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
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
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL224 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24559051 |
0.54 nM [Ki] | ||
Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24559051 |
32.0 nM [Ki] | ||
Target ID: CHEMBL228 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24559051 |
61.0 nM [Ki] |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse events |
---|---|---|
42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Other AEs: Somnolence, Nausea... Other AEs: Somnolence (24%) Sources: 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 |
60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 26 to 57 years n = 10 Health Status: unhealthy Condition: Schizophrenia Age Group: 26 to 57 years Sex: M+F Population Size: 10 Sources: |
Other AEs: Headache, Sedation... Other AEs: Headache (grade 1-2, 40%) 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, mean 38.3 years n = 84 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 38.3 years Sex: M+F Population Size: 84 Sources: |
Other AEs: Somnolence, Dry mouth... Other AEs: Somnolence (16.7%) Sources: Dry mouth (4.8%) Nausea (6%) Dizziness (4.8%) Akathisia (1.2%) Tachycardia (1.2%) |
90 mg 1 times / day steady, oral (mean) Studied dose Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: |
unhealthy, mean 39.7 years n = 167 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 39.7 years Sex: M+F Population Size: 167 Sources: |
Disc. AE: Dry mouth, Schizophrenia aggravated... AEs leading to discontinuation/dose reduction: Dry mouth (0.6%) Sources: Schizophrenia aggravated (0.6%) |
120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, mean 41.1 years n = 83 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 41.1 years Sex: M+F Population Size: 83 Sources: |
Other AEs: Somnolence, Dry mouth... Other AEs: Somnolence (32.5%) Sources: Dry mouth (8.4%) Nausea (4.8%) Dizziness (8.4%) Akathisia (2.4%) |
42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Disc. AE: Headache, Orthostatic hypotension... Other AEs: Headache, Somnolence... AEs leading to discontinuation/dose reduction: Headache (1.3%) Other AEs:Orthostatic hypotension (grade 3, 0.7%) Headache (grade 1-2, 19.3%) Sources: 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%) |
28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Disc. AE: Convulsions... Other AEs: Akathisia, Headache... AEs leading to discontinuation/dose reduction: Convulsions (grade 3, 0.7%) Other AEs:Akathisia (grade 1-2, 4%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Akathisia | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Difficulty breathing | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Drooling | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Dyskinesia | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Dystonia | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Extrapyramidal disorder | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Muscle contractions involuntary | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Muscle spasms | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Muscle twitching | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Musculoskeletal stiffness | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Protrusion tongue | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Restlessness | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Spasm of muscle | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Swallowing difficult | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Tardive dyskinesia | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Tremor | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
|
Decreased appetite | 2% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Transaminases increased | 2% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Somnolence | 24% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Fatigue | 3% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Vomiting | 3% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Creatine phosphokinase increased | 4% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Dizziness | 5% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Dry mouth | 6% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Extrapyramidal symptoms | 6.7% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Nausea | 9% | 42 mg 1 times / day steady, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: steady Dose: 42 mg, 1 times / day Sources: |
unhealthy, 19 to 60 years n = 406 Health Status: unhealthy Condition: Schizophrenia Age Group: 19 to 60 years Sex: M+F Population Size: 406 Sources: |
Sedation | grade 1, 40% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 26 to 57 years n = 10 Health Status: unhealthy Condition: Schizophrenia Age Group: 26 to 57 years Sex: M+F Population Size: 10 Sources: |
Headache | grade 1-2, 40% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 26 to 57 years n = 10 Health Status: unhealthy Condition: Schizophrenia Age Group: 26 to 57 years Sex: M+F Population Size: 10 Sources: |
Akathisia | 1.2% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, mean 38.3 years n = 84 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 38.3 years Sex: M+F Population Size: 84 Sources: |
Tachycardia | 1.2% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, mean 38.3 years n = 84 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 38.3 years Sex: M+F Population Size: 84 Sources: |
Somnolence | 16.7% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, mean 38.3 years n = 84 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 38.3 years Sex: M+F Population Size: 84 Sources: |
Dizziness | 4.8% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, mean 38.3 years n = 84 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 38.3 years Sex: M+F Population Size: 84 Sources: |
Dry mouth | 4.8% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, mean 38.3 years n = 84 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 38.3 years Sex: M+F Population Size: 84 Sources: |
Nausea | 6% | 60 mg 1 times / day steady, oral Studied dose Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, mean 38.3 years n = 84 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 38.3 years Sex: M+F Population Size: 84 Sources: |
Dry mouth | 0.6% Disc. AE |
90 mg 1 times / day steady, oral (mean) Studied dose Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: |
unhealthy, mean 39.7 years n = 167 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 39.7 years Sex: M+F Population Size: 167 Sources: |
Schizophrenia aggravated | 0.6% Disc. AE |
90 mg 1 times / day steady, oral (mean) Studied dose Dose: 90 mg, 1 times / day Route: oral Route: steady Dose: 90 mg, 1 times / day Sources: |
unhealthy, mean 39.7 years n = 167 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 39.7 years Sex: M+F Population Size: 167 Sources: |
Akathisia | 2.4% | 120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, mean 41.1 years n = 83 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 41.1 years Sex: M+F Population Size: 83 Sources: |
Somnolence | 32.5% | 120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, mean 41.1 years n = 83 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 41.1 years Sex: M+F Population Size: 83 Sources: |
Nausea | 4.8% | 120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, mean 41.1 years n = 83 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 41.1 years Sex: M+F Population Size: 83 Sources: |
Dizziness | 8.4% | 120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, mean 41.1 years n = 83 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 41.1 years Sex: M+F Population Size: 83 Sources: |
Dry mouth | 8.4% | 120 mg 1 times / day steady, oral Highest studied dose Dose: 120 mg, 1 times / day Route: oral Route: steady Dose: 120 mg, 1 times / day Sources: |
unhealthy, mean 41.1 years n = 83 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 41.1 years Sex: M+F Population Size: 83 Sources: |
Headache | 1.3% Disc. AE |
42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Nausea | grade 1-2, 10.7% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Sedation | grade 1-2, 12.7% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Somnolence | grade 1-2, 17.3% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Headache | grade 1-2, 19.3% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Fatigue | grade 1-2, 5.3% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Constipation | grade 1-2, 6.7% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Dizziness | grade 1-2, 6.7% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Dry mouth | grade 1-2, 7.3% | 42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Orthostatic hypotension | grade 3, 0.7% Disc. AE |
42 mg 1 times / day multiple, oral Recommended Dose: 42 mg, 1 times / day Route: oral Route: multiple Dose: 42 mg, 1 times / day Sources: |
unhealthy, mean 42.4 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 42.4 years Sex: M+F Population Size: 150 Sources: |
Akathisia | grade 1-2, 1.3% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Dyskinesia | grade 1-2, 1.3% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Somnolence | grade 1-2, 11.3% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Headache | grade 1-2, 16% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Akathisia | grade 1-2, 4% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Constipation | grade 1-2, 4% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Dizziness | grade 1-2, 4.7% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Fatigue | grade 1-2, 4.7% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Nausea | grade 1-2, 4.7% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Dry mouth | grade 1-2, 6% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Sedation | grade 1-2, 9.3% | 28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Convulsions | grade 3, 0.7% Disc. AE |
28 mg 1 times / day multiple, oral Studied dose Dose: 28 mg, 1 times / day Route: oral Route: multiple Dose: 28 mg, 1 times / day Sources: |
unhealthy, mean 43.5 years n = 150 Health Status: unhealthy Condition: Schizophrenia Age Group: mean 43.5 years Sex: M+F Population Size: 150 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf#page=130 Page: 130.0 |
yes | |||
yes | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf#page=130 Page: 130.0 |
yes | |||
yes | ||||
yes | ||||
yes | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf#page=130 Page: 130.0 |
yes | |||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000MultidisciplineR.pdf#page=127 Page: 127.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/209500Orig1s000OtherR.pdf#page=94 Page: 94.0 |
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Code | English | ||
|
Common Name | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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 | |||
|
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
|
PRIMARY | |||
|
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 | |||
|
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
|
PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)