Update on the development of lurasidone as a treatment for patients with acute schizophrenia

Yasui‐Furukori, Norio

doi:10.2147/dddt.s11180

Cited by 14 publications

(4 citation statements)

References 64 publications

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“…Although lurasidone is reported to induce modest, dose-dependent PRL elevations [ 400 , 401 ], especially at the beginning of treatment [ 402 ], as well as HPRL in some patients [ 71 , 403 , 404 ], in many patients it seems to be associated with no clinically meaningful PRL alterations [ 71 , 405 – 408 ].…”

Section: Prl and Antipsychoticsmentioning

confidence: 99%

The Effects of Novel and Newly Approved Antipsychotics on Serum Prolactin Levels: A Comprehensive Review

et al. 2014

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Since the 1970s, clinicians have increasingly become more familiar with hyperprolactinemia (HPRL) as a common adverse effect of antipsychotic medication, which remains the cornerstone of pharmacological treatment for patients with schizophrenia. Although treatment with second-generation antipsychotics (SGAs) as a group is, compared with use of the first-generation antipsychotics, associated with lower prolactin (PRL) plasma levels, the detailed effects on plasma PRL levels for each of these compounds in reports often remain incomplete or inaccurate. Moreover, at this moment, no review has been published about the effect of the newly approved antipsychotics asenapine, iloperidone and lurasidone on PRL levels. The objective of this review is to describe PRL physiology; PRL measurement; diagnosis, causes, consequences and mechanisms of HPRL; incidence figures of (new-onset) HPRL with SGAs and newly approved antipsychotics in adolescent and adult patients; and revisit lingering questions regarding this hormone. A literature search, using the MEDLINE database (1966–December 2013), was conducted to identify relevant publications to report on the state of the art of HPRL and to summarize the available evidence with respect to the propensity of the SGAs and the newly approved antipsychotics to elevate PRL levels. Our review shows that although HPRL usually is defined as a sustained level of PRL above the laboratory upper limit of normal, limit values show some degree of variability in clinical reports, making the interpretation and comparison of data across studies difficult. Moreover, many reports do not provide much or any data detailing the measurement of PRL. Although the highest rates of HPRL are consistently reported in association with amisulpride, risperidone and paliperidone, while aripiprazole and quetiapine have the most favorable profile with respect to this outcome, all SGAs can induce PRL elevations, especially at the beginning of treatment, and have the potential to cause new-onset HPRL. Considering the PRL-elevating propensity of the newly approved antipsychotics, evidence seems to indicate these agents have a PRL profile comparable to that of clozapine (asenapine and iloperidone), ziprasidone and olanzapine (lurasidone). PRL elevations with antipsychotic medication generally are dose dependant. However, antipsychotics having a high potential for PRL elevation (amisulpride, risperidone and paliperidone) can have a profound impact on PRL levels even at relatively low doses, while PRL levels with antipsychotics having a minimal effect on PRL, in most cases, can remain unchanged (quetiapine) or reduce (aripiprazole) over all dosages. Although tolerance and decreases in PRL values after long-term administration of PRL-elevating antipsychotics can occur, the elevations, in most cases, remain above the upper limit of normal. PRL profiles of antipsychotics in children and adolescents seem to be the same as in adults. The hyperprolactinemic effects of antipsychotic medication are mostly correlated with their affi...

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Section: Prl and Antipsychoticsmentioning

confidence: 99%

The Effects of Novel and Newly Approved Antipsychotics on Serum Prolactin Levels: A Comprehensive Review

et al. 2014

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“…50 Lurasidone's receptor profile suggests its potential to exert a pro-cognitive action through the blockade of serotonin receptors 5-HT 7 and 5-HT 1A . 52 Lurasidone significantly improved response rates in animal models of cognitive ability, learning and memory (Table 4). [53][54][55][56][57][58][59] The same positive effects have been also reported in a double-blind placebo-controlled study that evaluated change in cognitive performance and functional capacity in patients with schizophrenia treated with lurasidone and quetiapine XR over a 6-week period, followed by a 6-month extension.…”

Section: Reason For Consultationmentioning

confidence: 99%

Lurasidone for the treatment of schizophrenia in adult and paediatric populations

Guilera¹,

Pascual²,

Blasco³

et al. 2023

DIC

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Schizophrenia is a common debilitating disorder characterized by significant impairments in how reality is perceived, combined with behavioural changes. In this review, we describe the lurasidone development programme for adult and paediatric patients. Both the pharmacokinetic and pharmacodynamic characteristics of lurasidone are revisited. In addition, pivotal clinical studies conducted on both adults and children are summarized. Several clinical cases, which demonstrate the role of lurasidone in real-world practice, are also presented. Current clinical guidelines recommend lurasidone as the first-line treatment in the acute and long-term management of schizophrenia in both adult and paediatric populations.

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“…Lurasidone hydrochloride (LRD) is an atypical antipsychotic drug approved by the FDA for treating schizophrenia and bipolar disorder (manic depression) in adults and adolescents [ 1 ]. It has been reported to be capable of stabilizing schizophrenia after a short-term usage (~6 weeks) by clinical studies in adult patients using a placebo-controlled, randomized, and double-blinded scheme [ 2 ]. It has also shown anxiolytic and antidepressant effects through the combined blockade of the dopamine type-2 (D2) and serotonin type 2A (5-HT 2A ) receptors [ 3 ].…”

Section: Introductionmentioning

confidence: 99%

“…It presents low extrapyramidal activation and neuromotor detriment, along with low central nervous system depression, thus showing few adverse effects. In addition, it has minimal muscarinic and α1 receptor inactivation through blockade [ 2 ]. This profile suggests a minor propensity towards weight gain and metabolic dysfunction, while it has high potential for improving cognitive deficits related to schizophrenia [ 4 ].…”

Section: Introductionmentioning

confidence: 99%

Improving Lurasidone Hydrochloride’s Solubility and Stability by Higher-Order Complex Formation with Hydroxypropyl-β-cyclodextrin

et al. 2023

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The biopharmaceutical classification system groups low-solubility drugs into two groups: II and IV, with high and low permeability, respectively. Most of the new drugs developed for common pathologies present solubility issues. This is the case of lurasidone hydrochloride—a drug used for the treatment of schizophrenia and bipolar depression. Likewise, the stability problems of some drugs limit the possibility of preparing them in liquid pharmaceutical forms where hydrolysis and oxidation reactions can be favored. Lurasidone hydrochloride presents the isoindole-1,3-dione ring, which is highly susceptible to alkaline hydrolysis, and the benzisothiazole ring, which is susceptible to a lesser extent to oxidation. Herein, we propose to study the increase in the solubility and stability of lurasidone hydrochloride by the formation of higher-order inclusion complexes with hydroxypropyl-β-cyclodextrin. Several stoichiometric relationships were studied at between 0.5 and 3 hydroxypropyl-β-cyclodextrin molecules per drug molecule. The obtained products were characterized, and their solubility and stability were assessed. According to the obtained results, the formation of inclusion complexes dramatically increased the solubility of the drug, and this increased with the increase in the inclusion ratio. This was associated with the loss of crystalline state of the drug, which was in an amorphous state according to infrared spectroscopy, calorimetry, and X-ray analysis. This was also correlated with the stabilization of lurasidone by the cyclodextrin inhibiting its recrystallization. Phase solubility,1H-NMR, and docking computational characterization suggested that the main stoichiometric ratio was 1:1; however, we cannot rule out a 1:2 ratio, where a second cyclodextrin molecule could bind through the isoindole-1,3-dione ring, improving its stability as well. Finally, we can conclude that the formation of higher-order inclusion complexes of lurasidone with hydroxypropyl-β-cyclodextrin is a successful strategy to increase the solubility and stability of the drug.

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Update on the development of lurasidone as a treatment for patients with acute schizophrenia

Cited by 14 publications

References 64 publications

The Effects of Novel and Newly Approved Antipsychotics on Serum Prolactin Levels: A Comprehensive Review

The Effects of Novel and Newly Approved Antipsychotics on Serum Prolactin Levels: A Comprehensive Review

Lurasidone for the treatment of schizophrenia in adult and paediatric populations

Improving Lurasidone Hydrochloride’s Solubility and Stability by Higher-Order Complex Formation with Hydroxypropyl-β-cyclodextrin

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