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

Details

Stereochemistry ABSOLUTE
Molecular Formula C24H28FN3O
Molecular Weight 393.497
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LUMATEPERONE

SMILES

[H][C@]12CCN(CCCC(=O)C3=CC=C(F)C=C3)C[C@@]1([H])C4=CC=CC5=C4N2CCN5C

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 393.497
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

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.

Originator

Approval Year

2019
334
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 0.54 nM [Ki]
Antagonist
2778
 32.0 nM [Ki]
Inhibitor
8297
 61.0 nM [Ki]
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
19.7 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf
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
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf
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
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf
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%
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/30449883/
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:
https://pubmed.ncbi.nlm.nih.gov/30449883/
Other AEs: Headache, Sedation...
Other AEs:
Headache (grade 1-2, 40%)
Sedation (grade 1, 40%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/30449883/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
Disc. AE: Dry mouth, Schizophrenia aggravated...
AEs leading to
discontinuation/dose reduction:
Dry mouth (0.6%)
Schizophrenia aggravated (0.6%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
Other AEs: Somnolence, Dry mouth...
Other AEs:
Somnolence (32.5%)
Dry mouth (8.4%)
Nausea (4.8%)
Dizziness (8.4%)
Akathisia (2.4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209500s000lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/30449883/
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:
https://pubmed.ncbi.nlm.nih.gov/30449883/
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:
https://pubmed.ncbi.nlm.nih.gov/30449883/
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:
https://pubmed.ncbi.nlm.nih.gov/30449883/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
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:
https://pubmed.ncbi.nlm.nih.gov/31913424/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587

substrate
1737

inducer
781
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2C19
1478

OATP1B1
788

OAT1
599

OAT3
642

OCT2
647
UGT1A1
418

UGT1A4
347

UGT2B15
203

AKR1C1
19

AKR1B10
2

AKR1C4
6

CYP2C8
693

CYP1A2
1054

P-gp
1537

BCRP
561
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OAT1
603
 no
OAT1
603
 no
IC200131
2
OAT3
644
 no
OAT3
644
 no
IC200131
2
OATP1B1
803
 no
OATP1B1
803
 no
IC200131
2
OCT2
648
 no
OCT2
648
 no
IC200131
2
CYP1A2
1692
 yes
CYP1A2
1692
 yes
CYP2B6
1001
 yes
CYP2C19
1553
 yes
CYP2C9
1819
 yes
CYP2D6
1891
 yes
CYP3A4
1925
 yes
CYP3A4
1925
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
561
 no
P-gp
1537
 no
AKR1B10
2
 yes
AKR1C1
19
 yes
AKR1C4
6
 yes
CYP1A2
1054
 yes
CYP2C8
693
 yes
UGT1A1
418
 yes
UGT1A4
347
 yes
UGT2B15
203
 yes
CYP3A4
1737
 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
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA00I5U2
https://www.aablocks.com/goods/Goods/detail?id=AA00I5U2
Ambinter
Amb24183497
http://www.ambinter.com/reference/24183497
Angel Pharmatech
AG-15617
http://www.angelpharmatech.com/313368-91-1.html
Angene
AGN-PC-0WAMBU
http://www.angenechemical.com/productshow/AGN-PC-0WAMBU.html
Ark Pharm
AK173827
http://www.arkpharminc.com/products/313368-91-1.html
BOC Sciences
313368-91-1
https://www.bocsci.com/product/lumateperone-cas-313368-91-1-470913.html
BioChemPartner
BCP24038
http://www.biochempartner.com/313368-91-1-BCP24038
Chemspace
CSSB00016994610
https://chem-space.com/CSSB00016994610
DC Chemicals
DC22906
http://www.dcchemicals.com/product_show-DC22906.html
Excenen
EX-A3605
https://www.excenen.com/searchresultlist.php?id=EX-A3605
Hairui
LUJB004
http://www.hairuichem.com/en/product/313368-91-1.html
Lab Network
LN03247748
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN03247748
Smolecule
S531028
http://www.smolecule.com/products/s531028
Synblock Inc
SB17147
http://www.synblock.com/product/313368-91-1.html
THE BioTek
bt-270151
https://www.thebiotek.com/product/inhibitors/bt-270151
abcr GmbH
AB464020
http://www.abcr.de/shop/en/AB464020
eNovation Chemicals
D572903
http://www.enovationchem.com/productDetails.asp?productID=D572903
PubMed

PubMed

TitleDatePubMed
Dopamine D(2) receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia.
2019 Feb
Patents

Patents

6713471
2
Substance Class Chemical
Created
by admin
on Sat Dec 16 10:38:56 GMT 2023
Edited
by admin
on Sat Dec 16 10:38:56 GMT 2023
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
Lumateperone [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)-
Systematic Name English
LUMATEPERONE [USAN]
Common Name English
ITI-722
Code English
ITI-007
Code English
LUMATEPERONE [MI]
Common Name English
Code System Code Type Description
EPA CompTox
DTXSID401026211
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
USAN
DE-107
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
ChEMBL
CHEMBL3545045
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
CAS
313368-91-1
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
DRUG CENTRAL
5358
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
MERCK INDEX
m12238
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
INN
10156
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
DRUG BANK
DB06077
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
RXCUI
2275602
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
NCI_THESAURUS
C166975
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
WIKIPEDIA
LUMATEPERONE
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
FDA UNII
70BSQ12069
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
PRIMARY
SMS_ID
300000025855
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
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DAILYMED
70BSQ12069
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
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PUBCHEM
21302490
Created by admin on Sat Dec 16 10:38:57 GMT 2023 , Edited by admin on Sat Dec 16 10:38:57 GMT 2023
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Related Record Type Details
CYTOCHROME P450 1A2
METABOLIC ENZYME -> SUBSTRATE
Structure of LUMATEPERONE
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A1
METABOLIC ENZYME -> SUBSTRATE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
Protein binding of lumateperone is 97.4% at 5 μM (about 70-fold higher than therapeutic concentrations) in human plasma.
BINDING
5-HYDROXYTRYPTAMINE RECEPTOR 2A
TARGET->ANTAGONIST
BINDING
Ki
CYTOCHROME P450 2C8
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A4
METABOLIC ENZYME -> SUBSTRATE
SODIUM-DEPENDENT SEROTONIN TRANSPORTER
TARGET->ANTAGONIST
Ki
D(2) DOPAMINE RECEPTOR
TARGET->ANTAGONIST
BINDING
Ki
Structure of LUMATEPERONE TOSYLATE
SALT/SOLVATE -> PARENT
D(1A) DOPAMINE RECEPTOR
TARGET->ANTAGONIST
BINDING
Ki
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 2B15
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
Structure of (6BR,10AS)-.ALPHA.-(4-FLUOROPHENYL)-2,3,6B,9,10,10A-HEXAHYDRO-3-METHYL-1H-PYRIDO(3',4':4,5)PYRROLO(1,2,3-DE)QUINOXALINE-8(7H)-BUTANOL
METABOLITE -> PARENT
Structure of (6BR,10AS)-8-(4-(4-FLUOROPHENYL)-4-HYDROXYBUTYL)-6B,7,8,9,10,10A-HEXAHYDRO-1H-PYRIDO(3',4':4,5)PYRROLO(1,2,3-DE)QUINOXALIN-2(3H)-ONE
METABOLITE -> PARENT
Structure of 1H-PYRIDO(3',4':4,5)PYRROLO(1,2,3-DE)QUINOXALINE-8(7H)-BUTANOL, .ALPHA.-(4-FLUOROPHENYL)-2,3,6B,9,10,10A-HEXAHYDRO-, (6BR,10AS)-
METABOLITE -> PARENT
Structure of (6BR,10AS)-8-(4-(4-FLUOROPHENYL)-4-OXOBUTYL)-6B,7,8,9,10,10A-HEXAHYDRO-1H-PYRIDO(3',4':4,5)PYRROLO(1,2,3-DE)QUINOXALIN-2(3H)-ONE
METABOLITE -> PARENT
Related Record Type Details
Structure of LUMATEPERONE
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

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