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    Mechanism of action and pharmacology

    The antipsychotic activity of CAPLYTA is thought to be mediated through a combination of antagonism of serotonin 5-HT2A receptors and postsynaptic antagonism of dopamine D2 receptors. The mechanism of action of CAPLYTA is unknown.1

    CAPLYTA simultaneously has:

    Affinity at 5-HT2A approximately 60 times higher than at dopamine D21,2*

    High 5-HT2A/D2 occupancy ratio allows for lower amounts of dopamine D2 antagonism at therapeutic doses3

    A moderate binding affinity for dopamine D2, D1, and SERT1

    A low binding affinity for off-target receptors like muscarinic and histaminergic receptors1

    Elevated levels of dopamine D2 receptor occupancy are known to be associated with increases in extrapyramidal symptoms (EPS) and prolactin3

    The binding of CAPLYTA to the D1 receptor may contribute to indirect activation of the AMPA and NMDA receptors.

    *5-HT2A (Ki=0.48 nM); D2 (Ki=47 nM); human recombinant receptor expressed in HEK-293 cells. Observed values may vary.2

    CAPLYTA receptor-binding profile1,2

    • High binding affinity for 5-HT2A and moderate binding affinity for dopamine D21
    • Low affinity for off-target receptors1,3 - CAPLYTA shows little affinity (<50% inhibition at 100 nM) at muscarinic and histaminergic receptors

    CAPLYTA® (lumateperone) has a high binding affinity for 5-HT2A, moderate binding affinity for dopamine D2, and low affinity for off-target receptors.CAPLYTA® (lumateperone) has a high binding affinity for 5-HT2A, moderate binding affinity for dopamine D2, and low affinity for off-target receptors.

    Learn how CAPLYTA patients start on the effective dose

    Helpful tools & resources

    Prior Authorization FormPharmacy Callback Guide
    Resources

    References: 1. CAPLYTA prescribing information, 2022. 2. Data on File. 2021. 3. Davis RE, Correll CU. ITI-007 in the treatment of schizophrenia: from novel pharmacology to clinical outcomes. Expert Rev Neurother. 2016(6):601-614. 4. Kumar B, Kuhad A, Kuhad A. Lumateperone: a new treatment approach for neuropsychiatric disorders. Drugs Today (Barc). 2018;54(12):713-719.