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umeclidinium bromide + vilanterol (642444+573719 / Anoro / GSK573719/GW642444)

✓ Approved

Innoviva, Inc. · ADRB2 · 小分子

什么是 umeclidinium bromide + vilanterol？

umeclidinium bromide + vilanterol 是一种小分子，由Innoviva, Inc.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642444+573719, Anoro, GSK573719/GW642444
公司Innoviva, Inc.
药物类别小分子
分子靶点ADRB2, NR3C1
给药途径Inhaled
状态Approved
来源： ClinicalTrials.gov, Innoviva, Inc.

作用机制

分子靶点

umeclidinium bromide + vilanterol 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

umeclidinium bromide + vilanterol 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

PubMedClinical nutrition ESPEN2026-06-13

Comparison of different bromide equilibrium times to measure extracellular water in athletes: analysis before and after a 4-day intervention to increase water intake.

Jesus Filipe F, Francisco Rúben R, Kondo Emi E, Nunes Catarina L CL et al.

Bromide (Br-) dilution is the criterion to determine extracellular water. While 3h equilibrium is typically used in athletes, the optimal equilibrium time has not been assessed. The study aimed to determine the optimal time of equilibrium of Br- in athletes before and after increasing water intake (WI). Thirty-one athletes [21.5 (0.8) years; 41.9% females] from the H2OAthletes randomized controlled trial (clinicaltrials.gov ID: NCT05380089) were included in this longitudinal sub-analysis. Athletes were assessed before and after a 4-day intervention to increase WI (experimental group) or maintain WI (control group). Br- dilution was assessed through saliva before and 3, 4, and 5h post-dose. Total body water (TBW) and water turnover (rH2O) was measured through deuterium dilution. Body composition was determined through the 4-compartment model. At baseline, most athletes achieved equilibrium at 3h (45.2%) or 4h (48.4%). After the intervention, most athletes (70.4%) achieved peak concentration at 3h, with fewer reaching at 4h (14.8%) or 5h (14.8%). No differences in body composition, TBW, or rH2O were observed between athletes grouped according to the time of peak, both before and after the intervention. Time of peak was not associated with the intervention group [x2 (1)=1.439; p=0.487] or sex both before [x2 (1)=0.230; p=0.891] and after the intervention [x2 (1)=0.728; p=0.695]. Br- equilibrium appears to occur 3h to 4h post-dosing, suggesting it is unnecessary to extend the collection to 5h, reducing the burden on athletes. Future studies should include larger samples to confirm the current findings.

PMID 42285220
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PubMedAmerican journal of respiratory and critical care medicine2026-06-12

Defining disease stability in COPD: Evidence from Phase 3 clinical trials.

Singh Dave D, Stacey Rianne R, Halpin David M G DMG, Bhatt Surya P SP et al.

Disease stability in COPD is a low disease activity state proposed as a treatment target. Characterize COPD stability as a composite endpoint. Post hoc analyses were carried out on IMPACT and FULFIL (fluticasone furoate/umeclidinium/vilanterol [FF/UMEC/VI] vs dual therapies) and MATINEE/METREX/METREO (mepolizumab added onto triple therapy). Stability was defined as "no moderate/severe exacerbations and no worsening from baseline in CAT and FEV1". We assessed whether achieving stability at Week 28 was prognostic of subsequent outcomes (time to first on-treatment moderate/severe exacerbation and time to all-cause mortality [ACM]) after Week 28 (IMPACT). Bayesian joint modeling evaluated the probability of achieving stability (IMPACT). Stability was achieved with FF/UMEC/VI by 22% of patients in IMPACT (Week 52) and by 46% of patients in FULFIL (Week 24); stability was achieved with mepolizumab +triple therapy by 18% of patients in MATINEE/METREX/METREO (Week 52). Patients were more likely to achieve stability with triple versus dual therapy and with mepolizumab versus placebo. Many individuals achieving stability had clinically meaningful improvements in CAT and FEV1. Patients achieving stability at Week 28 (vs patients who were not stable) had a 45.7% reduction in the risk of moderate/severe exacerbations and a 51.7% reduction in the risk of ACM after Week 28. Bayesian joint modeling demonstrated a mean (SD) posterior probability of stability: 25.60% (0.66) at Week 52 (FF/UMEC/VI). Our data provide further evidence for disease stability as an achievable COPD treatment target that predicts long-term clinical benefits in exacerbations and mortality.

PMID 42281286
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PubMedOphthalmology and therapy2026-06-12

In Vitro Bactericidal Activity of Propamidine 0.1% and Other Ophthalmic Antiseptics on Conjunctivitis and Blepharitis Strains.

Paschier Adrien A, Chauchat Laure L, Rebika Hayette H, Sahyoun Marwan M et al.

The aim of this study was to assess the in vitro antimicrobial activity of propamidine isethionate 0.1% ophthalmic solution and other topical antiseptics, including hexamidine di-isethionate 0.1%, cethexonium bromide 0.025%, and picloxydine hydrochloride 0.05%. Antibacterial activity was tested in vitro on five Gram-positive bacterial strains commonly found in conjunctivitis and/or blepharitis. Test products were applied at a concentration of 80% at 20 °C (in accordance with NF EN 1040) for contact periods of 2, 5, 10, and 15 min. After neutralization, surviving bacteria were cultured, and colony forming units (CFU) were counted. Antimicrobial efficacy was expressed as log reduction in CFU. Bactericidal activity was defined as a reduction > 5 log. All tested antiseptics demonstrated antibacterial activity with variability in magnitude of their effects depending on the bacterial strain and contact time. Propamidine 0.1% showed rapid activity, achieving maximal log reduction within 2 min against Staphylococcus epidermidis, Streptococcus pneumoniae, and Propionibacterium acnes. Cethexonium bromide 0.025% exhibited the highest antibacterial activity, with bactericidal effects observed against Corynebacterium striatum, S. pneumoniae, and P. acnes; hexamidine 0.1% and picloxydine 0.05% showed more limited or inconsistent bactericidal activity. All tested antiseptics demonstrated measurable in vitro antibacterial activity against common pathogens associated with conjunctivitis and blepharitis. The observed variability in antimicrobial magnitude highlight the influence of bacterial strain and exposure conditions on antiseptic performance. These results support the potential clinical interest of ocular antiseptics, including propamidine 0.1% in the management of mild bacterial conjunctivitis and blepharitis, although confirmation under clinical conditions remains necessary.

PMID 42283971
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PubMedSensors (Basel, Switzerland)2026-06-12

Luminescent Wearable Sensor on Anions from Cotton Fabric Grafted with Cu-In-Zn-S Colloidal Quantum Dots.

Liu Xiao X, Zhu Pengbo P, Ren Hao H, Wang Yao Y et al.

Negatively charged molecules and anions are widely present in the natural environment and can pose a threat to aquatic life, affecting their survival and reproduction. As the understanding of the hazards of negatively charged molecules and ions deepens, the need for real-time monitoring governs the development of highly sensitive and convenient sensing materials. Here, highly luminescent Zn-Cu-In-S core-shell colloidal quantum dots were grafted onto cotton fabric to produce a fluorescence cotton fabric (FCF) optical sensor demonstrating photoluminescence response to the presence of several anions in water, such as phosphate (PO43-), hydroxide (OH-), fluoride (F-), chloride (Cl-), or bromide (Br-). After contact with water solutions containing these anions, PL output from FCF remarkably decreases, with specific functional dependence on the concentration of the selected anions. The fluorescent fabric sensing material is easy to operate, achieving real-time detection of negatively charged groups and showing great potential for application in environmental monitoring.

PMID 42281084
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PubMedJournal of computational chemistry2026-06-12

Synergistic Heavy-Atom and Vibronic-Coupling Effects for High-Performance Ionic TADF Emitters: A Theoretical Study.

Meng Yizi Y, Ning Ziye Z, Tang Bowen B, Zhang Yanying Y et al.

Ionic thermally activated delayed fluorescence (iTADF) materials are promising for organic optoelectronics due to their solution processability and structural tunability, yet the synergistic regulation of reverse intersystem crossing (RISC) by heteroatom anchoring, heavy-atom effects, and vibronic coupling remains underexplored. Four molecules (AC-TPPO+, AC-TPPS+, AC-TPPO[Br], and AC-TPPS[Br]) are systematically investigated via density functional theory (DFT), TD-DFT, and excited-state dynamics. All molecules feature twisted donor-acceptor conformations, enabling spatial separation of frontier molecular orbitals and a small singlet-triplet energy gap (ΔEST) for RISC. The bromide counterion (Br-) induces a heavy-atom effect, enhancing spin-orbit coupling strength and accelerating RISC rates by two orders of magnitude. Low-to-medium-frequency vibrations further facilitate RISC by driving S1 and T1 potential energy surfaces to near-degeneracy. The optimal AC-TPPO[Br] achieves a high delayed fluorescence quantum yield (ΦDF = 74.88%) with nearly 100% room-temperature TADF contribution. This work provides a synergistic design paradigm and theoretical guidance for high-performance OLED emitters.

PMID 42281343
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PubMedMolecules (Basel, Switzerland)2026-06-12

Isoxazole-Thiazole Hybrids: Synthesis, Structural Characterisation, Carbonic Anhydrase Inhibition, and Molecular Docking Studies.

Berber Nurcan N, Türkeri Özge Nur ÖN, Başoğlu Faika F, Çıkrıkcı Kubra K et al.

A new series of isoxazole-fused thiazole-oxazole derivatives (11a-n) was rationally designed and synthesised with the aim of developing potent carbonic anhydrase (CA) I and II inhibitors. The synthesis was achieved in five steps starting from 4-bromoacetophenone, involving key intermediates such as hydroxylamine hydrochloride, hydrazine hydrate, thioisocyanate, and various phenacyl bromide derivatives, using ethanol, triethylamine, tetrahydrofuran (THF), and dimethylformamide (DMF) as solvents. The synthetic route included the formation of a β-ketoester, isoxazole ester, hydrazine adduct, thiourea derivative, and, ultimately, a thiazole ring. The structures of the final compounds were confirmed by 1H-NMR, 13C-NMR, IR spectroscopy, and elemental analysis. All compounds were examined as inhibitors of human carbonic anhydrase (hCA) I and II, and all of them inhibited hCA I and hCA II. Kinetic investigation results revealed that these compounds inhibited hCA I and hCA II in a non-competitive manner. To further explore the molecular basis of their inhibitory activity, in silico studies, including molecular docking and 300 ns molecular dynamics (MD) simulations, were carried out against both CA I and CA II isoforms. These simulations provided detailed insights into the dynamic behaviour, stability, and key binding interactions of the compounds within the enzyme active sites, supporting their potential as promising carbonic anhydrase inhibitors.

PMID 42280128
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