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aclidinium bromide + formoterol (Eklira+ formoterol / Duaklir / LAS 40464)

✓ Approved

Kyorin · ADRB2 · 小分子

什么是 aclidinium bromide + formoterol?

aclidinium bromide + formoterol 是一种小分子,由Kyorin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Eklira+ formoterol, Duaklir, LAS 40464
公司Kyorin
药物类别小分子
分子靶点ADRB2, CHRM3
给药途径Inhaled
状态Approved

作用机制

分子靶点

aclidinium bromide + formoterol 作用于 2 个分子靶点:

ADRB2adrenoceptor beta 2 (B2AR, ARB2)
CHRM3cholinergic receptor muscarinic 3 (HM3, PBS)
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

aclidinium bromide + formoterol 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
Respiratory, thoracic and mediastinal disordersChronic obstructive pulmonary disease✓ Approved

相关研究文献

PubMedAdvances in respiratory medicine2026-10-26

Deciphering the Benefits and Risks of Single-Inhaler Triple Therapy in COPD.

Kopitovic Ivan I, Dimic-Janjic Sanja S, Stjepanovic Mihailo M, Hromis Sanja S et al.

Single-inhaler triple therapy (SITT) combines an inhaled corticosteroid (ICS; for example, fluticasone furoate, budesonide, or beclometasone dipropionate), a long-acting β2-agonist (LABA; for example, vilanterol or formoterol fumarate), and a long-acting muscarinic antagonist (LAMA; for example, umeclidinium or glycopyrronium bromide) in one device. Triple pharmacological therapy reduces exacerbations in selected patients with chronic obstructive pulmonary disease (COPD), but its effects on mortality and cardiovascular outcomes remain uncertain. This structured narrative review summarizes randomized trials, observational comparative-effectiveness studies, target trial emulations, systematic reviews, and health technology assessments published between 2015 and 2026. We grouped the evidence by comparator: LABA/LAMA, ICS/LABA, multiple-inhaler triple therapy (MITT), and ICS continuation versus withdrawal, because each comparison addresses a different clinical question. Pivotal trials and evidence syntheses consistently showed fewer moderate-to-severe exacerbations with triple therapy, with reported rate ratios of approximately 0.69-0.93. Mortality signals from IMPACT and ETHOS are clinically important, but previous ICS use and ICS withdrawal among participants assigned to ICS-free comparators make these findings difficult to interpret. Observational cardiovascular findings are also uncertain because residual confounding, treatment selection, exposure misclassification, outcome misclassification, and differences in baseline disease severity limit causal interpretation. Compared with MITT, the main advantages of SITT are simpler treatment and possible improvements in adherence and persistence, not greater pharmacological potency. Treatment decisions should consider exacerbation history, repeated blood eosinophil counts, pneumonia risk, cardiovascular disease, previous ICS exposure and response, inhaler technique, device suitability, and patient preference. Trials in patients with documented absence of previous ICS use and well-designed target trial emulations are needed to determine whether the observed mortality and cardiovascular associations are causal.

PMID 42930048
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PubMedInorganic chemistry2026-10-26

Crystal Morphology of Luminescent Microcrystals Based on Eu(III) Coordination Polymers Changed by Surfactant Solutions.

Enokido Masaki M, Wang Mengfei M, Kitagawa Yuichi Y, Hasegawa Yasuchika Y

The morphological control of Eu(III) coordination polymers with intermolecular interactions between polymer chains was demonstrated with surfactants as molecular modulators. [Eu(hfa)3(m-dpb)]n coordination polymers (hfa; hexafluoroacetylacetonate, m-dpb; 1,3-bis(diphenylphosphoryl)benzene) showed crystal growth in CTAB/SDS solution (CTAB, cetyltrimethylammonium bromide; SDS, sodium dodecyl sulfate). The crystal morphology of [Eu(hfa)3(m-dpb)]n was changed under the synthetic conditions with various types of cationic surfactants (N+(CH3)3CnH2n+1; n = 8, 12, and 16). The Eu(III) coordination polymer crystals were observed as plates and slender rod shapes. Their crystal morphologies suggest that the crystal growth along the chain growth direction is faster than that along the chain stacking direction.

PMID 42929628
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PubMedPeerJ2026-10-26

In vitro evaluation of N-acetylcysteine, calcium hydroxide, chlorhexidine digluconate and their combinations effect against five dental obligate anaerobic bacteria.

de Carvalho Lara Steffany LS, de Oliveira Júlia Andrade JA, Cezarino Gabriel Manente GM, Dos Santos Luiz Augusto Rodrigues LAR et al.

This study aimed to evaluate the antibacterial action of N-acetylcysteine (NAC), calcium hydroxide Ca(OH)2, chlorhexidine digluconate (CHX), and their combinations against five obligate anaerobic bacteria including Fusobacterium nucleatum, Porphyromonas endodontalis, Porphyromonas gingivalis, Prevotella intermedia, and Parvimonas micra in planktonic and biofilm forms. Eight experimental groups were evaluated in this study including saline solution (SS) (control group), Ca(OH)2, CHX, NAC, NAC + Ca(OH)2, NAC + CHX, Ca(OH)2 + CHX, and NAC + Ca(OH)2 + CHX. The anti-planktonic evaluation was performed by determination of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) following Clinical and Laboratory Standards Institute guidelines (CLSI M11). The antibiofilm was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and crystal violet (CV) assays. Data were analyzed statistically considering a significant level of (α ≤ 0.05). It was found that the MIC and MBC values of the tested intracanal medications ranged from 1.95-500 mg/mL. MTT and CV assays showed significant, species-dependent antibiofilm activity. CHX was most effective against F. nucleatum; NAC-based medications, especially combined with Ca(OH)2 and/or CHX, were superior against P. endodontalis, P. intermedia, and P. micra. Ca(OH)2-containing groups were particularly effective against P. gingivalis. Therefore, NAC + Ca(OH)2 and NAC + Ca(OH)2 + CHX can be considered as effective combinations of intracanal medication against different obligate anaerobic bacteria.

PMID 42928779
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PubMedCureus2026-10-26

Evaluation of the Cytotoxic Effect of Calcium Silicate-Based Bioceramic Sealers: An In Vitro Comparative Study.

Bagade Prashikkumar P, Borthakur Bikash Jyoti BJ, S Ganesan G, B Swathika S

Calcium silicate-based bioceramic sealers have become increasingly popular due to their biocompatibility, bioactivity, and potential for periapical tissue integration. However, evaluating their cytotoxic effects on fibroblast cell lines remains limited. The aim of this study was to compare the cytotoxic effects of two commercially available calcium silicate-based bioceramic root canal sealers on L929 mouse fibroblast cells, using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay to assess cell viability following exposure to serial dilutions (100%-6.25%) of sealer extracts. Leachates were prepared by incubating for 24 hours in 2 mL of serum-free Dulbecco's Modified Eagle Medium (DMEM) through 0.2 μm polyethersulfone (PES) syringe filters from sets of specimens from both sealers. L929 mouse fibroblast cells were seeded at a density of 1×104 cells/well and treated with five serial dilutions (100%, 50%, 25%, 12.5%, and 6.25%) of sealer extracts. Cell viability was determined spectrophotometrically at 570 nm by MTT assay. Dimethyl sulfoxide (DMSO) (10%) was used as a positive control, and cells without treatment were used as a negative control. Cell viability was significantly decreased with both 100% and 50% concentrations of Bio-C Sealer (Angelus Indústria de Produtos Odontológicos S/A, Londrina, Brazil) (4.89% and 9.31%, respectively) and Prime MTA Bioceramic Root Canal Sealer (Prime Dental Products Pvt Ltd, Maharashtra, India) (5.28% and 8.30%, respectively). However, at lower concentrations, cell viability recovered significantly and approached the control level at 6.25%. At 25% concentration, a statistically significant difference (p=0.002) was observed, with Bio-C Sealer showing better cytocompatibility (92.86% vs 68.35%). Bio-C Sealer and Prime MTA Bioceramic demonstrated significant cytotoxicity at high extract concentrations with acceptable biocompatibility at clinically relevant dilute concentrations. Bio-C Sealer exhibited superior cytocompatibility at the 25% concentration and a higher IC₅₀ value, indicating better overall cytocompatibility. The comparatively favourable cytocompatibility profile of Bio‑C Sealer at intermediate concentrations suggests that material selection may be influenced by its reduced cytotoxic potential, particularly in scenarios where periapical tissue contact is likely. These findings highlight the importance of considering biological performance alongside physicochemical properties when choosing endodontic sealers.

PMID 42928799
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PubMedCytotechnology2026-10-26

Creb1 aggravates glutamate-induced excitotoxicity and KA-induced seizure activity by transcriptionally activating Timp1.

Qiao Qiubo Q, Wang Man M

Epilepsy is a chronic neurological disorder, more common in children and the elderly. Although treatments have advanced, significant challenges remain. This study focuses on its molecular mechanisms to provide new insights and strategies for its treatment. Gene expression omnibus (GEO) database analysis, enrichment analysis, and the establishment of protein-protein interaction (PPI) networks were conducted for gene screening. HT-22 cells were treated with glutamate (Glu) to establish an in vitro epilepsy model. Gene knockdown and overexpression were achieved through cell transfection. Cell viability was measured by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, while gene expression at the protein and messenger RNA (mRNA) levels was detected by western blot (WB) and real-time quantitative polymerase chain reaction (RT-qPCR). Flow cytometry was used to analyze apoptosis and mitochondrial membrane potential. Lactate dehydrogenase (LDH), reactive oxygen species (ROS), and Fe2+ levels were measured using commercial kits. Kainic acid (KA) was administered intraperitoneally to mice to establish an epilepsy animal model, which was used to verify the role of the gene in epilepsy development. Transcription factor binding sites in target gene promoters were predicted using the JASPAR database and validated by chromatin immunoprecipitation (ChIP) and dual-luciferase reporter assays. Tissue inhibitor of metalloproteinases 1 (Timp1) was highly expressed in tissue samples from the epilepsy mouse models of GSE88992 and GSE73878, as well as in the Glu-induced HT-22 cell model. In these models, Timp1 knockdown increased cell viability, reduced apoptosis, decreased LDH, promoted mitochondrial membrane potential, and lowered ROS, Fe2+, and acyl-CoA synthetase long-chain family member 4 (Acsl4) levels. In KA-induced animal models, Timp1 knockdown reduced seizure score, cleaved caspase-3 (C-caspase3)/total caspase-3, and Acsl4 expression. cAMP response element-binding protein 1 (Creb1) transcriptionally activated Timp1. In the Glu-induced HT-22 cell model, Creb1 knockdown decreased Timp1 protein expression, increased cell viability and mitochondrial membrane potential, and reduced apoptosis, LDH, ROS, Fe2+, and Acsl4 levels, while Timp1 overexpression partially reversed these effects. Taken together, Creb1 promotes the progression of epilepsy by activating Timp1, providing a new perspective and potential targets for epilepsy treatment. The online version contains supplementary material available at https://doi.org/10.1007/s10616-026-01084-7.

PMID 42928721
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PubMedMikrochimica acta2026-10-25

Ag-decorated sulfur-rich covalent organic framework for SERS fingerprinting of β2-adrenergic agonists olodaterol, indacaterol, and formoterol.

Li Min M, Yang Fang F, Huang Qingyu Q, Luo Xiaojun X

Olodaterol, indacaterol, and formoterol are the most frequently abused β2-agonists. The World Anti-Doping Agency (WADA) has imposed a threshold limit of 40 ng/mL for formoterol in urine and a total ban on olodaterol and indacaterol. Therefore, it is urgent to develop sensitive analytical methods for the identification and quantification of the three compounds. Herein, for the first time, we fabricated a sulfur rich covalent organic framework supported silver-nanoparticle (Ag-SCOF) substrate for surface enhanced Raman spectroscopy (SERS). Benefiting from the strong Ag-S covalent bonds, silver nanoparticles can be firmly anchored on the SCOF matrix to effectively suppress nanoparticle aggregation and improve substrate stability. Target β2-agonists can be enriched into electromagnetic hot spots via Ag-N interactions, thereby greatly amplifying Raman signals. The analytical enhancement factor of this substrate reaches 3.89 × 105. The limits of detection (LODs) for olodaterol, indacaterol, and formoterol reach 8.61 × 10⁻8, 8.03 × 10⁻8, and 9.63 × 10⁻8 g·mL⁻1, respectively. This Ag-SCOF SERS platform achieves rapid (within 3 min), fingerprint-based simultaneous detection, overcoming the drawbacks of conventional methods such as high cost, long assay time and low specificity. The proposed method fully meets the detection requirements of WADA regulations and food safety monitoring, and has great potential for on-site analysis of real samples.

PMID 42925429
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