Illuminating Hope for Mental Health: A Drug Review on Lumateperone.

This drug review provides a comprehensive analysis of a novel antipsychotic called lumateperone, marketed as Caplyta. Lumateperone gained FDA approval in 2019 for treating schizophrenia and later, in 2021, for treating bipolar depression. The review begins by delving into lumateperone's mechanism of action, which involves the partial agonism of the dopamine D2 receptor as well as its unique effects on the dopamine transporter, N-methyl-D-aspartate (NMDA) receptor, and serotonin transporter. Additionally, the study examines lumateperone's distinctive pharmacokinetics. Moreover, this review assesses lumateperone's metabolic profile and highlights its favorable outcomes regarding mean body weight, BMI, and waist circumference, surpassing those of other second-generation antipsychotic medications. The study explicitly emphasizes the efficacy and safety of lumateperone in treating schizophrenia and bipolar depression associated with bipolar I and II disorders. An extensive investigation of multiple clinical trials provides compelling evidence of lumateperone's advantages over existing antipsychotic medications. The review also acknowledges the limitations of lumateperone compared to other antipsychotics. In conclusion, this drug review underscores the importance of further research to uncover the additional limitations of lumateperone while acknowledging its promising benefits and potential for advancing treatment options.

Lumateperone tosylate, A Selective and Concurrent Modulator of Serotonin, Dopamine, and Glutamate, in the Treatment of Schizophrenia.

PURPOSE OF REVIEW: This is a comprehensive review of the literature regarding the use of Lumateperone tosylate for schizophrenia. This review presents the background, evidence, and indications for the use of lumateperone tosylate in the treatment of schizophrenia. RECENT FINDINGS: Schizophrenia is a chronic mental health disorder that affects approximately 3.3 million people in the United States. Its symptoms, which must be present more than six months, are comprised of disorganized behavior and speech, a diminished capacity to comprehend reality, hearing voices unheard by others, seeing things unseen by others, delusions, decreased social commitment, and decreased motivation. The majority of these symptoms can be managed with antipsychotic medication. Lumateperone is a selective and concurrent modulator of serotonin, dopamine, and glutamate, which all mediate or modulate serious mental illness. SUMMARY: Schizophrenia is a complex, severe mental illness that affects how the brain processes information. There are many medications used to treat schizophrenia. One antipsychotic agent, lumateperone tosylate, is a newer agent that the FDA recently approved. The most common adverse effects are shown to be mild such as somnolence, constipation, sedation, and fatigue, with the 42 mg recommended dose. Lumateperone tosylate is an FDA-approved drug that can be given only at the 42mg dose once daily with no titration requirements.

Lumateperone: A Novel Antipsychotic for Schizophrenia.

OBJECTIVE: To provide a concise review of the new Food and Drug Administration (FDA)-approved antipsychotic, lumateperone, for use in schizophrenia. DATA SOURCES: A literature search of PubMed was performed (January 2000 to May 2020) using the following key terms: lumateperone, Caplyta, and ITI-007. Abstracts from conferences, review articles, clinical trials, and drug monographs were reviewed. STUDY SELECTION AND DATA EXTRACTION: Relevant English-language monographs and studies conducted in humans were considered. DATA SYNTHESIS: Lumateperone was FDA approved for the treatment of schizophrenia in December 2019 based on 2 published randomized, double-blind, placebo-controlled trials. Lumateperone's pharmacology is consistent with that of other second-generation antipsychotics in that it has a higher affinity for the serotonin (5-HT2A) receptors compared with dopamine (D2) receptors but with lower affinities for α-1 and histaminergic receptors. In addition, it serves as a presynaptic dopamine partial agonist, serotonin reuptake inhibitor, and an indirect modulator of glutamatergic systems. Based on the 4-week clinical trials, lumateperone was well tolerated. Most common treatment-emergent adverse events were headache, somnolence, and dizziness. RELEVANCE TO PATIENT CARE AND CLINICAL PRACTICE: At this time, lumateperone had a statistically significant reduction in Positive and Negative Syndrome Scale when compared with placebo and was not significantly associated with the extrapyramidal symptoms (EPS) and metabolic adverse effects commonly seen with other antipsychotics. CONCLUSIONS: Lumateperone has the potential to benefit individuals with schizophrenia who are intolerant to the EPSs or metabolic adverse effects of other antipsychotics. However, further head-to-head trials with commercially available antipsychotics are still required to assist in establishing its role in treatment.

Lumateperone for the Treatment of Schizophrenia.

Introduction: Schizophrenia is a severe psychotic disorder that is diagnosed by the presence of hallucinations or delusions along with disorganized speech, disorganized thought, or negative symptoms that are present for at least six months. Roughly 1 in 10,000 people a year are diagnosed with this psychiatric disorder. It is a chronic disorder requiring a lifetime of treatment of which antipsychotics have been the mainstay of this treatment. First-generation antipsychotics have dystonia, parkinsonism, and development of Tardive Dyskinesia as major side effects, and they are also nonspecific in terms of their actions. Second Generation antipsychotics target more specific dopamine and sometimes serotonin receptors with less dystonic side effects; however, there are additional concerns for the development of metabolic syndrome. This review aims to look at new medication on the market, lumateperone, for the treatment of Schizophrenia. Recent studies: In one four week study with 60mg and 120mg of Lumateperone compared, 4mg of Risperdal, and a placebo found that Lumateperone significantly decreased the total Positive and Negative Syndrome Scale (PANSS) from baseline. Safety analysis of this study also found that Lumateperone was not associated with EPS or significant weight gain. Another study found that 42mg of Lumateperone significantly decreased PANSS score over placebo and 28mg of Lumateperone with associated TEAEs of somnolence, sedation, fatigue, and constipation. In an open-label safety, patients were switched from their current antipsychotic to Lumateperone and then switched back to their previous treatment after six weeks. PATIENTS were found to have statistically significant improvements in metabolic parameters, weight, and endocrine parameters, which were all lost when they were switched back to their previous treatment and their schizophrenic symptoms at pre-trial levels or improved them while on Lumateperone. In a continuation of the previous study over 12 months, 4 TEAEs occurred in 5% or more of the participants: diarrhea, dry mouth, weight decrease, and headache. Prolactin, metabolic labs, BMI, and weight all decreased as compared to the standard of care. Pooled studies revealed EPS related TEAEs were less frequent in patients receiving 42 mg lumateperone over Risperdal. Another pooled study looked at the safety profile; they found patients treated with lumateperone, two TEAEs occurred at twice the placebo rate and at a rate of 5% or more: dry mouth (5% vs. 2.2%) and sedation (24.1% vs. 10.0%) though TEAE discontinuation rates were lower than with Risperdal. Summary: Taken together, data from these trials suggest that lumateperone can effectively treat positive symptoms, negative symptoms, and cognitive dysfunction in schizophrenia. Lumateperone entrance to the market introduces an innovative way to treat schizophrenia featuring both a novel mechanism of action and a markedly reduced side effect profile. Further research is needed to determine the efficacy of Lumateperone in treating bipolar disorder in addition to schizophrenia.