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fluticasone propionate + formoterol fumarate dihydrate

✓ Approved

Vectura Group Ltd · ADRB2 · 小分子

什么是 fluticasone propionate + formoterol fumarate dihydrate?

fluticasone propionate + formoterol fumarate dihydrate 是一种小分子,由Vectura Group 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

公司Vectura Group Ltd
药物类别小分子
分子靶点ADRB2, NR3C1
给药途径Inhaled
状态Approved

作用机制

分子靶点

fluticasone propionate + formoterol fumarate dihydrate 作用于 2 个分子靶点:

ADRB2adrenoceptor beta 2 (B2AR, ARB2)
NR3C1nuclear receptor subfamily 3 group C member 1 (GR, GCCR)
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

fluticasone propionate + formoterol fumarate dihydrate 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 disordersAsthma✓ 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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PubMedCell death discovery2026-10-26

Palmitoylation-driven upregulation of NKAα2 improves diabetic cardiomyopathy: a role for the fumarate hydratase/fumarate metabolic pathway.

Lu Xi-Xi XX, Feng Yu-Yan YY, Yang Le L, Yang Ming-Tao MT et al.

The sodium pump Na⁺/K⁺-ATPase (NKA) plays an essential role in maintaining cellular ion homeostasis. Dysregulation of its α2 subunit (NKAα2) has been implicated in cardiovascular and metabolic diseases, yet its contribution to diabetes-induced cardiac dysfunction remains poorly defined. Therefore, this study aimed to elucidate the role of NKAα2 in diabetic cardiomyopathy (DCM). We performed gain-of-function experiments to investigate the effects of NKAα2 on DCM-associated pathological processes. Both in vivo mouse models and in vitro cardiomyocyte systems were employed to ensure mechanistic consistency. We found that both NKA activity and NKAα2 protein, rather than its transcriptional level, were significantly downregulated in the hearts of diabetic mice and high glucose/palmitic acid (HG/PA)-incubated NRCMs. Cardiac-specific overexpression of NKAα2 markedly alleviated myocardial injury and improved cardiac function in diabetic mice. Consistently, NKAα2 overexpression attenuated HG/PA-induced hypertrophy and apoptosis in primary neonatal rat cardiomyocytes (NRCMs). Mechanistically, ATP-1 mediated de-palmitoylation increased NKAα2 in the mitochondrial-enriched fraction, where it interacted with E3 ubiquitin protein ligase 1 (MUL1), which was responsible for NKAα2 ubiquitination and degradation. Metabolomic analyses revealed that NKAα2 downregulation dissociated Mul1 from fumarate hydratase (FH), leading to increased FH expression and decreased intracellular fumarate levels. Exogenous fumarate administration mimicked the cardioprotective effects of NKAα2 overexpression and mitigated the damage caused by NKAα2 deficiency in HG/PA-treated cardiomyocytes. Overexpression of FH blocked the effects of NKAα2 on diabetic cardiac dysfunction. Collectively, these findings identify NKAα2 as a critical regulator in DCM. These results also underscore the requirement of tightly controlled FH activity and fumarate metabolism for NKAα2-dependent cardioprotection. A diagram illustrating the molecular mechanism of the NKAα2/FH/fumarate metabolic axis in the development of DCM.

PMID 42928350
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PubMedDiseases (Basel, Switzerland)2026-10-26

Assessing Renal Outcomes After Switching from Tenofovir Disoproxil Fumarate to Tenofovir Alafenamide in People with HIV: Proteinuria Changes and Limits of Causal Attribution.

D'Anna Tommaso T, Trizzino Marcello M, Belmonte Beatrice B, Gioè Claudia C et al.

Background: The total urinary protein-to-creatinine ratio (PCr) measures proteinuria but does not establish tubular injury or its recovery. Methods: We examined PCr changes after switching from tenofovir disoproxil fumarate (TDF) to tenofovir alafenamide (TAF) in a single-centre retrospective cohort of 364 adults with human immunodeficiency virus (HIV) infection. Paired PCr values were available for 159 patients (43.7%). The primary descriptive endpoint was a PCr reduction below 20%, an operational, nonvalidated threshold. Analyses comprised paired rank-based comparisons, baseline-adjusted regression, threshold and influence sensitivity analyses, and nested cross-validation of ridge logistic regression using three predictor sets. Results: The median paired PCr change was -4.0 mg/g (interquartile range -41.5 to 11.5; signed-rank Benjamini-Hochberg-adjusted q = 0.0098); 99/159 patients (62.3%) had a reduction below 20%. Baseline log(1 + PCr) was positively associated with post-switch log(1 + PCr), while its coefficient in the corresponding change model was exactly one unit lower, illustrating mathematical coupling. The cross-validated area under the curve was 0.709 for baseline PCr alone, 0.475 for the other covariates, and 0.701 for all predictors. Conclusions: PCr changes were heterogeneous, and additional covariates did not improve discrimination over the baseline PCr alone. Missing outcomes, unavailable specimen dates, the absence of tubular-specific biomarkers and the uncontrolled design preclude conclusions about irreversible tubular injury, causal treatment effects or clinical prediction utility.

PMID 42929980
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PubMedAging cell2026-10-26

Metabolomic Signatures of Longevity in Bivalves Reveal Reorganization of TCA Cycle and Amino Acid Metabolism.

Bertrand Pauline P, Chevret Clément J L CJL, Rodríguez Enrique E, Lemieux Hélène H et al.

Mitochondria are central regulators of cellular metabolism, integrating energy production, redox balance, and signaling pathways that shape aging trajectories. If mitochondrial organization contributes to lifespan divergence, exceptionally long-lived species should exhibit distinctive metabolic signatures reflecting adaptations promoting long-term cellular maintenance. Comparative approaches across species with extreme lifespan variation provide a powerful framework for identifying potential metabolic strategies underlying longevity. We conducted targeted metabolomic profiling of five marine bivalve species spanning a lifespan gradient from approximately 30 to more than 500 years, including the exceptionally long-lived ocean quahog, Arctica islandica. Fifty metabolites were quantified in gill and mantle tissue to determine whether lifespan variation is associated with coordinated changes in metabolic organization. Lifespan emerged as a dominant axis of metabolomic variation across species. Long-lived bivalves exhibited a distinct metabolic phenotype characterized by a global reduction in free amino acid pools and coordinated changes in metabolites associated with mitochondrial metabolism. Longevity was associated with increased succinate-to-fumarate ratios, reduced fumarate and malate concentrations, and reduced engagement of pyruvate-derived anaerobic pathways under basal conditions. Although these patterns varied in magnitude across tissues, they converged on a common longevity-associated metabolic signature. Together, these patterns suggest that exceptional longevity is associated with a distinct organization of mitochondrial-related metabolism and a more selective allocation of metabolic resources, rather than a generalized suppression of metabolism. Our findings identify metabolomic signatures associated with exceptional longevity across the bivalve species studied and support the hypothesis that long lifespan is characterized by a distinctive metabolic architecture favoring long-term cellular maintenance.

PMID 42928049
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PubMedPhysiologia plantarum2026-10-26

Unraveling the Chemical Dialogue: The Impact of Volatiles on the Interaction Between PGPR and Verticillium dahliae in Pepper Plants.

Triantafyllou Aikaterini A, Kamou Nathalie N, Mellidou Ifigeneia I, Testempasis Stefanos S et al.

Plant growth-promoting rhizobacteria (PGPR) have attracted increasing scientific interest due to their potential to enhance crop productivity and alleviate plant stress. An important trait of PGPR is the production of volatile organic compounds (VOCs), which can play crucial roles in plant-microbe and interspecies communication. This study investigates the volatilome composition of a novel PGP strain, Chryseobacterium sp. SAESo14, and its impact during interactions with the soilborne pathogen Verticillium dahliae and pepper plants. First, volatiles from SAESo14 and V. dahliae co-inoculated in dual cultures were analyzed by Gas chromatography-mass spectrometry (GC-MS). A diverse set of VOCs, including alcohols, ketones, esters, and sulfur-containing compounds, was detected. Among these, VOCs with known antifungal activity, such as 2-heptanone, ethyl propionate, and ethyl acetate, were identified. To further investigate the role of VOCs in tripartite interactions, volatilomes of a pepper-V. dahliae pathosystem treated with SAESo14 were analyzed. Seedlings treated with SAESo14 showed viable root cells and enhanced terpenoid metabolism, leading to the emission of 1,8-cineole, β-elemene, and sclarene, whereas V. dahliae-inoculated seedlings released 4,5-di-epi-aristolochene. When tested in planta, pepper plants treated with SAESo14 exhibited increased net photosynthesis and improved growth, along with a 25% reduction in disease index compared to pathogen-inoculated plants, in which distinct metabolic and transcriptomic reprogramming was observed. Collectively, these findings highlight the importance of VOC-mediated signaling in plant-microbe-pathogen interactions in a tripartite system and support the potential of a novel Chryseobacterium strain and its derived VOCs as sustainable alternatives for improving plant performance and disease management.

PMID 42928643
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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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