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bepotastine besilate (Talion OD)

✓ Approved

Mitsubishi Tanabe Pharma Corporation · HRH1 · 小分子

什么是 bepotastine besilate？

bepotastine besilate 是一种小分子，由Mitsubishi Tanabe Pharma Corporation研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Talion OD
公司Mitsubishi Tanabe Pharma Corporation
药物类别小分子
分子靶点HRH1
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Mitsubishi Tanabe Pharma Corporation

作用机制

分子靶点

bepotastine besilate 作用于 1 个分子靶点：

HRH1histamine receptor H1 (HH1R, H1R)
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

bepotastine besilate 针对 4 个适应症，涉及 3 个治疗领域。

治疗领域疾病/病症分期
Immune system disordersHypersensitivity✓ Approved
Skin and subcutaneous tissue disordersPruritus✓ Approved
Respiratory, thoracic and mediastinal disordersRhinitis allergic✓ Approved
Skin and subcutaneous tissue disordersUrticaria✓ Approved

相关研究文献

PubMedLangmuir : the ACS journal of surfaces and colloids2026-10-23

Correlating Force-Conductance-Structure in Au-1,8-Octanedithiol-Au Molecular Electronics.

Wang Huachuan H, Ma Xiangyu X, Li Qinrao Q, Rao Qi Q et al.

Because atomic-scale junction configurations cannot be directly resolved during break-junction measurements, simulations are needed to connect experimental force and conductance signatures with plausible interfacial structures. Here, we use configurational-bias Monte Carlo, driven molecular dynamics, and DFT+NEGF transport calculations to interpret the electromechanical response of Au-1,8-octanedithiol (ODT)-Au junctions measured by conductive atomic force microscopy break-junction experiments. Under cyclic stretching and compression with a modulation amplitude of 1.2 Å, reproducible force and conductance responses are observed. The simulations generate metastable configurations containing one, two, and three bridging ODT molecules and reproduce characteristic force ranges and conductance levels consistent with experiment. Structural analysis reveals configuration-dependent load distribution, junction deformation, molecular reorientation, and local Au-S coordination. The DFT+NEGF results further show that conductance modulation is governed mainly by changes in the Au-S contacts rather than deformation of the alkane backbone. These findings provide an atomistic interpretation of the measured electromechanical responses and clarify how junction configuration and contact rearrangement influence transport in Au-ODT-Au molecular junctions.

PMID 42918148
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PubMedPharmacology research & perspectives2026-10-17

Comparative Pharmacokinetics and Safety of Orally Disintegrating and Conventional Tablet Formulations of Zastaprazan in Healthy Subjects.

Kim Hyung-Gun HG, Kang Seunghyun S, Min Sunyoung S, Hong Heejoo H et al.

Zastaprazan, a potassium-competitive acid blocker, has been developed as an orally disintegrating tablet (ODT) to improve administration flexibility. This study evaluated the pharmacokinetics and safety of a single 20 mg dose of Zastaprazan ODT administered with or without water compared with the conventional tablet in healthy volunteers. In this open-label, randomized, single-dose, 6-sequence, 3-period crossover study, 54 healthy volunteers received a conventional tablet with water, an ODT with water, and an ODT without water. Serial blood samples were collected up to 36 h post-dose, and pharmacokinetic parameters were calculated using a non-compartmental method. Safety was assessed through adverse events, laboratory tests, vital signs, and electrocardiograms. Fifty-one subjects completed all periods. The geometric mean ratios (90% confidence intervals) of Cmax and AUCt were 95.05% (88.38%-102.21%) and 108.00% (100.50%-116.06%) for ODT without water versus the conventional tablet, and 90.85% (84.96%-97.16%) and 101.88% (96.69%-107.36%) for ODT with water versus the conventional tablet, respectively. All 90% confidence intervals were within the predefined bioequivalence range. Ka and Tmax showed similar patterns across treatments, and no apparent additional early systemic exposure was observed within 30 min following ODT administration. Two mild adverse events were reported in one subject, with no serious adverse events. Zastaprazan ODT administered either with or without water was pharmacokinetically equivalent to the conventional tablet, with no apparent additional early systemic exposure and no clinically meaningful safety concerns. Trial Registration: ClinicalTrials.gov: NCT07181538.

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PubMedThe Journal of allergy and clinical immunology2026-10-16

Comparative efficacy and safety of antihistamines, increased antihistamine dosing, and antihistamine adjuncts for chronic urticaria: a systematic review, dose-response, and network meta-analysis of randomized trials.

Chu Alexandro W L AWL, Zhao Irene X IX, Rayner Daniel G DG, Guyatt Gordon H GH et al.

Chronic urticaria is a common immune-mediated condition characterized by wheals (itch and hives), angioedema, or both, lasting for greater than six weeks. It is managed with H1 antihistamines as the first-line therapy. Fundamental unresolved questions remain regarding the comparative benefits and harms of antihistamines and their adjuncts, and of H1 antihistamine dose-escalation. To analyze the comparative benefits and harms of antihistamines and their adjuncts (H2 blockers or montelukast), and of H1 antihistamine dose-escalation. As part of updating the American Academy of Allergy, Asthma & Immunology and American College of Allergy, Asthma and Immunology Joint Task Force on Practice Parameters Chronic Urticaria guidelines, we searched MEDLINE, EMBASE, CENTRAL, and regulatory databases from inception to March 17, 2025, for randomized trials addressing antihistamines or their adjuncts for chronic urticaria. Paired reviewers independently screened records, extracted data, and assessed risk of bias. Random effects network and dose-response meta-analyses addressed urticaria activity (composed of itch and wheal scores), angioedema activity, urticaria-related quality of life, and harms including sedation. The GRADE approach informed certainty of evidence ratings. CRD42022367280. 211 trials (22,187 participants) evaluated 55 unique treatments. Bilastine, desloratadine, fexofenadine, and levocetirizine are among the most effective in improving overall urticaria activity, urticaria-related quality of life, and sleep disturbance. Cetirizine and loratadine are among the most effective in reducing overall urticaria activity and its subcomponents, with cetirizine also among the most effective in improving urticaria-related quality of life. Escalating from a single to quadruple daily dose may yield diminishing additional benefit. Second-generation agents as a class may be more effective than first-generation agents in improving urticaria activity and sleep disturbance. Sedation risk likely increases with higher doses, with first-generation agents (e.g., diphenhydramine, hydroxyzine) and doxepin among the most sedating; cetirizine, ketotifen, levocetirizine, and rupatadine among the intermediate sedating; and bepotastine, bilastine, desloratadine, ebastine, fexofenadine, and loratadine among the least sedating. Adding montelukast (moderate certainty) or an H2 blocker (very low certainty) to a second-generation agent may further reduce urticaria activity. For chronic urticaria, second-generation agents differ in their efficacy and safety. First-generation agents are less beneficial and more harmful. Escalating to higher daily doses may provide additional benefits but likely increases sedation.

PMID 42887704
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PubMedTrials2026-10-14

Evaluating sedation efficacy and perioperative safety of fospropofol disodium versus propofol in elderly patients undergoing elective TURP: study protocol for a randomized controlled trial.

Sui Hongyuan H, Wu Tong T, Gao Lijuan L, He Qingying Q et al.

Fospropofol disodium is the first novel water-soluble propofol prodrug in China. After administration, it is mainly converted to propofol by alkaline phosphatase on the surface of endothelial cells to exert its pharmacological effects. Compared with propofol, fospropofol disodium has the characteristics of longer duration of action, lower incidence of injection pain and adverse events related to the respiratory and circulatory systems, and no adverse reactions related to lipid metabolism. At present, there are few reports on the safety and efficacy of fospropofol disodium in the induction and maintenance of general anesthesia. Therefore, this study aims to evaluate the safety and efficacy of fospropofol disodium in routine anesthesia for elective surgery in the elderly, so as to provide new medication guidance for its application in the induction and maintenance stages of general anesthesia in the elderly population. Seventy elderly patients aged 65-85 years with American Society of Anesthesiologists (ASA) physical status II or III, scheduled for elective transurethral resection of the prostate under general anesthesia, will be enrolled. Patients will be randomly divided into the propofol group (group E) and the fospropofol disodium group (group F) using a random number table, with 35 cases in each group. Anesthesia induction: sufentanil 0.2-0.4 µg/kg and cisatracurium besilate 0.15 mg/kg will be administered intravenously. Group E will receive an intravenous bolus of propofol 1-1.5 mg/kg, while group F will receive an intravenous bolus of fospropofol disodium 10-15 mg/kg, both infused within 60 s. Tracheal intubation will be performed when the patient's Modified Observer's Assessment of Alertness/Sedation (MOAA/S) score decreases to 1 with BIS < 60 sustained for ≥3 min, followed by routine mechanical ventilation. For anesthesia maintenance, group E will receive continuous intravenous infusion of propofol 4-12 mg/(kg·h) and remifentanil 0.2-0.4 µg/(kg·min) via a syringe pump; group F will receive continuous intravenous infusion of fospropofol disodium 10-20 mg/(kg·h) and remifentanil 0.2-0.4 µg/(kg·min) via a syringe pump. During the operation, the infusion rates of maintenance anesthetics will be adjusted according to hemodynamic status to maintain blood pressure and heart rate fluctuations within 20% of the baseline values, and the Bispectral Index (BIS) value will be maintained between 40 and 60. After the operation, patients will be transferred to the post-anesthesia care unit (PACU). Primary outcomes of this study: success rate of sedation and time to onset of sedation. (1) perioperative indicators, (2) hemodynamic indices at each time point, (3) adverse reactions. Elderly patients undergoing transurethral resection of the prostate (TURP) are often complicated with multiple comorbidities, leading to a relatively high anesthetic risk. This trial takes the success rate of sedation and time to onset of sedation as the primary endpoints, to compare the application differences between fospropofol disodium and propofol. The aim of this study is to evaluate the safety and efficacy of fospropofol disodium in routine anesthesia for elective surgeries in the elderly population. The study was registered at the Chinese Clinical Trials Registry (ChiCTR2500115343) on December 24, 2025 ( http://www.chictr.org.cn/showproj.html?proj=294899 ).

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PubMedClinical pharmacology in drug development2026-10-09

Pharmacokinetic and Bioequivalence of Mirtazapine Orally Disintegrating Tablets: A Randomized, Crossover Study.

Liew Kai Bin KB, Yee Kar Ming KM, Nalaiya Jeyashanthini J, Amran Atiqah A et al.

The study aimed to assess the bioequivalence of a new generic orally disintegrating tablet (ODT) formulation containing mirtazapine 30 mg with the reference formulation, and to support biowaiver for an additional 15 mg strength. Fifty-five healthy Malaysian males completed an open-label, balanced, randomized, 2-treatment, 2-period, single oral dose study with a 14-day washout period under fasting conditions. Each participant received a single 30 mg dose of mirtazapine test or reference ODT. Plasma concentrations of mirtazapine up to 72 h post-dose were quantified using a validated high-performance liquid chromatography-tandem mass spectrometry detection method following a liquid-liquid extraction. Non-compartmental analysis was used to derive the pharmacokinetic parameters, which were then compared between the test and reference formulations using a multivariate analysis of variance. The pharmacokinetic parameters of the test formulation were not statistically different from the reference formulation. The 90% confidence intervals of mirtazapine for AUC0-72 and Cmax concentration were within 80%-125% based on the bioequivalence acceptance range criteria. The test and reference formulations of mirtazapine 30 mg ODT are bioequivalent and well tolerated under fasting conditions. These findings support the extrapolation of bioequivalence and the justification of a biowaiver for the additional mirtazapine ODT 15 mg strength.

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PubMedComputer methods in biomechanics and biomedical engineering2026-10-09

Comparing Maximally Collapsing Metric Learning and Optimized Tunable Q-Wavelet Transform for Schizophrenia Identification Using EEG Signals.

Djemili Rafik R

Electroencephalography (EEG) is a noninvasive technique for recording brain electrical activity and supporting the assessment of psychiatric disorders. This study proposes a framework for distinguishing individuals with Schizophrenia (SZ) from healthy subjects using EEG data. The approach employs a transformer based on Maximally Collapsing Metric Learning (MCML) applied to feature-vector matrices and compares it with optimized Tunable Q-Wavelet Transform (TQWT) decomposition. Eight nonlinear features are extracted from both approaches and evaluated using *k*-Nearest Neighbor (*k*-NN), Optimized Decision Tree (ODT), and Deep Neural Network (DNN) classifiers. Results achieve accuracies of 100%, 99.94%, and 99.91%, respectively, using one electrode channel.

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