What category of medication is Caplyta (lumateperone)?

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Caplyta Medication Category

Caplyta (lumateperone) is classified as a third-generation antipsychotic medication. 1

Classification Details

Lumateperone is specifically categorized as a third-generation antipsychotic alongside aripiprazole, cariprazine, and brexpiprazole, distinguishing it from second-generation antipsychotics (such as olanzapine, risperidone, and quetiapine) and first-generation antipsychotics (such as haloperidol and chlorpromazine). 1

Pharmacological Characteristics

The FDA-approved drug label describes lumateperone as an atypical antipsychotic with a unique mechanism of action. 2

Lumateperone simultaneously modulates three key neurotransmitter systems:

  • Serotonin: High binding affinity for 5-HT2A receptors (Ki = 0.54 nM) and moderate affinity for serotonin transporters (Ki = 33 nM) 2, 3
  • Dopamine: Moderate binding affinity for D2 receptors (Ki = 32 nM), acting as both a presynaptic partial agonist and postsynaptic antagonist 2, 4
  • Glutamate: Indirect modulation of glutamatergic neurotransmission 3, 4

This multi-target-directed mechanism differentiates lumateperone from traditional second-generation antipsychotics, as it has lower affinity for histaminergic (H1) and muscarinic receptors, which contributes to its favorable metabolic and sedation profile. 4, 5

FDA-Approved Indications

Lumateperone received FDA approval in December 2019 for the treatment of schizophrenia in adults, making it the first-in-class selective and simultaneous modulator of serotonin, dopamine, and glutamate. 6

The medication is also approved for depressive episodes associated with bipolar I or II disorder, though the primary classification remains as an antipsychotic agent. 2

Clinical Positioning

As a third-generation antipsychotic, lumateperone is positioned as a novel therapeutic option for patients who may be intolerant to the extrapyramidal symptoms or metabolic adverse effects commonly seen with other antipsychotics. 4, 5

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Lumateperone: A Novel Antipsychotic for Schizophrenia.

The Annals of pharmacotherapy, 2021

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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