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Details

Stereochemistry ABSOLUTE
Molecular Formula C24H28FN3O
Molecular Weight 393.4979
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LUMATEPERONE

SMILES

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

InChI

InChIKey=HOIIHACBCFLJET-SFTDATJTSA-N
InChI=1S/C24H28FN3O/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/h2,4-5,7-10,20-21H,3,6,11-16H2,1H3/t20-,21-/m0/s1

HIDE SMILES / InChI

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
0.540000000000000036 nM [Ki]
32 nM [Ki]
61 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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 26 to 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: steady
Dose: 90 mg, 1 times / day
Sources:
unhealthy, mean 39.7 years
Health Status: unhealthy
Age Group: mean 39.7 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 26 to 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 26 to 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
Sources:
Dry mouth 0.6%
Disc. AE
90 mg 1 times / day steady, oral
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: steady
Dose: 90 mg, 1 times / day
Sources:
unhealthy, mean 39.7 years
Health Status: unhealthy
Age Group: mean 39.7 years
Sex: M+F
Sources:
Schizophrenia aggravated 0.6%
Disc. AE
90 mg 1 times / day steady, oral
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: steady
Dose: 90 mg, 1 times / day
Sources:
unhealthy, mean 39.7 years
Health Status: unhealthy
Age Group: mean 39.7 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Tox targets

Tox targets

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 11:45:59 UTC 2021
Edited
by admin
on Sat Jun 26 11:45:59 UTC 2021
Record UNII
70BSQ12069
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LUMATEPERONE
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
LUMATEPERONE [INN]
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)-
Systematic Name English
LUMATEPERONE [USAN]
Common Name English
ITI-722
Code English
LUMATEPERONE [WHO-DD]
Common Name English
ITI-007
Code English
Code System Code Type Description
ChEMBL
CHEMBL3545045
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
CAS
313368-91-1
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
DRUG CENTRAL
5358
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
INN
10156
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
DRUG BANK
DB06077
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
RXCUI
2275602
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
NCI_THESAURUS
C166975
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
WIKIPEDIA
LUMATEPERONE
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
FDA UNII
70BSQ12069
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
PUBCHEM
21302490
Created by admin on Sat Jun 26 11:45:59 UTC 2021 , Edited by admin on Sat Jun 26 11:45:59 UTC 2021
PRIMARY
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
Protein binding of lumateperone is 97.4% at 5 ?M (about 70-fold higher than therapeutic concentrations) in human plasma.
BINDING
TARGET->ANTAGONIST
BINDING
Ki
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TARGET->ANTAGONIST
Ki
TARGET->ANTAGONIST
BINDING
Ki
SALT/SOLVATE -> PARENT
TARGET->ANTAGONIST
BINDING
Ki
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
ORAL BIOAVAILABILITY PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

Biological Half-life PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

Tmax PHARMACOKINETIC ONCE DAILY

ORAL ADMINISTRATION