Lumateperone in schizophrenia: a profile of its use

Frampton, James E.

doi:10.1007/s40267-020-00780-4

Cited by 4 publications

(8 citation statements)

References 18 publications

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“…A search of items for 'ITI-007' and 'lumateperone' on PubMed, ScienceDirect, Web of Science, Google Scholar, and www.clinicaltrials.gov generated extant publications on lumateperone in schizophrenia. As several reviews of lumateperone have utilized the available publications from investigators who have financial conflicts of interest to present articles that emphasize the potential benefits, 5,[24][25][26][27][28][29][30][31] we sought to construct a selective review assessing the trustworthiness of the available evidence on the pharmacodynamics, pharmacokinetics, pharmacotherapy, and clinical trials of lumateperone in schizophrenia in order to provide expert insight for the possible role of this agent for people with schizophrenia. To enhance the trustworthiness of this article, we have limited ourselves to published articles and abstracts.…”

Section: Data Sources and Searchesmentioning

confidence: 99%

“…21,38,43,44 Mechanism of action Lumateperone is a serotonin transport inhibitor and a potent antagonist at serotonin 5-HT 2A receptors 5,24,[45][46][47][48][49] acting as a presynaptic partial agonist and a postsynaptic antagonist at dopamine D 2 receptors, 5,50,51 and as a dopamine receptor phosphoprotein modulator. 5,22,28,[45][46][47][48][49] It is also a dopamine D 1 receptor-dependent indirect modulator of glutamatergic α-amino-3hydroxy-5-methyl-4-isoxazolepropionic acid 52 and N-methyl-D -aspartate (NMDA) GluN 2B receptors. 5,19,24,53,54…”

Section: Introduction To the Compoundmentioning

confidence: 99%

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The role of lumateperone in the treatment of schizophrenia

Syed

Brašić

2021

Therapeutic Advances in Psychopharmacology

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Schizophrenia is a devastating mental disorder resulting in marked morbidity and mortality despite the optimal use of all currently available interventions. For this reason, the release of lumateperone (CaptylaR), also known as ITI-007, an orally administered, atypical antipsychotic provided a welcome novel tool for clinicians to utilize precision medicine to tailor an optimal treatment plan to the specific needs of each person with schizophrenia. To generate a foundation for clinicians to assess the risks and benefits of lumateperone in relation to other interventions for schizophrenia, we conducted a search of items for ‘ITI-007’ and ‘lumateperone’ on PubMed, ScienceDirect, Web of Science, Google Scholar, and www.clinicaltrials.gov . We present a critical evaluation of the limited information about lumateperone for schizophrenia, its use approved by the US Food and Drug Administration. Lumateperone merits consideration for patients with treatment-resistant schizophrenia and for patients with schizophrenia who are vulnerable to developing metabolic dysfunction and movement disorders. On the other hand, lumateperone should not be used for (a) women who are pregnant or breastfeeding, children, adolescents, and elderly patients with dementia-related psychosis, (b) patients who are at risk for cerebrovascular diseases, (c) patients who use inducers and moderate or strong inhibitors of the cytochrome P450-3A4 (CYP3A4) isozyme, and (d) patients who use alcohol and other sedating agents. Clinical trials from multiple centers without financial conflicts of interest to market lumateperone are needed to directly compare and contrast lumateperone and other antipsychotic agents to generate trustworthy evidence to be assessed objectively by clinicians treating patients with schizophrenia. Future investigations will provide the foundations to identify the evidence for comprehensive evaluations of the role of lumateperone in the treatment of people with schizophrenia and other conditions.

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Section: Data Sources and Searchesmentioning

confidence: 99%

Section: Introduction To the Compoundmentioning

confidence: 99%

The role of lumateperone in the treatment of schizophrenia

Syed

Brašić

2021

Therapeutic Advances in Psychopharmacology

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“…However, the higher affinity of brexpiprazole could have a potential benefit in patients who suffer from nightmares, as seen by the α 1 R antagonistic effects of prazosin. Unlike the other atypical antipsychotics mentioned, lumateperone also has moderate affinity as an α 2 R antagonist (Blair, 2020; Frampton, 2020). This α 2 R antagonism may give lumateperone antidepressant properties similar to the antidepressant mirtazapine, which utilizes this pharmacodynamic property to lower depressive symptoms.…”

Section: Introductionmentioning

confidence: 99%

“…The capsule is available in 10.5 mg, 21 mg, and 42 mg (equivalent to lumateperone tosylate 60 mg). For the treatment of adults with schizophrenia and depressive episodes of bipolar, a dosage of 42 mg administered orally once daily is recommended (Frampton, 2020; Therapies, 2021). No titration dose is required.…”

Section: Introductionmentioning

confidence: 99%

“…Even though lumateperone has the weakest affinity for D 2 R, it demonstrates comparable antipsychotic activity at relatively low D 2 R occupancy to other atypical antipsychotics (e.g. aripiprazole, risperidone, olanzapine) (Frampton, 2020). This characteristic may allow lumateperone to have a relative low risk of excessive D2 antagonism unwanted adverse events such as EPS, especially akathisia, and hyperprolactinemia (Frampton, 2020).…”

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confidence: 99%

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Differentiating the third generation of antipsychotics: a focus on lumateperone’s similarities and differences

Munayco Maldonado,

Schwartz

2023

International Clinical Psychopharmacology

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The development of atypical antipsychotics has evolved to include newer pharmacodynamic properties. Lumateperone, aripiprazole, brexpiprazole, and cariprazine are all dopamine-2 receptor partial agonists with varying receptor affinities. This review aims to compare the clinical and pharmacodynamic differences among these four atypical antipsychotics, all of which are unique when compared to first- and second-generation antipsychotics. For consideration is further delineating these agents as being third-generation antipsychotics. PubMed searches were conducted to compile preclinical and clinical studies derived from animal models and human subjects. Information gathered included pharmacological mechanisms, clinical efficacy, future-oriented clinical approaches, and adverse effects. Efficacy for the shared indications of these drugs seems comparable. Differences among these drugs lie more in their adverse effect profiles. For example, lumateperone was found to have the lowest rate of weight gain while brexpiprazole was found to have the highest rate of weight gain associated with increased appetite. Aripiprazole had the lowest rates of extrapyramidal symptoms not including akathisia while cariprazine had the highest. All four agents reviewed have a variety of receptor affinities, which likely generates a variety of different adverse effects. This suggests that in any given patient, clinicians may see differential clinical effects.

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Crystal structure and X-ray powder diffraction data for Lumateperone tosylate

Liu,

Shi,

Liu

et al. 2023

Powder Diffr.

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X-ray powder diffraction data, unit-cell parameters, and space group for the Lumateperone tosylate, C24H29FN3O⋅C7H7O3S, are reported [a = 15.5848(10) Å, b = 6.0700(4) Å, c = 31.3201(14) Å, β = 96.544(5)°, V = 2943.58 Å3, Z = 4, and space group C2]. In each case, all measured lines were indexed and were consistent with the corresponding space group. The single-crystal data of Lumateperone tosylate is also reported, respectively [a = 15.626(3) Å, b = 6.0806(10) Å, c = 31.415(5) Å, β = 96.609(7)°, V = 2965.1(8) Å3, Z = 4, and space group C2]. The experimental powder diffraction pattern has been well matched with the simulated pattern derived from the single-crystal data with preferred orientation in the [002] direction (orientation coefficient = 0.75).

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Lumateperone in schizophrenia: a profile of its use

Cited by 4 publications

References 18 publications

The role of lumateperone in the treatment of schizophrenia

The role of lumateperone in the treatment of schizophrenia

Differentiating the third generation of antipsychotics: a focus on lumateperone’s similarities and differences

Crystal structure and X-ray powder diffraction data for Lumateperone tosylate

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