Lurasidone

Nowadays, about 90% of new drug candidates under development are poorly bioavailable due to their low solubility and/or permeability. Herein, w e introduce a natural liquid small molecule trans-anethole (TA) into drug-polymer system lurasidone (LUS)-poly (1-vinylpyrrolidone-co-vinyl acetate) (VA64), notably improving the compatibility of components for the successful preparation of amorphous solid dispersion (ASD) and facilitating the formation of self-emulsifying drug delivery system (SEDDS) during dissolution...

PURPOSE: Lurasidon is a relatively new, second-generation antipsychotic drug with an interesting receptor profile. It is considered to be safe and has a low risk of side effects. It is a substance with a multi-receptor mechanism of action: it mainly blocks dopaminergic D2 and serotonergic 5-HT2A receptors. According to the Summary of Product Characteristics, the adverse reaction of neutropenia was too rare to enable the estimation of its frequency. CASE DESCRIPTION: A case of 39-year-old patient is presented in the article, diagnosed with paranoid schizophrenia, who developed neutropenia as a result of treatment with lurasidone...

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Background: A liquid chromatography-tandem mass spectrometry method for quantifying lurasidone in rat dried blood spot (DBS) samples was developed. Method: The analyte was extracted from DBSs using the liquid-liquid extraction method. Chromatographic separation was achieved using a C18, Phenomenex, 150 × 4.6 mm, 3.0 μm column. The mobile phase composed of methanol, acetonitrile and water (70:10:20 v/v/v) with 0.1% heptafluorobutyric acid performed well in terms of reducing the matrix effect and achieving shorter retention time...

In the present study, a reliable LC-QTOF-MS method was developed and employed for the separation and characterization of process-related substances and forced degradation products of Lurasidone hydrochloride. The chromatographic separation was carried out using an Agilent Poroshell 120 Bonus-RP C18 column (100 mm × 4.6 mm, 2.7 µm) and a mobile phase consisting of a gradient elution of 10 mM ammonium formate solution and methanol. The degradation studies followed the guidelines outlined in ICH Q1A (R2)...

A bioanalytical method was developed and validated for determining lurasidone (LUR) in rat plasma. The analyte and internal standard were extracted from rat plasma using a liquid-liquid extraction method. The mobile phase consisted of methanol, acetonitrile and water, with an ion pairing agent, 0.1% heptafluorobutyric acid, added to minimise the matrix effect. The detection was achieved using a tandem mass spectrometer (API 2000) in positive ion multiple reaction monitoring mode. All parameters were validated, including selectivity, specificity, carry-over effect, linearity, precision, accuracy, matrix effect, sensitivity and stability...

The aim of this study was to investigate the impacts of 24 variants of recombinant human CYP3A4 and drug interactions on the metabolism of lurasidone. In vitro, enzymatic reaction incubation system of CYP3A4 was established to determine the kinetic parameters of lurasidone catalyzed by 24 CYP3A4 variants. Then, we constructed rat liver microsomes (RLM) and human liver microsomes (HLM) incubation system to screen potential anti-tumor drugs that could interact with lurasidone and studied its inhibitory mechanism...

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The objective of this case report is to describe and document the use of transcranial magnetic stimulation (TMS) to aid in the treatment of bipolar II disorder. A 35-year-old male with a past medical history of attention-deficit/hyperactivity disorder (ADHD), post-traumatic stress disorder (PTSD), severe depression, and bipolar II disorder was presented to an outpatient psychiatric clinic 1.5 years after his initial TMS treatment for TMS maintenance therapy. He reported feeling depressed, brain fogginess, loss of concentration, fatigue, and constant changes in moods...

No abstract text is available yet for this article.

Exposure to stressful experiences accounts for almost half of the risk for mental disorders. Hence, stress-induced alterations represent a key target for pharmacological interventions aimed at restoring brain function in affected individuals. We have previously demonstrated that lurasidone, a multi-receptor antipsychotic drug approved for the treatment of schizophrenia and bipolar depression, can normalize the functional and molecular impairments induced by stress exposure, representing a valuable tool for the treatment of stress-induced mental illnesses...

INTRODUCTION: Adverse event (AE) data in randomized controlled trials (RCTs) allow quantification of a drug's safety risk relative to placebo and comparison across medications. The standard US label for Food and Drug Administration-approved drugs typically lists AEs by MedDRA Preferred Term that occur at ≥ 2% in drug and with greater incidence than in placebo. We suggest that the drug label can be more informative for both patients and physicians if it includes, in addition to AE incidence (percent of subjects who reported the AE out of the total subjects in treatment), the absolute prevalence (percent of subject-days spent with an AE out of the total subject-days spent in treatment) and expected duration (days required for AE incidence to be reduced by half)...

IMPORTANCE: Bipolar disorder affects approximately 8 million adults in the US and approximately 40 million individuals worldwide. OBSERVATIONS: Bipolar disorder is characterized by recurrent episodes of depression and mania or hypomania. Bipolar depressive episodes are similar to major depressive episodes. Manic and hypomanic episodes are characterized by a distinct change in mood and behavior during discrete time periods. The age of onset is usually between 15 and 25 years, and depression is the most frequent initial presentation...

This review aims to provide a comprehensive overview of the current literature on the drug design, development, and therapy of lurasidone for the treatment of schizophrenia. Lurasidone has antagonistic effects on the dopamine D2 , 5-hydroxytryptamine (5-HT)2A , and 5-HT7 receptors and a partial agonistic effect on the 5-HT1A receptor with low affinities for muscarinic M1 , histamine H1 , and a1 adrenergic receptors. The receptor-binding profile of lurasidone is thought to be associated with fewer side effects such as anticholinergic effects, lipid abnormalities, hyperglycemia, and weight gain...

No abstract text is available yet for this article.

Lurasidone is a second-generation antipsychotic drug used to treat schizophrenia, mania, and bipolar disorder. The drug is an antagonist of the 5-HT2A and D2 receptors. No effect of lurasidone on the voltage-gated K+ (Kv) channels has yet been identified. Here, we show that lurasidone inhibits the vascular Kv channels of rabbit coronary arterial smooth muscle cells in a dose-dependent manner with an IC50 of 1.88 ± 0.21 μM and a Hill coefficient of 0.98 ± 0.09. Although lurasidone (3 μM) did not affect the activation kinetics, the drug negatively shifted the inactivation curve, suggesting that the drug interacted with the voltage sensors of Kv channels...

BACKGROUND: Bipolar depression constitutes a major public health problem due to its substantial burden of disease. Although pharmacological interventions are available, guidelines required updated evidence synthesis to improve their current recommendations. In order to inform evidence-based prescribing, we investigated the comparative efficacy and tolerability of pharmacological interventions for acute bipolar depression. METHODS: We conducted a systematic review and network meta-analysis...

BACKGROUND: We tested the hypothesis that, after initial improvement with intravenous ketamine in patients with bipolar disorder (BD) with severe depression and acute suicidal thinking or behavior, a fixed-dose combination of oral D-cycloserine (DCS) and lurasidone (NRX-101) can maintain improvement more effectively than lurasidone alone. METHODS: This was a multi-center, double-blind, twostage, parallel randomized trial. Adult BD patients with depression and suicidal ideation or behavior were infused with ketamine or saline (Stage 1); those who improved were randomized to a fixed-dose combination of DCS and lurasidone vs...

Obsessive-compulsive disorder (OCD) is a pervasive disabling disorder that may overlap with other psychiatric conditions, including anorexia nervosa. Recent guidelines recommend low doses of second-generation antipsychotics as add-on therapy to selective serotonin reuptake inhibitors (SSRIs) for those patients presenting OCD who display residual symptomatology. Here we report a clinical case of a 45-years-old woman affected by severe OCD in comorbidity with anorexia nervosa, restrictive type (AN-r), treated with fluoxetine (titrated up to 40 mg/day) in augmentation with low doses of lurasidone (37 mg/day)...

Somnolence is a common adverse effect of antipsychotic drugs used to treat psychotic disorders. It causes problems in many areas of life, such as gainful employment, driving, childcare, and social interactions. Somnolence is a major problem for a relatively new antipsychotic drug, lurasidone, whose dose-effect relationship remains unclear. Based on data from a bioequivalence study of two 40 mg lurasidone hydrochloride tablets, we designed two case-control studies to explore the correlation between somnolence and exposure to lurasidone and determine the factors associated with lurasidone-induced somnolence...