Lumateperone: First Approval

Blair, Hannah A.

doi:10.1007/s40265-020-01271-6

Cited by 46 publications

(66 citation statements)

References 8 publications

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“…72,74 Ingestion of a high-fat meal leads to an approximate decrease in C max of 33%, and T max is extended to approximately 2 hours. 73,79 Dosages at 120 mg/day have not been shown to produce any statistically significant improvement in efficacy. When taken with a high-fat meal, the area under the plasma-concentration-time curve (AUC) increases by 9%.…”

Section: Pharmacokinetics/pharmacodynamics Absorption and Distributionmentioning

confidence: 96%

“…Lumateperone received approval in the USA to treat schizophrenia in adults in December 2019. 73 The most common adverse effects are mild, such as somnolence, constipation, sedation, and fatigue with the 42 mg recommended dose. 72 Serious adverse events include orthostatic hypotension, hyperglycemia, dyslipidemia, leukopenia, neutropenia, extrapyramidal disease, neuroleptic malignant syndrome, and tardive dyskinesia.…”

Section: Lumateperone Tosylate Drug Informationmentioning

confidence: 99%

“…74 The drug has a black-box warning for elderly patients with dementia-related psychosis who are at an increased risk for a serious cerebrovascular accident when taking the medication; lumateperone is not approved to treat patients with dementia-related psychosis. 73 It is contraindicated in patients with known hypersensitivity reactions to lumateperone (Caplyta FDA Label). Also, patients taking CYP3A4 inducers or moderate to potent CYP3A4 inhibitors are advised to avoid lumateperone.…”

Section: Lumateperone Tosylate Drug Informationmentioning

confidence: 99%

“…When taken with a high-fat meal, the area under the plasma-concentration-time curve (AUC) increases by 9%. 73 Steady-state is achieved in about five days, and the half-life of the drug is 13 to 21 hours. The volume of distribution of lumateperone is approximately 4.1 L/ kg following intravenous administration.…”

Section: Pharmacokinetics/pharmacodynamics Absorption and Distributionmentioning

confidence: 99%

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

Maini

Hollier

Gould

et al. 2021

Health Psychology Research

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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 FindingsSchizophrenia 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.

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Section: Pharmacokinetics/pharmacodynamics Absorption and Distributionmentioning

confidence: 96%

Section: Lumateperone Tosylate Drug Informationmentioning

confidence: 99%

Section: Lumateperone Tosylate Drug Informationmentioning

confidence: 99%

Section: Pharmacokinetics/pharmacodynamics Absorption and Distributionmentioning

confidence: 99%

See 2 more Smart Citations

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

Maini

Hollier

Gould

et al. 2021

Health Psychology Research

View full text Add to dashboard Cite

show abstract

“…Considering that the serotonin 5-HT2AR polymorphisms and altered functioning of these receptors are associated with psychosis and aggressiveness onset in AD patients, recent studies have been focused on the effects of pimavanserin, a selective inverse agonist of the 5-HT2AR (212) or lumateperone and brexpiprazole, two novel atypical antipsychotics acting as 5-HT2A antagonists. After showing promising efficacy in phase II RCTs, these drugs now face validation through phase III RCTs (213)(214)(215).…”

Section: Clinical Pharmacological Trials and Future Prospectsmentioning

confidence: 99%

Agitation and Dementia: Prevention and Treatment Strategies in Acute and Chronic Conditions

et al. 2021

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Agitation is a behavioral syndrome characterized by increased, often undirected, motor activity, restlessness, aggressiveness, and emotional distress. According to several observations, agitation prevalence ranges from 30 to 50% in Alzheimer's disease, 30% in dementia with Lewy bodies, 40% in frontotemporal dementia, and 40% in vascular dementia (VaD). With an overall prevalence of about 30%, agitation is the third most common neuropsychiatric symptoms (NPS) in dementia, after apathy and depression, and it is even more frequent (80%) in residents of nursing homes. The pathophysiological mechanism underlying agitation is represented by a frontal lobe dysfunction, mostly involving the anterior cingulate cortex (ACC) and the orbitofrontal cortex (OFC), respectively, meaningful in selecting the salient stimuli and subsequent decision-making and behavioral reactions. Furthermore, increased sensitivity to noradrenergic signaling has been observed, possibly due to a frontal lobe up-regulation of adrenergic receptors, as a reaction to the depletion of noradrenergic neurons within the locus coeruleus (LC). Indeed, LC neurons mainly project toward the OFC and ACC. These observations may explain the abnormal reactivity to weak stimuli and the global arousal found in many patients who have dementia. Furthermore, agitation can be precipitated by several factors, e.g., the sunset or low lighted environments as in the sundown syndrome, hospitalization, the admission to nursing residencies, or changes in pharmacological regimens. In recent days, the global pandemic has increased agitation incidence among dementia patients and generated higher distress levels in patients and caregivers. Hence, given the increasing presence of this condition and its related burden on society and the health system, the present point of view aims at providing an extensive guide to facilitate the identification, prevention, and management of acute and chronic agitation in dementia patients.

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Polypharmacology in Clinical Applications: Neurological Polypharmacology

Wang

Yang²

2022

Polypharmacology

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Lumateperone: First Approval

Cited by 46 publications

References 8 publications

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

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

Agitation and Dementia: Prevention and Treatment Strategies in Acute and Chronic Conditions

Polypharmacology in Clinical Applications: Neurological Polypharmacology

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