Products
Lumateperone was approved in the United States in 2019 in capsule form (Caplyta).
Structure and properties
Lumateperone (C24H28FN3O, Mr = 393.5 g/mol) is present in the drug as lumate perontosylate. Like haloperidol (Haldol), for example, it belongs to the butyrophenone group.
Effects
Lumateperone has antipsychotic and antidepressant properties. Effects are attributed to antagonism at central serotonin 5-HT2A receptors and postsynaptic dopamine D2 receptors, among others. According to the literature, it is effective at both serotonergic, dopaminergic, and glutaminergic systems. Enhancement of NMDA and AMPA (glutaminergic system) activity is thought to cause the antidepressant effect. In addition, the reuptake of serotonin is also inhibited (SERT). The half-life is in the range of 18 hours.
Indications
For the treatment of schizophrenia in adults.
Dosage
According to the SmPC. Capsules are taken once daily with food.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
CYP, AKR, and UGT isozymes are involved in the metabolism of lumateperone. Corresponding interactions are possible.
Adverse effects
The most common potential adverse effects include drowsiness, dullness (sedation), and dry mouth.
