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fluticasone propionate + formoterol fumarate dihydrate

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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

PubMedThe journal of physical chemistry. B2026-09-10

The Origin of the Kinetic Isotope Effect and Mechanism of H/D Exchange in Radical C-C Bond Formation Catalyzed by Benzylsuccinate Synthase: Experiments and Microkinetic Modeling.

Szaleniec Maciej M, Oleksy Gabriela G, Aleksic Ivana I, Krämer Kai K et al.

Fumarate-adding enzymes (FAE) are a subset of the glycyl radical enzyme superfamily involved in anaerobic hydrocarbon degradation. Benzylsuccinate synthase (BSS) catalyzes the enantiospecific formation of (R)-benzylsuccinate from toluene and fumarate, initiating anaerobic toluene degradation. In this paper, we present the first microkinetic analysis of the full reaction, predicting kinetic isotope effects in the range of 2.587-2.604, close to the experimentally observed value (KIEexp= 2.13 ± 0.1). Our experiments confirmed that KIE values are lower in direct assays with substrate-saturated enzyme, relative to the values obtained for competitive kinetic isotope effects D(V/K) via substrate fractionation (3.69 ± 0.16). We postulate that this apparent KIE suppression originates from preferential binding of unlabeled versus labeled substrates to the enzyme, as well as from the rates of product release. We also show that tunneling effects have only minor influence on the observed KIE and D(V/K) values, although they have been estimated to potentially accelerate the overall reaction rate by approximately 17%. On the other hand, inclusion in the kinetic equation of the barrier recrossing effect, jointly with tunneling correction can result in a lowering of predicted KIE values to the range of 2.38-2.43. Furthermore, we analyze a slowly occurring, experimentally observed H/D exchange process in the product during incubation in D2O, confirming partial reversibility of the reaction. We estimate the rate of this H/D exchange and propose a potential mechanism. Our study contributes to elucidating the processes catalyzed by BSS and its role in the bioremediation of hydrocarbon pollutants.

PMID 42720366
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PubMedIJU case reports2026-09-10

Pathology-Driven Diagnosis of Hereditary Leiomyomatosis and Renal Cell Carcinoma: A Clinicopathological and Genetic Analysis of Three Cases.

Uchiyama Tomoko T, Okazaki Shunsuke S, Ando Sayaka S, Takeda Maiko M et al.

Hereditary leiomyomatosis and renal cell carcinoma (HLRCC) is an autosomal dominant disorder characterized by three principal clinical features: cutaneous leiomyomas (cLMs), uterine leiomyomas, and fumarate hydratase (FH)-deficient renal cell carcinoma (RCC). Although 200-300 families have been identified worldwide, its true prevalence remains unknown. We present three HLRCC cases in which detailed pathological examination raised initial clinical suspicion. Cases 1 and 2 presented with advanced RCC exhibiting diverse morphologies. Case 3 presented with multiple painful cLMs and no renal tumors. All three cases were confirmed via germline genetic testing, which revealed distinct FH mutations. These cases underscore the importance of careful histopathological and immunohistochemical evaluation for the diagnosis of HLRCC. Multidisciplinary discussion integrating clinical, radiological, pathological, and genetic findings is essential for identifying affected families and initiating timely surveillance.

PMID 42719935
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PubMedFrontiers in medicine2026-09-10

Renal function and urinary tubular biomarker abnormalities in untreated and entecavir- or tenofovir disoproxil fumarate-treated patients with chronic hepatitis B: a retrospective cross-sectional study.

Lan Haiyan H, Nie Qilong Q, Liang Qiuyan Q, Huang Caiyang C et al.

Renal safety is an important consideration during nucleos(t)ide analogue (NA) therapy for chronic hepatitis B (CHB). Tenofovir disoproxil fumarate (TDF) may affect proximal tubular function, while serum creatinine and estimated glomerular filtration rate (eGFR) primarily reflect glomerular filtration. This study compared glomerular-function measures and urinary tubular biomarker patterns among NA-untreated, entecavir (ETV)-treated, and TDF-treated patients with CHB. This single-center retrospective cross-sectional study included 242 adults with CHB assessed between June 2025 and June 2026: 113 NA-untreated, 64 ETV-treated, and 65 TDF-treated participants. For treated participants, the single index assessment was obtained after at least 12 months of continuous corresponding monotherapy. Serum creatinine, eGFR, urinary α1-microglobulin (A1M), urinary β2-microglobulin (B2M), and urinary microalbumin (U-mAlb) were compared among groups. eGFR was calculated using the 2009 CKD-EPI creatinine equation and analyzed primarily as a continuous measure; eGFR <90 mL/min/1.73 m2 was retained as a secondary screening outcome. Urinary biomarkers were measured as spot-urine concentrations without urinary creatinine normalization. Urinary A1M ≥ 12.0 mg/L occurred in 13.3%, 42.2%, and 67.7% of NA-untreated, ETV-treated, and TDF-treated participants, respectively; corresponding frequencies of urinary B2M > 0.30 mg/L were 25.7%, 48.4%, and 75.4%. Both A1M and B2M concentration-threshold exceedance were more frequent in TDF-treated than ETV-treated participants (Bonferroni-adjusted P = 0.0108 and P = 0.0048, respectively), and continuous B2M was also higher with TDF (adjusted P = 0.0074). Median eGFR was 112.98 (102.47-119.36), 104.79 (92.08-112.39), and 104.47 (91.24-116.58) mL/min/1.73 m2, respectively (overall P = 0.0008). Both treated groups had lower continuous eGFR than the NA-untreated group, whereas serum creatinine, continuous eGFR, and the frequency of eGFR <90 mL/min/1.73 m2 did not differ between ETV and TDF (all Bonferroni-adjusted P = 1.0000). TDF-treated participants showed a more prominent urinary A1M/B2M concentration-based biomarker pattern than ETV-treated participants, whereas conventional glomerular-function measures did not differ between the two treated groups. These findings represent cross-sectional associations rather than evidence of treatment-induced renal injury. The absence of pretreatment and serial renal measurements, urinary creatinine normalization, and a complete proximal tubular dysfunction assessment requires cautious interpretation and prospective longitudinal confirmation.

PMID 42719150
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PubMedScientific reports2026-09-10

"Green spectrophotometric determination of rupatadine, its toxic impurity, and methyl paraben: comparative AI-assisted univariate versus multivariate chemometrics".

Mansour Salma S SS, Mahmoud Amr M AM, Moustafa Azza A AA, Nashat Nancy W NW

Sensitive and selective green UV-spectrophotometric univariate and multivariate chemometric methods were developed to resolve the overlapped spectra of rupatadine fumarate (RUP), its impurity desloratadine (DES), and methyl paraben (MP). The univariate approach employed was the dual-wavelength (DW) method. Guided by artificial intelligence (AI) in the selection of the optimal wavelength pair, the determination of RUP was performed at 230 and 284.3 nm, and for MP at 236.6 and 253.8 nm. Among the multivariate methods, ANN demonstrated superior predictive accuracy (lowest RMSEP values), followed by PLS-1 and MCR-ALS, highlighting the power of machine learning for complex mixture resolution, particularly in the presence of the preservative MP. A three-factor, five-level experimental design was adopted to construct a calibration set comprising 25 mixtures with varying component ratios, along with 6 independent validation mixtures. The developed methods were successfully applied to pharmaceutical formulation containing the studied drug and were validated in accordance with International Conference of Harmonization (ICH) guidelines. The results obtained were reliable and reproducible, confirming the suitability of these methods for routine analysis and quality control in laboratories. Moreover, the GLANCE tool (Graphical Layout for Analytical Chemistry Evaluation) offered a clear visual summary of the twelve structured method attributes.

PMID 42716967
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PubMedJournal of phycology2026-09-10

Genome-scale insights into metabolic streamlining and photosynthetic energy balance in the extremophile green alga Picocystis salinarum (Picocystophyceae, Chlorophyta).

Lemieux Claude C, Otis Christian C, Turmel Monique M

Picocystis salinarum is an early-diverging chlorophyte and the sole described member of the Picocystophyceae, frequently dominating hypersaline and alkaline lakes despite extreme physicochemical constraints. To elucidate the genomic foundations of its ecological success, we generated a fully annotated, chromosome-scale nuclear genome assembly of the type strain originally isolated from a saline pond in San Francisco Bay. The 18.5-Mb genome comprises 30 chromosomal assemblies, exhibits clear diploidy, and contains multiple copies of intact Ty3/Gypsy and Ty1/Copia long terminal repeat retrotransposons encoding polyproteins with atypical accessory domains. Phylogenomic analyses reveal strong affinity with the Nephroselmidophyceae. Comparative analyses reveal extensive metabolic streamlining, including the absence of a queuosine salvage pathway, the 2-methylcitrate cycle, β-oxidation of propionate, and branched-chain amino acid catabolism, traits retained in several marine prasinophyte lineages. In contrast, the genome preserves multiple ancestral bacterial derived systems. Notably, P. salinarum features a complete chloroplast NADH dehydrogenase-like complex, including all membrane, electron binding, and assembly components, a configuration not previously reported in sequenced chlorophyte algae. This retention implies substantial capacity for cyclic electron flow and chlororespiration, processes expected to be critical in chronically low-light and chemically extreme environments. The genome further reveals a distinctive biochemical CO2-concentrating mechanism centered on plastid-targeted phosphoenolpyruvate carboxykinase, complete plastid peptidoglycan biosynthetic and remodeling pathways, and partial retention of lipid-A-related machinery. Conversely, P. salinarum lacks canonical non-photochemical quenching proteins while retaining xanthophyll-cycle enzymes that support slower photoprotective responses. Together, these features define a coordinated genomic architecture that underpins the specialization of P. salinarum to hypersaline, alkaline, and persistently low-light ecosystems.

PMID 42717851
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PubMedScience advances2026-09-09

Metabolic regulation of calcium homeostasis via SERCA succination.

Ham Su Jin SJ, Kim Yena Y, Kim Sehyeon S, Bang Sunhoe S et al.

Although calcium homeostasis is disrupted in metabolic diseases, its metabolic regulation remains unclear. Here, we identify a mechanism by which fumarate suppresses sarco/endoplasmic reticulum (ER) calcium ion-adenosine triphosphatase (SERCA) activity via succination of a conserved cysteine residue, impairing ER calcium uptake and promoting metabolic dysfunction in Drosophila. In mammalian cells, high glucose or fumarate inhibits SERCA activity and increases ER calcium release and cytosolic and mitochondrial calcium levels. Mechanistically, we show that fumarate covalently modifies SERCA2b at Cys875 and that a Cys875Ser mutant resists fumarate-induced inhibition. In Drosophila, knock-in flies with the corresponding Cys875Ser mutation preserve ER calcium homeostasis and are protected from hyperglycemia, glucose intolerance, and reduced survival on a high-sugar diet. These effects are phenocopied by pharmacological fumarate reduction or allosteric SERCA activation. Collectively, these findings suggest that fumarate-mediated SERCA inhibition provides a mechanistic link between glucose metabolism and calcium homeostasis, with potential relevance to metabolic dysfunction.

PMID 42715317
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