Schizophrenia is a lifelong illness affecting approximately 2.4 million Americans and is characterized by psychotic, negative, cognitive, and affective symptoms. Although there are numerous antipsychotic agents available to treat schizophrenia, optimized treatment for the individual patient varies and is often hindered by serious side effects including extrapyramidal symptoms (EPS) and cardiometabolic effects. Adding to the antipsychotic armamentarium, Intra-Cellular Therapies, Inc has just announced the approval of lumateperone (CAPLYTA®) for the treatment of schizophrenia in adults. The approval was based on promising results from 2 placebo-controlled trials in which lumateperone 42 mg showed efficacy on the Positive and Negative Syndrome Scale (PANSS) total score with most common side effects being somnolence and dry mouth. Although its exact mechanism of action is unknown, lumateperone acts similar to other atypical antipsychotics with antagonist actions at both dopamine D2 and serotonin 5HT2A receptors (Figure). Notably, lumateperone was not associated with EPS, weight gain, or changes in other metabolic parameters.
Like other atypical antipsychotics, lumateperone binds as an antagonist to both dopamine D2 and serotonin receptors with relatively high affinity. Additionally, lumateperone has affinity for the serotonin reuptake transporter (SERT) as well as dopamine D1, adrenergic alpha1, and serotonin 5HT2C receptors.
» Intra-Cellular Therapies Press Release
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