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loxapine (Adasuve / loxapine, Staccato / AZ004)

✓ Approved

Teva Pharmaceutical Industries Ltd. · DRD2 · 小分子

什么是 loxapine？

loxapine 是一种小分子，由Teva Pharmaceutical Industries Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Inhaled。

药物档案

商品名Adasuve, loxapine, Staccato, AZ004
公司Teva Pharmaceutical Industries Ltd.
药物类别小分子
分子靶点DRD2
给药途径Inhaled
状态Approved
来源： ClinicalTrials.gov, Teva Pharmaceutical Industries Ltd.

作用机制

分子靶点

loxapine 作用于 1 个分子靶点：

DRD2dopamine receptor D2 (D2DR, D2R)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

loxapine 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersAgitation✓ Approved

相关研究文献

PubMedNeurourology and urodynamics2026-09-07

Pelvic Floor Dysfunctions in Children With Lower Urinary Tract Dysfunction and Relationship With Urine Flow.

Dayanç Murat M, Ozturk Asli A, Kopru Burak B, Asik Rabia R et al.

Pelvic floor muscle (PFM) dynamics play a significant role alongside bladder and rectal dynamics in the pathophysiology of lower urinary tract dysfunction (LUTD) in children. This study aimed to determine PFM activities (PFMA), including resting tone and contractile functions, of LUTD subtypes in children according to their voiding patterns. 160 children presenting to our clinic with symptoms of lower pelvic floor voiding (LUTD) were evaluated using noninvasive diagnostic methods, and LUTD subtypes were determined. Based on voiding patterns, 31 had intermittent, 59 had staccato, 28 had tower, 31 had bell and 11 had plateau voiding pattern. 18 healthy children served as a control group and also exhibited bell curve voiding. PFMA was measured using superficial electrodes after voiding. Children performed five cycles of 5-s relaxation followed by 5-s voluntary PFM contraction, resulting in a total recording period of 50 s. Mean relaxation and contraction EMG values were recorded for analysis. According to PFMA measurements, pelvic floor dysfunction (PFD) subtypes defined and frequencies determined. According to the LUTD subtype, the frequency of pelvic floor overactivity (PFO) ranged from 59% to 86%, and the overall frequency of contractile dysfunctions (Nonfunctional or weak functional pelvic floor) ranged from 64% to 78%. As the voiding pattern improved, the resting tone decreased and normalized, thus the frequency of PFO reduced from 84% to 45% (p = 0.0001). The measurement of PFMA enables the identification of PFD subtypes in children with LUTD. The pathophysiology of LUTD can be better understood noninvasively.

PMID 42703842
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PubMed[Nihon koshu eisei zasshi] Japanese journal of public health2026-09-06

[Comparison of pertussis incidence trends before and after the COVID-19 pandemic: Investigation of factors behind the surge in pertussis cases in Kanagawa Prefecture (Week 1, 2018 - Week 33, 2025)].

Kimura Mutsumi M, Kaneto Chie C, Ito Mai M, Shinohara Ryosuke R et al.

Objective　To investigate the causes of the sharp increase in pertussis cases, by comparing the trends in pertussis incidence in Kanagawa Prefecture before and after the COVID-19 pandemic.Methods　Epidemiological data of pertussis cases reported in Kanagawa Prefecture from epidemiological week 1 of 2018 to week 33 of 2025 were examined based on infectious disease surveillance. Since changes in pertussis trends may have been influenced by behavioral changes that were implemented during the COVID-19 pandemic, such as droplet infection prevention and social distancing, the study period was divided into two sections: before and after the pandemic. The number of cases was compared across variables, including age group, vaccination history, symptoms, and diagnostic methods.Results　A pertussis outbreak was observed between 2018 and 2020, and a large-scale outbreak starting in 2024 continued to persist as of week 33 of 2025. Comparing the periods before and after the COVID-19 pandemic, the age group with the highest number of case reports shifted from children aged 5-10 years to those aged 10-15 years. Moreover, the number of reported cases has decreased in infants under 6 months of age, who are at the highest risk of severe complications from pertussis. Regarding vaccination history, in both time frames, the proportion of cases with "four doses received" was the highest; after the COVID-19 pandemic, an increase in the number of cases for those with four doses of DPT or DPT-IPV vaccines was observed in the 7-15 age group. Regarding symptoms, the percentage of patients with nocturnal cough, dyspnea, staccato, whoop, vomiting, apnea, cyanosis, and leukocytosis decreased. In terms of diagnostic methods, the frequency of genetic testing and rapid diagnostic tests increased compared to serological techniques.Conclusion　Factors contributing to the sharp increase in pertussis cases included the accumulation of susceptible individuals due to droplet and contact infection control measures and behavioral restrictions during the COVID-19 pandemic, waning immunity due to the time elapsed following pertussis vaccination, a possible increase in the number of reported cases due to an expanded set of diagnostic methods, and an increase in macrolide-resistant Bordetella pertussis strains. Advancing the starting age of routine vaccinations to 2 months contributed to the prevention of infant pertussis. However, additional DPT vaccinations at the ages of 5-7 and 11-12 years, as recommended by the Japanese Pediatric Society, are considered necessary.

PMID 42702539
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PubMedJournal of voice : official journal of the Voice Foundation2026-09-03

Comparison of Vertical Laryngeal Positions Between Classical Turkish Music and Classical Western European Opera Singers.

Kasapbaşı Fidan Kurt FK, Sağer Turan T, Yelken Kürşat K

This study aims to investigate the Vertical Laryngeal Position (VLP) used by professional Classical Turkish Music (CTM) and Classical Western European Opera (CWEO) singers during singing using endoscopic imaging techniques, and to determine whether there is a significant difference in VLP between these two vocal disciplines. The study included a total of 13 professional singers (7 from CTM, 6 from CWEO) with at least 10 years of experience. Participants were asked to perform various vocal exercises (staccato/legato in low, medium, and high ranges) as well as a repertoire piece reflecting the stylistic characteristics of their genre during video-laryngostroboscopy (VLS). The obtained video recordings were viewed in a blinded manner by three Otorhinolaryngology (ENT) professors specializing in laryngology, who independently scored VLP levels on a scale of 1 to 5. Data were analyzed comparatively using statistical methods. Comparative analysis revealed statistically significant differences in VLP between the two groups. It was determined that the laryngeal positions of the CTM group were significantly higher compared to the CWEO (Opera) group during repertoire performance ($P = 0.048$), low-range staccato exercises ($P = 0.039$), and low-range legato exercises ($P = 0.028$) ($P < 0.05$). No significant difference was observed between the groups in medium and high-frequency exercises ($P > 0.05$). This study presents objective data on the VLP characteristics of CTM performers. The findings indicate that CTM singers use a significantly higher laryngeal position compared to CWEO singers, particularly during repertoire performance and in low tones. However, it is noteworthy that this difference disappears at high frequencies. While this divergence in low tones can be explained by genre-specific timbral preferences, the similarity in high tones is thought to stem from the combined effect of the obligatory nature of laryngeal physiology and the Western-based voice training curriculum implemented in conservatories in Türkiye. These data emphasize the importance of genre-specific approaches in voice pedagogy and therapy processes.

PMID 42686454
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PubMedJournal of aerosol medicine and pulmonary drug delivery2026-08-07

Preclinical Development of a Dry Powder Formulation of Loxapine for Intranasal Delivery.

Shields Paul P, Rossi Irene I, Schwotzer Daniela D, Kuehl Philip J PJ et al.

Acute agitation (AA) is a common symptom of psychiatric conditions such as bipolar disorder and schizophrenia, resulting in 1.7 million emergency room visits per year in the United States. Loxapine, administered by inhalation, is an approved treatment for such scenarios. A boxed warning for bronchospasm when administered via inhalation limits its use to inpatient settings, making effective treatment for AA in outpatient settings an unmet need. The objective of this study was to develop and identify a lead intranasal dry powder formulation for outpatient treatment of AA. Seven spray-dried nasal powders (Formulations A-G) consisting of loxapine succinate (Medichem, ES) and various excipients were manufactured and filled in a Unidose Nasal Powder system (Aptar Pharma, FR). In this pharmacokinetic study with non-compartmental analysis, formulations were evaluated both in vitro and in vivo (n = 4 non-human primates [NHPs]). Formulations were characterized by yield, assay, water content, particle size distribution, emitted dose, and impactor-sized mass. Formulation B, comprising mannitol and hypromellose with 30% loxapine by weight, was identified as the lead candidate. In the in vivo portion of the study, all formulations were well tolerated. The plasma versus time profile for the NHP study indicated that Formulation B achieved the greatest extent of absorption (203.9 ng/mL*h) compared to the intravenous (control) formulation (231.5 ng/mL*h), each administered as a 3 mg dose. The full pharmacokinetic results for all formulations showed similar rapid absorption following dosing, although the area under the concentration-time curve and maximum concentration were lower than those observed with Formulation B. All formulations had similar apparent terminal half-lives. Formulation B showed clear advantages both in vitro and in vivo, supporting its suitability for further development as an outpatient treatment for AA in schizophrenia and bipolar disorder.

PMID 42566289
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PubMedEpilepsia2026-07-19

Progress report on new epilepsy treatments: A summary of the Eighteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XVIII). II. Treatments in more advanced clinical development.

Bialer Meir M, Johannessen Landmark Cecilie C, Koepp Matthias J MJ, Perucca Emilio E et al.

This article summarizes data for 13 investigational treatments for which at least preliminary seizure outcome data in patients with epilepsy were reported at the Eighteenth Eilat Conference on New Antiepileptic Drugs and Devices held in Madrid, Spain, on May 3-6, 2026. The treatments reviewed include bexicaserin, a selective 5-hydroxytryptamine (5-HT, serotonin) type 2C (5-HT2C) receptor superagonist investigated as a treatment for developmental and epileptic encephalopathies (DEEs); BMB-101, a selective 5-HT2C receptor agonist investigated for the treatment of absence seizures and DEEs; elsunersen, an antisense oligonucleotide designed for the treatment of early-onset SCN2A-DEE; EPX-100 (clemizole hydrochloride), an antihistamine endowed with agonist activity at 5-HT2A and 5-HT2B receptors, repurposed as a treatment for DEEs; ES-481, an antagonist of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors containing the transmembrane AMPA receptor regulatory protein γ8 (TARP-γ8), under investigation for the treatment of drug-resistant epilepsy; ETX-101, a gene therapy in development for the treatment of SCN1A-positive Dravet syndrome; PrevEp-006 (intranasal seletracetam), a synaptic vesicle glycoprotein 2A (SV2A) ligand under investigation as an acute seizure rescue therapy; radiprodil, a negative allosteric modulator that binds to the GluN2B subunit of the N-methyl-D-aspartate (NMDA) receptor, in development for the treatment of seizures and other symptoms associated with GRIN-related neurodevelopmental disorder, tuberous sclerosis complex, and focal cortical dysplasia type II; RAP-219, a selective negative allosteric modulator of TARP-γ8, in development for drug-resistant focal epilepsy; relutrigine, a selective disease-state sodium channel modulator investigated as a treatment for SCN2A- and SCN8A-DEE; Staccato Alprazolam, a breath-actuated device that delivers alprazolam to the lungs for rapid seizure termination; vormatrigine, a functionally selective sodium channel modulator in development for the treatment of focal seizures; and zorevunersen, an antisense oligonucleotide engineered to restore endogenous Nav1.1 protein expression, investigated for the treatment of Dravet syndrome. Overall, the evidence reviewed justifies expectations for improved health outcomes for the millions of children and adults with epilepsy who do not fully benefit from existing therapies.

PMID 42470359
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PubMedWorld journal of urology2026-06-25

Irritable bowel syndrome subtype predicts treatment response and defines distinct mechanistic phenotypes in OAB-IBS comorbidity: a prospective observational study.

Sun Qi Q, Gao Yubo Y, Shi Xinhang X, Xie Ming M et al.

To investigate the heterogeneity of treatment response in patients with concomitant Overactive Bladder (OAB) syndrome and Irritable Bowel Syndrome (IBS), including diarrhea-predominant (IBS-D), constipation-predominant (IBS-C), and mixed-type (IBS-M), by stratifying outcomes by both treatment strategy and IBS subtype. We hypothesized that IBS subtype would predict therapeutic response and define distinct mechanistic phenotypes. In this prospective, observational cohort study (N = 144, screened from 259), patients were allocated to one of four non-randomized cohorts: OAB-Targeted Monotherapy (OAB-TM, n = 45), OAB-Targeted Dual Therapy (OAB-TD, n = 29), IBS-Targeted Monotherapy (IBS-TM, n = 47), or IBS-Targeted Dual Therapy (IBS-TD, n = 23). Outcomes included changes in OABSS, IBS-SSS, PHQ-9, GAD-7, and QOL scores over 8 weeks. Efficacy was compared using ANCOVA, adjusted for baseline scores. Objective data from uroflowmetry parameters and baseline predictors of response were analyzed. Dual therapy demonstrated superior improvement over monotherapy across all symptom, mood, and QOL domains. However, stratified analysis revealed significant heterogeneity. In the IBS-targeted cohort, the superiority of dual therapy for OAB improvement was highly significant in the IBS-D subtype but not in IBS-M or IBS-C subtypes. This corresponded to distinct baseline uroflowmetry parameters: IBS-D patients typically showed high-peak tower-shaped curves, while IBS-C patients showed staccato patterns. Furthermore, baseline anxiety (GAD-7) and depression (PHQ-9) scores significantly predicted OAB cross-organ improvement in the IBS-TM cohort. OAB-IBS comorbidity is not a monolithic entity but comprises distinct clinical phenotypes (pelvic floor-driven, central sensitization-driven, bladder-primary). These findings suggest that a uniform treatment protocol may be suboptimal, supporting a precision-medicine framework where management is tailored based on the patient's specific IBS subtype.

PMID 42347939
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