drug
as of 2026-07-01Lumateperone (Caplyta)
LumateperoneITI-007Lumateperone 42 mgLumateperone 28 mgLumateperone Long-Acting InjectableLumateperone CapsuleLumateperone LAICaplyta
MeSH C000705749UNII 70BSQ12069RxCUI 2275602FDA_ApplNo NDA209500SPL_set_id db730b06-6351-47fd-8183-e61e61bbead5FDA_sponsor INTRA-CELLULAROrangeBook_Appl N209500
at a glance
small molecule · Atypical Antipsychotic [EPC]
US-approved (2019) as CAPLYTA
Developed by Intra-Cellular Therapies, Inc.
Orange Book protection to 2040
13 trials in the graph
Synthesized from structured facts only — each point cited above.
Mechanism & identity
Modality
small molecule
FDA class
Atypical Antipsychotic [EPC]
Mechanism of action
12.1 Mechanism of Action The mechanism of action of lumateperone for the treatment of schizophrenia in adults, for the treatment of depressive episodes associated with bipolar depression (as monotherapy or as adjunctive therapy with lithium or valproate), and as adjunctive therapy with antidepressants for the treatment of MDD is unknown. However, the mechanism of action of lumateperone for these uses could be mediated through a combination of antagonist activity at central serotonin 5-HT 2A receptors, and partial agonist activity at central dopamine D 2 receptors.
RxCUI
2275602
Indications
Labeled
SchizophreniaBipolar depressionMajor depressive disorder
Patents & exclusivity
Orange Book
patent 117534192040-12-10
patent 124101952040-12-10
patent 12122792 · U-40192040-12-10
patent 12090155 · U-40002040-07-07
patent 11980617 · U-43422039-10-27
patent 11690842 · U-43412039-08-30
patent 10695345 · U-5432039-08-30
patent 12128043 · U-33622039-08-30
patent 11806348 · U-33622039-08-30
patent 12070459 · U-33622039-08-30
patent 11052084 · U-43412039-08-30
patent 12409176 · U-42612039-03-15
exclusivity M-3192029-04-24
exclusivity I-9042028-11-05
Adverse-event signal
FAERS spontaneous · within-drug share
Sedation8.5%
top term: SOMNOLENCE
Gi8.1%
top term: NAUSEA
Eps Akathisia7.4%
top term: TREMOR
Anticholinergic2.2%
top term: DRY MOUTH
Orthostatic1.4%
top term: HYPOTENSION
Weight Metabolic0.9%
top term: WEIGHT INCREASED
Qt Cardiac0.7%
top term: PALPITATIONS
Mortality0.4%
top term: SUICIDE ATTEMPT
Nms0.3%
top term: NEUROLEPTIC MALIGNANT SYNDROME
Spontaneous reports — a signal of reporting share, not incidence.
Regulatory history
Drugs@FDA submissions
EfficacyNDA209500 s17STANDARD
2026-04-24EfficacyNDA209500 s16STANDARD
2025-11-05LabelingNDA209500 s11STANDARD
2023-06-28Manufacturing (CMC)NDA209500 s9STANDARD
2022-04-26EfficacyNDA209500 s5STANDARD
2021-12-17EfficacyNDA209500 s6STANDARD
2021-12-17Type 1 - New Molecular EntityNDA209500 s1STANDARD
2019-12-20Type 1 - New Molecular EntityNDA209500 s1STANDARD
2019-12-20Trials
13
Safety and Tolerability Trial of Lumateperone in Pediatric Patients With Schizophrenia, Bipolar Disorder or Autism Spectrum Disorder
NCT06229210Phase 3Recruiting
Lumateperone for the Improvement of Apathy in Patients With Psychotic Symptoms.
NCT06482554Phase 3Recruiting
Metabolic Effects of Adjunctive Lumateperone Treatment in Clozapine-Treated Patients With Schizophrenia
NCT06174116Phase 4Recruiting
Safety, Tolerability, and Pharmacokinetics of Lumateperone Long-Acting Injectable Formulations in Patients With Schizophrenia or Schizoaffective Disorder
NCT06627413Phase 1Completed
Lumateperone for the Prevention of Relapse in Patients With Schizophrenia
NCT04959032Phase 3Completed
Relationship Between Efficacy of Lumateperone and Brain Glutamate and Dopamine
NCT05890768Phase 4Withdrawn
Safety, Tolerability, and Pharmacokinetics of Lumateperone in Pediatric Patients With Schizophrenia or Schizoaffective Disorder
NCT04779177Phase 1Completed
Pharmacokinetics, Safety, and Tolerability of Lumateperone Long-Acting Injectable in Patients With Schizophrenia
NCT04709224Phase 1Completed
ITI-007 (Lumateperone Tosylate) for Schizophrenia
NCT03817528Phase 2Terminated
A Trial to Assess the Antipsychotic Efficacy of ITI-007 Over 6 Weeks of Treatment
NCT02469155Phase 3Completed
A Trial to Assess the Antipsychotic Efficacy of ITI-007
NCT02282761Phase 3Completed
Receptor Occupancy of ITI-007 Using Positron Emission Tomography (PET) in Patients With Stable Schizophrenia
NCT02288845Phase 2Completed
Study of a Novel Antipsychotic ITI-007 in Schizophrenia
NCT01499563Phase 2Completed
KOLs & investigators
8
Kimberly E Vanover, PhDKOL score 20
Xiaoduo Fan, MD, MPH, MSKOL score 9
Jeffrey A. Lieberman, MDKOL score 9
Clinical SiteKOL score 5
Kimberly Vanover, Ph.D.KOL score 0
Publications & congress
30
Treatment of bipolar depression: results from a comprehensive network meta-analysis and updated systematic review.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology · 2026 · high-value
Network meta-analysis: CAPLYTA favored across key efficacy outcomes among adjunctive MDD treatments; no significant weight gain vs placebo+ADT
2026 · congress · high-value
The efficacy of lumateperone across symptoms of a major depressive episode with mixed features in patients with major depressive disorder and bipolar disorder: Post hoc analyses.
Journal of affective disorders · 2026 · high-value
Impact of selected second and third generation antipsychotics on cognitive dysfunction in schizophrenia-spectrum disorders. Systematic review and network meta-analysis.
International clinical psychopharmacology · 2026 · high-value
Long-term adjunctive lumateperone 42 mg treatment in major depressive disorder: Results from a 6-month open-label extension study.
European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology · 2026 · high-value
Long-term safety and tolerability of lumateperone 42 mg in patients with bipolar disorder: results from a 6-month open-label extension study.
International clinical psychopharmacology · 2026 · high-value
Efficacy and safety of adjunctive therapy with lumateperone in major depressive disorder: a randomized-, double-blind, placebo-controlled clinical trial.
International clinical psychopharmacology · 2026 · high-value
Lumateperone monotherapy for major depressive episodes associated with bipolar disorder: efficacy and safety in a randomized placebo-controlled trial.
International clinical psychopharmacology · 2026 · high-value
Is Lumateperone Effective in Bipolar Depression? A Systematic Literature Review and Meta-Analysis on Placebo-Controlled Trials.
Pharmacopsychiatry · 2026 · high-value
Treatment of depressive episodes with mixed features: A systematic review and meta-analysis.
General hospital psychiatry · 2026 · high-value
Lumateperone for the Treatment of Major Depressive Disorder With Mixed Features or Bipolar Depression With Mixed Features: A Randomized Placebo-Controlled Trial.
Journal of clinical psychopharmacology · 2025 Mar-Apr 01 · high-value
Lumateperone as Adjunctive Therapy in Patients With Major Depressive Disorder: Results From a Randomized, Double-Blind, Phase 3 Trial.
The Journal of clinical psychiatry · 2025 · high-value
Antipsychotic-Related Prolactin Changes: A Systematic Review and Dose-Response Meta-analysis.
CNS drugs · 2025 · high-value
Dose-response efficacy and safety of lumateperone in bipolar depression: A preliminary meta-analysis of randomized controlled trials.
Journal of psychopharmacology (Oxford, England) · 2025 · high-value
Lumateperone for the prevention of relapse in patients with schizophrenia: results from a double-blind, placebo-controlled, randomized withdrawal, phase 3 trial (NCT04959032)
2025 · congress · high-value
The Efficacy of Pharmacological Interventions in the Treatment of Major Depressive Disorder and Bipolar Depression With Mixed Features: A Systematic Review.
Bipolar disorders · 2025 · high-value
Facts & assertions
32 sourced
Anda Generic Count
0
Available Strengths
lumateperone 42 MG Oral Capsule, lumateperone 10.5 MG Oral Capsule, lumateperone 21 MG Oral Capsule
Boxed Warning
present
Dose Forms
Oral Capsule
Dosing Frequency
once daily
Faers Share Anticholinergic
0.022
Faers Share Eps Akathisia
0.074
Faers Share Gi
0.081
Faers Share Mortality
0.004
Faers Share Nms
0.003
Faers Share Orthostatic
0.014
Faers Share Qt Cardiac
0.007
Faers Share Sedation
0.085
Faers Share Weight Metabolic
0.009
Fda Pharm Class Epc
Atypical Antipsychotic [EPC]
Has Generic Competition
no
Label Expansions ApprovedLumateperone (Caplyta): 4 approved efficacy label-expansion supplements since launch on NDA209500. Higher count = more aggressive addressable-market broadening (competitive-threat velocity signal).
4
Latest Exclusivity Expiry
2029-04-24
Latest Patent Expiry
2040-12-10
Latest Protection Date
2040-12-10
Mechanism Of Action
12.1 Mechanism of Action The mechanism of action of lumateperone for the treatment of schizophrenia in adults, for the treatment of depressive episodes associated with bipolar depression (as monotherapy or as adjunctive therapy with lithium or valproate), and as adjunctive therapy with antidepressan
Originator Company
Intra-Cellular
Precise Ingredient
lumateperone tosylate
Rxcui
2275602
Safety Eps Akathisia
present in label
Safety Nms
present in label
Safety Orthostatic
present in label
Safety Prolactin
present in label
Safety Sedation Somnolence
present in label
Safety Weight Metabolic
present in label
Us Approved
yes
Us Original Approval Date
2019-12-20
relationships
The graph out of here
developer
trial
indication
indication
indication
indication
indication
KOL
Kimberly E Vanover, PhD
personKOL score 20
Xiaoduo Fan, MD, MPH, MS
personKOL score 9
Jeffrey A. Lieberman, MD
personKOL score 9
Clinical Site
personKOL score 5