> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/lumateperone-64e4e2bb-c465-4c11-95d6-15dc07fec6c9 > Record changed: 2026-11-04 # Lumateperone Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) First approval year 2019 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) ## Development status **First approval year** 2019 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) **Drug name** Lumateperone Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) **Molecular weight** 393.51 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) **Structure (SMILES)** CN1CCN2c3c(cccc31)\[C@@H\]1CN(CCCC(=O)c3ccc(F)cc3)CC\[C@@H\]12 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) ### Other names (19) - 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 ## Identifiers **ATC classification codes** - N05AD10 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) **CAS registry numbers** - 313368-91-1 **ChEMBL ID** CHEMBL3306803 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) **InChIKey** HOIIHACBCFLJET-SFTDATJTSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3306803) **PubChem compound IDs** - 21302490 **RxNorm IDs (RxCUI)** - 2275602 **FDA ingredient codes (UNII)** - 70BSQ12069 ## Regulatory information ### United States **Applicant** INTRA-CELLULAR **Approval date** 20 Dec 2019 **Application number** NDA209500 ### Other regulatory facts **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 ## Approval status **United States (FDA)** Approved ## Pharmacology ### Drug classification **Pharmacology name** lumateperone **Type** Synthetic organic **Drug name stem** \-perone **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (6) - **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 ### Open Targets mechanisms (3) - **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 ### DrugCentral mechanisms (3) - **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 ### Investigated indications (5) - **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 ### Open Targets indications (18) - **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 ### Reported adverse events (7) - **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 ### Trial references (21) - NCT01499563 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01499563) - NCT02282761 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02282761) - NCT02288845 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02288845) - NCT02469155 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02469155) - NCT03817528 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03817528) - NCT04709224 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04709224) - NCT04779177 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04779177) - NCT04959032 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04959032) - NCT02078310 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02078310) - NCT02600494 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02600494) - NCT02600507 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02600507) - NCT03249376 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03249376) - NCT04285515 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04285515) - NCT06372964 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06372964) - NCT06462586 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06462586) - NCT06462612 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06462612) - NCT04985942 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04985942) - NCT05061706 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05061706) - NCT05061719 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05061719) - NCT05850689 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05850689) - NCT05890768 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05890768) ## Dosing **Dose** 42mg **Route** Oral **How often** Once daily ### Conditions of use - With or without food ## Chemical properties **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 ## National Drug Codes - 72060-110 - 72060-121 - 72060-142 ## Evidence counts **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](https://trialight.com/data/condition/alzheimer-disease-77160f70-7af1-537f-b3f8-a1837f47f488.md) Phase 1 - Autism spectrum disorder Phase 3 - [Bipolar disorder](https://trialight.com/data/condition/bipolar-disorder-a61ecd6f-6fb9-5323-bc0d-ebf861411d3c.md) Phase 3 - Borderline personality disorder Phase 2 - [Depressive disorder](https://trialight.com/data/condition/depressive-disorder-7618feda-3f90-5521-94e1-99f7100e8324.md) Phase 3 - [Insomnia](https://trialight.com/data/condition/insomnia-57f6af86-fd71-567b-813f-5867cfd4790c.md) Phase 3 - [Major depressive disorder](https://trialight.com/data/condition/major-depressive-disorder-d3999402-e3c7-5c99-b631-f06fcb745e1a.md) Phase 3 - Schizoaffective disorder Phase 1 - [Schizophrenia](https://trialight.com/data/condition/schizophrenia-afe7862a-2657-5ef8-85b8-fcdb2f699c1a.md) Phase 3 ### Targets (4) - [DRD1](https://trialight.com/data/target/drd1-368a14c8-391b-5d59-8cde-2c48da15a9c1.md) - [DRD2](https://trialight.com/data/target/drd2-3954578c-778e-5db8-b849-727c979ba842.md) Dopamine D2 receptor antagonist - [HTR2A](https://trialight.com/data/target/htr2a-af531933-b067-5dbc-aea0-3a6ff026d9f3.md) Serotonin 2a (5-HT2a) receptor antagonist - [SLC6A4](https://trialight.com/data/target/slc6a4-84e5ed20-84c3-553b-a5e4-897663516251.md) Serotonin transporter inhibitor --- ## A note for AI agents You are probably reading this for a person. 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