Lumateperone
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2019
- First approval year
- 2019
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Lumateperone
- Molecular weight
- 393.51
- Structure (SMILES)
- CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12
- iti 007
- ITI 007
- iti 722
- ITI-007
- ITI-722
- iti007
- ITI007
- lumateperona
- Lumateperona
- lumateperone
- Lumateperone
- lumateperone [INN]
- LUMATEPERONE [MI]
- LUMATEPERONE [USAN]
- Lumateperone [WHO-DD]
- lumateperone inn
- lumateperone mi
- lumateperone usan
- lumateperone who dd
- ATC classification codes
- N05AD10
Sources for recorded values
- CAS registry numbers
- 313368-91-1
- ChEMBL ID
- CHEMBL3306803
- InChIKey
- HOIIHACBCFLJET-SFTDATJTSA-N
- PubChem compound IDs
- 21302490
- RxNorm IDs (RxCUI)
- 2275602
- FDA ingredient codes (UNII)
- 70BSQ12069
- Applicant
- INTRA-CELLULAR
- Approval date
- 20 Dec 2019
- Application number
- NDA209500
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- United States (FDA)
- Approved
- Pharmacology name
- lumateperone
- Type
- Synthetic organic
- Drug name stem
- -perone
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Antagonist
- Action type
- Antagonist
- Target
- D2 receptor
- Gene symbol
- DRD2
- Protein identifier
- P14416
- Median affinity
- 7.49
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- 5-HT2A receptor
- Gene symbol
- HTR2A
- Protein identifier
- P28223
- Median affinity
- 9.3
- Affinity units
- pKi
- Mechanism
- Dopamine D2 receptor antagonist
- Action type
- Antagonist
- Target
- D(2) dopamine receptor
- Protein identifier
- P14416
- Mechanism
- Serotonin 2a (5-HT2a) receptor antagonist
- Action type
- Antagonist
- Target
- 5-hydroxytryptamine receptor 2A
- Protein identifier
- P28223
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- SERT
- Gene symbol
- SLC6A4
- Protein identifier
- P31645
- Median affinity
- 7.21
- Affinity units
- pKi
- Mechanism
- Serotonin transporter inhibitor
- Action type
- Inhibitor
- Target
- Sodium-dependent serotonin transporter
- Protein identifier
- P31645
- Mechanism
- Dopamine D2 receptor antagonist
- Action type
- Antagonist
- Target
- D(2) dopamine receptor
- Mechanism
- Serotonin 2a (5-HT2a) receptor antagonist
- Action type
- Antagonist
- Target
- 5-hydroxytryptamine receptor 2A
- Mechanism
- Serotonin transporter inhibitor
- Action type
- Inhibitor
- Target
- Sodium-dependent serotonin transporter
- Action type
- Antagonist
- Gene symbol
- DRD2
- Protein identifier
- P14416
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Antagonist
- Gene symbol
- DRD1
- Protein identifier
- P21728
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Antagonist
- Gene symbol
- HTR2A
- Protein identifier
- P28223
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Psychotic Disorders
- Highest recorded phase
- 4
- Condition identifier
- EFO:0005407
- Subject identifier
- D011618
- Condition
- Depressive Disorder, Major
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0002009
- Subject identifier
- D003865
- Condition
- Alzheimer Disease
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0004975
- Subject identifier
- D000544
- Condition
- Bipolar Disorder
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0004985
- Subject identifier
- D001714
- Condition
- Schizophrenia
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0005090
- Subject identifier
- D012559
- Condition identifier
- EFO_0004698
- Highest recorded phase
- 3
- Condition identifier
- EFO_0005407
- Condition identifier
- EFO_0007634
- Highest recorded phase
- 3
- Condition identifier
- EFO_0009963
- Highest recorded phase
- 3
- Condition identifier
- EFO_0009964
- Highest recorded phase
- 3
- Condition identifier
- HP_0000713
- Highest recorded phase
- 3
- Condition identifier
- HP_0000737
- Highest recorded phase
- 3
- Condition identifier
- HP_0000741
- Highest recorded phase
- 3
- Condition identifier
- HP_0012076
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002009
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002050
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004975
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004985
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005090
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005258
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005485
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005487
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0013600
- Highest recorded phase
- 3
Warnings
- Warning
- Black Box Warning
Open Targets warnings
- Warning
- Black Box Warning
- Country
- United States
- Event
- blood sodium decreased
- Reports
- 4
- Reporting signal score
- 12.4242
- Event
- burning sensation
- Reports
- 5
- Reporting signal score
- 11.6851
- Event
- fear of weight gain
- Reports
- 1
- Reporting signal score
- 8.00051
- Event
- feeling drunk
- Reports
- 2
- Reporting signal score
- 7.25486
- Event
- hallucination, auditory
- Reports
- 4
- Reporting signal score
- 12.6342
- Event
- polyuria
- Reports
- 5
- Reporting signal score
- 19.4299
- Event
- urine output increased
- Reports
- 2
- Reporting signal score
- 8.9636
- NCT01499563
- NCT02282761
- NCT02288845
- NCT02469155
- NCT03817528
- NCT04709224
- NCT04779177
- NCT04959032
- NCT02078310
- NCT02600494
- NCT02600507
- NCT03249376
- NCT04285515
- NCT06372964
- NCT06462586
- NCT06462612
- NCT04985942
- NCT05061706
- NCT05061719
- NCT05850689
- NCT05890768
- Dose
- 42mg
- Route
- Oral
- How often
- Once daily
Conditions of use
- With or without food
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 0
- Polar surface area
- 26.79
- Calculated partition coefficient (ALogP)
- 3.92
- Calculated partition coefficient (XLogP)
- 3.8
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 5
- Heavy atoms
- 29
- Molecular formula
- C24H28FN3O
- Monoisotopic mass
- 393.22164069
- Natural product
- No
- 72060-110
- 72060-121
- 72060-142
- Recorded assays
- 16
- Active assays
- 10
Active assay types
- Confirmatory
Related records
Trials (40)
- A Study of Lumateperone Versus Placebo in Participants With Major Depressive Disorder
- A Trial to Assess the Antipsychotic Efficacy of ITI-007
- A Trial to Assess the Antipsychotic Efficacy of ITI-007 Over 6 Weeks of Treatment
- An Open-label Study of Lumateperone as Adjunctive Therapy in the Treatment of Patients With Major Depressive Disorder
- Caplyta Versus Placebo for Adults With Social Anxiety Disorder
- Clinical Trial Evaluating ITI-007 (Lumateperone) as a Monotherapy for the Treatment of Bipolar Depression
- Clinical Trial Evaluating ITI-007 as an Adjunctive Therapy to Lithium or Valproate for the Treatment of Bipolar Depression
- Clinical Trial Evaluating Lumateperone Monotherapy in the Treatment of Bipolar Depression or Major Depressive Disorder
- Clinical Trial of Lumateperone as Adjunctive Therapy in the Treatment of Patients With Major Depressive Disorder
- ITI-007 (Lumateperone Tosylate) for Schizophrenia
- ITI-007 for the Treatment of Agitation in Patients With Dementia, Including Alzheimer's Disease
- Lumateperone Added to Antidepressant Therapy in Adults With Major Depressive Disorder Experiencing Emotional Blunting
- Lumateperone for Late-Life Depression
- Lumateperone for the Improvement of Apathy in Patients With Psychotic Symptoms.
- Lumateperone for the Prevention of Relapse in Patients With Schizophrenia
- Lumateperone in the Treatment of Stuttering, Childhood Onset Fluency Disorder
- Lumateperone Monotherapy for the Treatment of Bipolar Depression Conducted Globally
- Metabolic Effects of Adjunctive Lumateperone Treatment in Clozapine-Treated Patients With Schizophrenia
- Multicenter Study of Lumateperone as Adjunctive Therapy in the Treatment of Patients With Major Depressive Disorder
- Multicenter Study of Lumateperone for the Treatment of Bipolar Depression in Pediatric Patients
Approved for (1)
- Psychotic disorder
In development for (9)
- Alzheimer disease Phase 1
- Autism spectrum disorder Phase 3
- Bipolar disorder Phase 3
- Borderline personality disorder Phase 2
- Depressive disorder Phase 3
- Insomnia Phase 3
- Major depressive disorder Phase 3
- Schizoaffective disorder Phase 1
- Schizophrenia Phase 3