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

CN1CCN2[C@H]3CCN(CCCC(=O)C4=CC=C(F)C=C4)C[C@H]3C5=C2C1=CC=C5

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
2849
 0.54 nM [Ki]
Antagonist
2849
 32.0 nM [Ki]
Inhibitor
8504
 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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 26 to 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
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
Health Status: unhealthy
Age Group: mean 39.7 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 19 to 60 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 26 to 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 26 to 57 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 38.3 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
unhealthy, mean 39.7 years
Health Status: unhealthy
Age Group: mean 39.7 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/26444072/
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:
https://pubmed.ncbi.nlm.nih.gov/26444072/
unhealthy, mean 39.7 years
Health Status: unhealthy
Age Group: mean 39.7 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 41.1 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 42.4 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
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
Health Status: unhealthy
Age Group: mean 43.5 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31913424/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
2252

substrate
1946

inducer
1087
inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2C19
2057

OATP1B1
1079

OAT1
725

OAT3
747

OCT2
779
UGT1A1
479

UGT1A4
399

UGT2B15
236

AKR1C1
22

AKR1B10
2

AKR1C4
7

CYP2C8
810

CYP1A2
1197

P-gp
2052

BCRP
697
CYP1A2
832

CYP2B6
669
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OAT1
730
 no
OAT1
730
 no
IC200131
2
OAT3
749
 no
OAT3
749
 no
IC200131
2
OATP1B1
1095
 no
OATP1B1
1095
 no
IC200131
2
OCT2
782
 no
OCT2
782
 no
IC200131
2
CYP1A2
2333
 yes
CYP1A2
2333
 yes
CYP2B6
1160
 yes
CYP2C19
2141
 yes
CYP2C9
2497
 yes
CYP2D6
2546
 yes
CYP3A4
2633
 yes
CYP3A4
2633
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
697
 no
P-gp
2052
 no
AKR1B10
2
 yes
AKR1C1
22
 yes
AKR1C4
7
 yes
CYP1A2
1197
 yes
CYP2C8
810
 yes
UGT1A1
479
 yes
UGT1A4
399
 yes
UGT2B15
236
 yes
CYP3A4
1946
 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
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA00I5U2
https://www.aablocks.com/goods/Goods/detail?id=AA00I5U2
abcr GmbH
AB464020
http://www.abcr.de/shop/en/AB464020
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
BioChemPartner
BCP24038
http://www.biochempartner.com/313368-91-1-BCP24038
BOC Sciences
313368-91-1
https://www.bocsci.com/product/lumateperone-cas-313368-91-1-470913.html
Chemspace
CSSB00016994610
https://chem-space.com/CSSB00016994610
DC Chemicals
DC22906
http://www.dcchemicals.com/product_show-DC22906.html
eNovation Chemicals
D572903
http://www.enovationchem.com/productDetails.asp?productID=D572903
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
PubMed

PubMed

TitleDatePubMed
Dopamine D2 receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia.
2019-02
Patents

Patents

6713471
2
Substance Class Chemical
Created
by admin
on Mon Mar 31 23:22:29 GMT 2025
Edited
by admin
on Mon Mar 31 23:22:29 GMT 2025
Record UNII
70BSQ12069
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
lumateperone [INN]
Preferred Name English
Lumateperone
INN   USAN   WHO-DD  
USAN   INN  
Official 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 Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
USAN
DE-107
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
ChEMBL
CHEMBL3545045
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
CAS
313368-91-1
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
DRUG CENTRAL
5358
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
MERCK INDEX
m12238
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
INN
10156
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
DRUG BANK
DB06077
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
RXCUI
2275602
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
NCI_THESAURUS
C166975
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
WIKIPEDIA
LUMATEPERONE
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
FDA UNII
70BSQ12069
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
SMS_ID
300000025855
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
DAILYMED
70BSQ12069
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
PUBCHEM
21302490
Created by admin on Mon Mar 31 23:22:29 GMT 2025 , Edited by admin on Mon Mar 31 23:22:29 GMT 2025
PRIMARY
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 ?M (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
Structure of Lumateperone C-14
LABELED -> NON-LABELED
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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