Lumateperone, sold under the brand name Caplyta, is an atypical antipsychotic medication of the butyrophenone class.
It is approved for the treatment of schizophrenia as well as bipolar depression, as either monotherapy or adjunctive therapy with lithium or valproate.
Oral agent.
Atypical antipsychotic
Bioavailability 4.4%.
Protein binding 97.4%
Metabolism Multiple UGTs, CYP450s, and AKR enzymes
Excretion <1% excreted unchanged in urine
Medical uses
Schizophrenia
Bipolar depression
Adverse effects
The most common adverse effects (≥5%) were somnolence and dry mouth, low rate of serum aminotransferase elevations during therapy, but has not been linked to acute liver injury.
Lumateperone acts as a receptor antagonist of 5-HT2A receptor and antagonizes several dopamine receptors (D1, D2, and D4) with lower affinity.
It has moderate serotonin transporter reuptake inhibition.
It has additional off-target antagonism at α1 receptors, without appreciable antimuscarinic or antihistaminergic properties, limiting side effects associated with other atypical antipsychotics.
After taking the medication by mouth, lumateperone reaches maximum plasma concentrations within 1–2 hours and has a terminal elimination half-life of 18 hours.
Lumateperone is a substrate for numerous metabolic enzymes.
Lumateperone does not cause appreciable inhibition of any common CYP450 enzymes.
It is not a substrate for p-glycoprotein.