Drug intelligence / Profile preview

lumateperone

Development stage
Approved
Lead developer
Intra-Cellular Therapies
Modality
Small Molecules
Administration
Oral
01

Overview

Lumateperone is a second-generation (atypical) antipsychotic medication of the butyrophenone class, approved for the treatment of schizophrenia and depressive episodes associated with bipolar I or II disorder in adults, either as monotherapy or adjunctive therapy. Its mechanism of action involves modulation of several neurotransmitter systems: it acts as an antagonist at serotonin 5-HT2A receptor (with high affinity), binds to dopamine receptor D1, dopamine receptor D2, and dopamine receptor D4 (acting as a partial agonist at presynaptic dopamine receptor D2 and antagonist at postsynaptic dopamine receptor D2), inhibits serotonin transporter reuptake moderately, and has some off-target antagonism at α1 adrenergic receptors. Lumateperone also indirectly augments glutamatergic neurotransmission via effects on NMDA receptor phosphorylation through its activity at dopamine receptor D1. This unique pharmacological profile allows it to address both positive and negative symptoms of schizophrenia while minimizing certain side effects common to other antipsychotics[1][2][3][5][7].

Brand names
Caplyta
Other names
lumateperone tosylate
02

Targets

DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)DAT (Dopamine plasma membrane transport protein)HTR2A (Serotonin receptor 5-HT2A)SERT (Sodium-dependent serotonin transporter)

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