若生智能
Drug Database
UM

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

PubMedRSC advances2026-08-06

Electrochemical α-acyloxylation of dibenzoylmethane with C-terminal carboxylic acids for peptide and drug diversification.

Jiang Shuqiang S, Hu Fan F, Huang Jun J, Zhang Linxing L et al.

Carboxylic acids are common functional handles in peptides and drug molecules, but their direct use for DBM derivatization remains limited. Herein, a bromide-mediated electrochemical α-acyloxylation of dibenzoylmethane (DBM) with amino acid-, peptide-, and drug-derived carboxylic acids is described. The reaction proceeds in an undivided cell under mild conditions, providing DBM-amino acid, DBM-peptide, and DBM-drug conjugates through C-O bond formation. Various amino acids, DBM derivatives, drug acids, dipeptides, and bioactive peptides are tolerated. Mechanistic studies support α-bromination of DBM followed by carboxylate substitution. Representative peptide conjugation improves the aqueous behaviour of DBM.

PMID 42559229
阅读全文 →
PubMedInfection and immunity2026-08-06

Dual roles of genes required for intrinsic resistance to clarithromycin in evasion of killing by serum complement in Haemophilus influenzae.

Huhn Cameron C, Dees Justine J, Gawronski Jeffrey J, Taslim Asma Ul AU et al.

Macrolide antibiotics are commonly prescribed to treat Haemophilus influenzae respiratory tract infections. Studies have primarily focused on emerging H. influenzae strains with acquired macrolide resistance, while the bacterium's intrinsic resistance to antibiotics has been underexamined. Here, we used a genome-wide approach of transposon insertion-site sequencing to screen an H. influenzae mutant library grown in sub-inhibitory doses of the macrolide antibiotic clarithromycin (CLR) to identify 33 genes involved in intrinsic CLR resistance. Almost half of these genes are also needed for survival in the mouse lung. We focused on candidate genes necessary for both intrinsic macrolide resistance and lung survival. Two of these genes affect the outer-membrane composition of H. influenzae, orfH and omp26. Deletions of these genes in Rd and nontypeable H. influenzae clinical isolates, Hi375 and NT127, conferred sensitivity to CLR and polymyxin B and increased membrane permeability to ethidium bromide (EtBr). The omp26 mutant was sensitive to killing by human serum. Deletions of orfH or omp26 in an acrR mutant strain overexpressing a multidrug efflux pump abrogated resistance of the acrR mutant to CLR and restored permeability to EtBr. Thus, deletion of these genes not only mitigates the effects of an acquired resistance mechanism but also remarkably overrides it. Complementation of these deletion mutations restored CLR resistance and decreased permeability to EtBr. Our results indicate that the subset of genes with dual roles in intrinsic resistance and host lung survival may provide potential novel combination antimicrobial therapeutic targets.

PMID 42560181
阅读全文 →
PubMedThe Journal of pharmacology and experimental therapeutics2026-08-06

Cardiac homing peptide-decorated epigallocatechin gallate-loaded poly(lactic-co-glycolic acid) nanoparticles alleviate acute myocardial infarction.

Li Haiqi H, Huang Ruohui R, Zhang Jinhong J, Jiang Dongli D et al.

Epigallocatechin gallate (EGCG) exerts cardioprotective effects on acute myocardial infarction through multiple pathways. However, the clinical application of EGCG is limited because of its instability under physiological conditions and low bioavailability. In this study, poly(lactic-co-glycolic acid) was used as a drug carrier to prepare EGCG nanoparticles (NPs), then an EGCG targeting drug delivery system was designed by modifying with cardiac homing peptide. We constructed a preparation route combining the double-emulsion solvent evaporation method and the carbodiimide method. By optimizing the preparation process, the particle size of the EGCG NP was reduced, and the dispersibility was improved. In addition, the established preparation procedure uses safe and low-toxicity reagents, requires no strict temperature control or specialized instrumentation, and therefore significantly reduces the technical difficulty of large-scale industrial production. EGCG-poly(lactic-co-glycolic acid)-cardiac homing peptide had myocardial targeting and good safety in the 3‑(4,5‑dimethyl‑2‑thiazolyl)‑2,5‑diphenyl‑2H‑tetrazolium bromide (MTT) cytotoxicity test, and alleviated acute myocardial infarction by regulating apoptosis-related protein expression in a dose-dependent manner. Compared with EGCG monomer, EGCG-poly(lactic-co-glycolic acid)-cardiac homing peptide achieved a better therapeutic effect. This study provides a new strategy for promoting the application of EGCG in the clinical treatment of acute myocardial infarction. SIGNIFICANCE STATEMENT: This study develops cardiac homing peptide-modified poly(lactic-co-glycolic acid) nanoparticles to enable targeted delivery of epigallocatechin gallate for acute myocardial infarction therapy. By overcoming the inherent instability and poor bioavailability of epigallocatechin gallate, this scalable nanoplatform achieves superior cardioprotection through regulated apoptosis and exhibits excellent safety in the MTT cytotoxicity test. These findings establish a clinically translatable strategy for targeted drug delivery in the treatment of cardiovascular disease.

PMID 42557166
阅读全文 →
PubMedChemistry, an Asian journal2026-08-05

Hydrogen-Bond DonorAssisted Cycloaddition of CO2 to Epoxides Catalyzed by Schiff Base Derived Ionic Liquids: Catalytic, Mechanistic, and Kinetic Studies.

Paul Saurav S, Lahkar Surabhi S, Brahma Sanfaori S

Four new salicylaldehyde, o-vanillin, 5-nitrosalicylaldehyde and benzaldehyde derived Schiff base ionic liquids (ILs) with bromide counterion (IL-Sal, IL-Van, IL-NSal, and IL-Bz) have been facilely synthesized. The co-existing phenolic-OH and counteranion, Br- in IL-Sal, IL-Van, and IL-NSal are employed as bifunctional organocatalysts for epoxide-CO2 coupling reaction, where -OH activates the epoxide via hydrogen bonding and Br- promotes ring opening. Experimental evidence from controlled experiments, FT-IR and NMR spectroscopy corroborates a catalytic mechanism involving catalyst-epoxide hydrogen bonding. A control experiment using IL-Bz, lacking phenolic-OH, shows inferior activity compared to IL-Sal [cf. substrate: butyl glycidyl ether; conversion: 9% (cat. IL-Bz); 90% (cat. IL-Sal)], confirming the crucial role of -OH as HBD in epoxide activation. Further, NMR spectroscopic investigation reveals H-bonding via downfield shifts with slightly reduced intensity, supported by FT-IR through shifting of the O-H stretching band. Kinetic studies indicate first-order kinetics with rate constants of 1.2 × 10-5 s-1, 2.2 × 10-5 s-1 and 2.7 × 10-5 s- 1 at 40°C, 60°C, and 80°C, respectively. Activation parameters are ΔH# = 7.50 ± 0.40 kJ·mol-1 and ΔS# = -244.5 ± 1.21 J·mol-1·K-1. The catalyst also shows good recyclability with conversions of 94%, 89%, and 85% in three consecutive cycles.

PMID 42554322
阅读全文 →
PubMedAnalytical sciences : the international journal of the Japan Society for Analytical Chemistry2026-08-05

Raman scattering spectroscopic analysis on the structural changes in the micelles of a CTAB-NapTS system.

Yuki Ishige I, Oguchi Kenichi K, Yui Hiroharu H

Condensed micelle solutions are ubiquitously seen and utilized in foods, medicine, oil recovery, and so on. It is well-known that micelles formed from ionic surfactants drastically change their aggregate morphologies from spherical to short, rigid rod-like, and occasionally to long, winding worm-like structures as the concentration of the co-existing salts is varied. In general, these large-scale morphological changes induced by additive salt have been directly assessed by X-ray or neutron scattering spectroscopies. However, industrial processes are often carried out under open-system and atmospheric conditions, thus they show transient and dynamic changes of their structures and resultant viscoelastic properties according to the environmental changes. Here we examined whether Raman scattering spectroscopy is applicable for detecting such large-scale morphological changes in micelles by monitoring the corresponding changes occurring in the local packing environment of neighboring surfactant alkyl chains. As a representative micelle-salt system, cetyltrimethylammonium bromide (CTAB) and sodium p-toluene sulfonate (NapTS) were studied by varying their concentration ratio. As a result, it was proposed that the CH2 twisting and scissoring modes were useful indices to discriminate the morphological changes in micelles. These results provide a useful index for monitoring the transient structural changes of micelle solutions and elucidating the mechanism of the resultant changes in viscoelastic properties in situ and on-site monitoring.

PMID 42554953
阅读全文 →
PubMedFrontiers in veterinary science2026-08-05

Management practices and continuing education in the treatment of canine idiopathic epilepsy among Indian primary care veterinarians.

Srinath A T AT, Muñana K R KR, Deshmukh P P, Caddiell R R et al.

In India and countries without veterinary neurologists, dogs with idiopathic epilepsy (IE) are managed by primary care veterinarians. Data are lacking on their practice patterns. Describe management of canine IE among Indian primary care veterinarians and explore the impact of access to educational materials about epilepsy. Prospective, two-phased, survey-based study of Indian veterinarians focused on treatment and monitoring of canine IE and perceived confidence in management recommendations (1/not comfortable to 5/very comfortable). Participants who agreed to Phase II received concise guidelines about IE with a follow-up survey distributed after 6 months. Descriptive statistics summarized management trends and compared confidence scores between surveys. 187 veterinarians participated in Phase I and of these, 36 participated in Phase II. Phenobarbital was the most common anti-seizure drug prescribed, chosen mostly due to efficacy. Most respondents (118/187; 63%) recommended routine lab work and (84/187; 45%) recommended measuring phenobarbital or potassium bromide blood concentration every 6-12 months; (61/187; 33%) reported not measuring blood concentrations routinely. Long-term management of IE and adverse effects of medications were rated as most challenging. Nearly half of Phase II respondents (17/36; 47%) ranked the educational materials as extremely beneficial. Mean self-reported comfort level was 3.3 (SD 0.97) and 3.69 (SD 0.89) for Phase I and II, respectively; most (20/36; 56%) reported no change between surveys. Challenges for Indian veterinarians in the chronic management of canine IE related to anti-seizure drug monitoring and adverse effects. Exploratory Phase II findings identified positive reception to educational support from specialists.

PMID 42553078
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多umeclidinium bromide + vilanterol