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Lumateperone

Generic Name
Lumateperone
Brand Names
Caplyta
Drug Type
Small Molecule
Chemical Formula
C24H28FN3O
CAS Number
313368-91-1
Unique Ingredient Identifier
70BSQ12069

Overview

Schizophrenia is a complex mental illness and impacts approximately 1% of the population. Although there are several antipsychotics including aripiprazole, paliperidone and clozapine available for clinical use, they are generally accompanied by significant metabolic and/or neurological adverse effects. Lumateperone is a newly approved 2nd generation antipsychotic currently indicated for the treatment of schizophrenia. It has a unique receptor binding profile and differs from other antipsychotics in that it modulates glutamate, serotonin and dopamine, which are all neurotransmitters that contribute to the pathophysiology of schizophrenia. The data so far indicates that lumateperone can alleviate both positive and negative symptoms of schizophrenia. Further, not only is the new antipsychotic selective for dopamine (D2) receptors in the mesolimbic and mesocortical brain regions, but it also has minimal off-target activity. Both characteristics lend to a more favourable adverse effect profile and ultimately safer drug.

Background

Schizophrenia is a complex mental illness and impacts approximately 1% of the population. Although there are several antipsychotics including aripiprazole, paliperidone and clozapine available for clinical use, they are generally accompanied by significant metabolic and/or neurological adverse effects. Lumateperone is a newly approved 2nd generation antipsychotic currently indicated for the treatment of schizophrenia. It has a unique receptor binding profile and differs from other antipsychotics in that it modulates glutamate, serotonin and dopamine, which are all neurotransmitters that contribute to the pathophysiology of schizophrenia. The data so far indicates that lumateperone can alleviate both positive and negative symptoms of schizophrenia. Further, not only is the new antipsychotic selective for dopamine (D2) receptors in the mesolimbic and mesocortical brain regions, but it also has minimal off-target activity. Both characteristics lend to a more favourable adverse effect profile and ultimately safer drug.

Indication

Lumateperone is approved for the treatment of schizophrenia in adults. It is also approved for the treatment of depressive episodes associated with bipolar disorder (i.e. bipolar depression) in adults, as monotherapy and/or adjunctive therapy with lithium or valproate.

Associated Conditions

  • Depressive Episodes
  • Schizophrenia

Research Report

Published: Jun 9, 2025

Comprehensive Report on Lumateperone (Caplyta)

1. Introduction to Lumateperone (Caplyta)

1.1 Overview

Lumateperone, marketed under the brand name Caplyta®, is a novel second-generation (atypical) antipsychotic agent developed for the treatment of serious central nervous system (CNS) disorders.[1] It is specifically approved for schizophrenia and bipolar depression in adults.[1] Lumateperone is distinguished by a unique receptor binding profile, which contributes to its mechanism of action and a generally favorable tolerability profile, particularly concerning metabolic disturbances and extrapyramidal symptoms (EPS), when compared to some other antipsychotic medications.[1]

Schizophrenia, a complex mental illness affecting approximately 1% of the population, presents a significant treatment challenge [User Query]. While several antipsychotics, including aripiprazole, paliperidone, and clozapine, are available, their use is often accompanied by significant metabolic and/or neurological adverse effects [User Query]. Lumateperone's development appears to be a direct response to these limitations. The emphasis on its "novel" mechanism involving the modulation of glutamate, serotonin, and dopamine, coupled with "minimal off-target activity" and a "more favourable adverse effect profile," suggests a targeted drug design strategy aimed at improving upon existing therapies [User Query]. This approach seeks to provide efficacy in managing both positive and negative symptoms of schizophrenia with enhanced safety and tolerability [User Query].

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2024/11/26
Phase 3
Recruiting
2024/11/15
Phase 3
Recruiting
2024/10/04
Phase 1
Recruiting
2024/08/16
Phase 1
Recruiting
2024/07/01
Phase 3
Recruiting
Louisiana State University Health Sciences Center Shreveport
2024/06/17
Phase 3
Recruiting
2024/06/17
Phase 3
Recruiting
2024/04/18
Phase 3
Recruiting
2024/01/29
Phase 3
Recruiting
2023/12/18
Phase 4
Recruiting
University of Massachusetts, Worcester

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
REMEDYREPACK INC.
70518-3497
ORAL
42 mg in 1 1
1/12/2024
Intra-Cellular Therapies, Inc
72060-142
ORAL
42 mg in 1 1
9/22/2022
Intra-Cellular Therapies, Inc
72060-121
ORAL
21 mg in 1 1
9/22/2022
Intra-Cellular Therapies, Inc
72060-110
ORAL
10.5 mg in 1 1
9/22/2022

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
No TGA approvals found for this drug.
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