Atypical antipsychotic with multimodal activity
Potent antagonism at serotonin 5-HT₂A receptors, presynaptic partial agonism and postsynaptic antagonism at dopamine D₂ receptors, and indirect modulation of glutamatergic neurotransmission via dopamine D₁ receptor-dependent mechanisms. This multi-receptor activity is thought to underlie its antipsychotic, antidepressant, and procognitive effects, distinguishing it from other second-generation antipsychotic agents.
Schizophrenia; depressive episodes associated with bipolar I or II disorder (monotherapy and adjunctive to lithium or valproate)
Limited off-label use due to novel status; potential utility in neuropsychiatric symptom management
Oral capsules
42 mg p.o. once daily with food; no titration required
42 mg daily
Oral bioavailability improved with food; metabolized primarily via CYP3A4 and CYP1A2; half-life approximately 18 hours
Somnolence, dry mouth, dizziness, nausea
Low risk of weight gain, extrapyramidal symptoms, or metabolic abnormalities reported
Monitor for sedation, metabolic parameters, and extrapyramidal symptoms as clinically indicated
Increased mortality in elderly patients with dementia-related psychosis
Lumateperone may be preferred in patients with dementia, Parkinson’s disease (PD), or traumatic brain injury (TBI) due to its low sedation, metabolic, and extrapyramidal symptom risks. Its once-daily dosing can improve adherence in neuropsychiatric populations.