAN-1-ONE 4-METHYLBENZENESULFONATE (1:1)
Systematic Name English
CAPLYTA
Brand Name English
ITI-007 TOSYLATE
Code English
LUMATEPERONE TOSYLATE [USAN]
Common Name English
Code System Code Type Description
RXCUI
2275731
Created by admin on Sat Jun 26 09:00:26 UTC 2021 , Edited by admin on Sat Jun 26 09:00:26 UTC 2021
PRIMARY
PUBCHEM
44241743
Created by admin on Sat Jun 26 09:00:26 UTC 2021 , Edited by admin on Sat Jun 26 09:00:26 UTC 2021
PRIMARY
CAS
1187020-80-9
Created by admin on Sat Jun 26 09:00:26 UTC 2021 , Edited by admin on Sat Jun 26 09:00:26 UTC 2021
PRIMARY
NCI_THESAURUS
C170138
Created by admin on Sat Jun 26 09:00:26 UTC 2021 , Edited by admin on Sat Jun 26 09:00:26 UTC 2021
PRIMARY
DRUG BANK
DBSALT001873
Created by admin on Sat Jun 26 09:00:26 UTC 2021 , Edited by admin on Sat Jun 26 09:00:26 UTC 2021
PRIMARY
FDA UNII
JIE88N006O
Created by admin on Sat Jun 26 09:00:26 UTC 2021 , Edited by admin on Sat Jun 26 09:00:26 UTC 2021
PRIMARY
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PARENT -> SALT/SOLVATE
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