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estradiol acetate (Menoring / Femring / Estrace VR)

✓ Approved

Actavis · ESR1 · 小分子

什么是 estradiol acetate?

estradiol acetate 是一种小分子,由Actavis研发。该药已获批,用于治疗相关适应症,给药途径:Intravaginal、Surgical Implantation。

药物档案

商品名Menoring, Femring, Estrace VR
公司Actavis
药物类别小分子
分子靶点ESR1
给药途径Intravaginal, Surgical Implantation
状态Approved

作用机制

分子靶点

estradiol acetate 作用于 1 个分子靶点:

ESR1estrogen receptor 1 (ER, ESR)
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

estradiol acetate 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
Surgical and medical proceduresHormone replacement therapy✓ Approved

相关研究文献

PubMedAnnals of African medicine2026-10-27

A Systematic Review of Elagolix for the Management of Endometriosis-associated Pain.

Aafreen Sana S, Haque Ekramul E, Kumar Tushar T

Endometriosis is a chronic, estrogen dependent condition affecting up to 10% of women of reproductive age, characterized by dysmenorrhea, dyspareunia, and nonmenstrual pelvic pain. Conventional treatments are often limited by inadequate efficacy or tolerability. Elagolix, an oral nonpeptide gonadotropin releasing hormone (GnRH) antagonist approved by the Food and Drug Administration in 2018, offers dose dependent estrogen suppression with rapid reversibility upon discontinuation. This systematic review synthesizes the current evidence on elagolix for the management of endometriosis associated pain. A comprehensive search was conducted across PubMed, Embase, Cochrane Library, Web of Science, and ClinicalTrials.gov from inception to September 2024. Studies were screened per Preferred Reporting Items for Systematic Reviews and Meta Analyses guidelines and quality appraised using the a measurement tool to assess systematic reviews 2. (AMSTAR 2) checklist. From 103 identified records, 20 studies were included, encompassing Phase II/III randomized controlled trials, long term extension studies, systematic reviews, network meta analyses, real world data analyses, postmarketing safety reports, and cost effectiveness studies. Elagolix significantly reduced dysmenorrhea (up to ~75% responder rate), nonmenstrual pelvic pain (~55%-69%), and dyspareunia (~60%) compared to placebo, with benefits sustained at 12 months. Efficacy was dose dependent; higher doses yielded greater symptom relief but increased hypoestrogenic adverse effects, primarily hot flushes and decreased bone mineral density (BMD). BMD loss remained minimal (<2% annually) with add back estradiol/norethindrone acetate therapy. Network meta analyses demonstrated comparable or superior efficacy versus other oral GnRH antagonists. Elagolix was cost effective compared to leuprolide acetate in the US settings, and patients favored its oral administration. Elagolix represents an effective, patient centered therapeutic option for moderate to severe endometriosis associated pain, with a well characterized safety profile. Future research should address long term safety beyond 48 months, direct comparisons with first line hormonal therapies, and cost effectiveness in non US healthcare settings.

PMID 42937421
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PubMedAntonie van Leeuwenhoek2026-10-27

Therapeutic potential of the exometabolic crude ethyl acetate extract of an endophytic Bacillus sp. against multidrug-resistant pathogens associated with cancer patients.

Elebiary Deyaa M DM, El-Sherbiny Gamal M GM, Sharaf Mohamed H MH, Elnady Maha S MS et al.

The alarming emergence of multidrug-resistant bacterial pathogens (MDRBPs), esp.ecially associated with cancer patients, necessitates the exploration of novel biological agents as endophytic microorganisms that are natural reservoirs of bioactive substances. The purpose of the present study was to isolate endophytic bacteria and evaluate the exometabolic crude ethyl acetate extract against MDRBPs in vitro and in vivo, study their effects on cancer cells and wound recovery, and elucidate some mechanisms supporting their efficacy. In our study, a bacterium was isolated from Sp.inacia oleracea and identified as a Bacillus isolate closely related to Bacillus amyloliquefaciens and deposited in GenBank as PX736878. The exometabolic crude ethyl acetate of Bacillus sp. exhibited a strong antibacterial activity against MDRBPs, and the highest activity was against Klebsiella pneumoniae (21.2 mm). The MIC values showed its efficacy, particularly at 500 µg/ml. The extract also exhibited significant anti-biofilm activity sp.ecifically against K. pneumoniae. The cytotoxicity assays showed a selective toxicity of Bacillus sp. extract against the cancer cell lines (HCT116 and MCF7). In vivo, significant wound healing potential of the exometabolic crude ethyl acetate of Bacillus sp. was demonstrated by histological evidence of near-normal tissue regeneration. The strong activities exometabolic crude ethyl acetate of Bacillus sp. were due to the high antioxidant capacity. GC-MS analysis further supported our results and identified diverse bioactive compounds in the exometabolic crude ethyl acetate of Bacillus sp., including Diketopyrazine, fatty acids, and dipeptides. In conclusion, the extract of exometabolic crude ethyl acetate extract of Bacillus sp. is a promising multifunctional agent with strong antibacterial, anti-biofilm, antioxidant, and anticancer properties. This could be a new way to fight MDRBPs and aid damaged tissue to heal.

PMID 42934348
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PubMedSmall (Weinheim an der Bergstrasse, Germany)2026-10-27

Pluripotent Hydrogels With Ion-Tempered Mechanical Properties.

Lu Jianlei J, Guan Xin X, Jia Jiangpeng J, He Xinyue X et al.

Functional soft materials have a wide application prospect in many fields. However, these materials often have elaborately designed polymer network structures to generate unique performance for specific applications. In this work, we present a versatile strategy for adjusting the mechanical properties and thermoresponsive behaviors of hydrogels by ion-tempering, enabling their application in diverse scenarios. Thermoresponsive hydrogels with versatile applications are prepared by treating non-thermoresponsive poly(acrylic acid) (PAA) hydrogels with acetate solutions containing metal ions of Mg2+, Ca2+, Sr2+, Mn2+, Ni2+, and Zn2+, respectively. Except for poly(acrylic acid)/ magnesium acetate (PAA/MgAc), all the other hydrogels exhibit thermo-induced phase separation behavior and shape memory properties with tunable hysteresis ratios. By exploiting the controllable recovery behavior of stretch-programmed hydrogels, the poly(acrylic acid)/ manganese acetate (PAA/MnAc) hydrogel could be applied as artificial muscles and generate effective contractile actuation. Furthermore, the strong ionic bonds within the poly(acrylic acid)/zinc acetate (PAA/ZnAc) hydrogel provide remarkable energy dissipation capability, rendering it ideal for damping and impact protection applications.

PMID 42935001
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PubMedNan fang yi ke da xue xue bao = Journal of Southern Medical University2026-10-27

[Positive association of exposure to per- and polyfluoroalkyl substances with arterial stiffness parameters and its interaction with sex hormone levels].

Zheng Chaoyuan C, Yu Yinglei Y, Zhang Haoyan H, Li Ying Y et al.

To examine the associations of per- and polyfluoroalkyl substances (PFAS) with estimated pulse wave velocity (ePWV) and assess their interactions with estradiol and testosterone. Based on the data of healthy adults with measurements of 5 PFAS from NHANES 2013-2016, we assessed linear and nonlinear associations of exposure to a single PFAS with ePWV using weighted linear regression and restricted cubic spline (RCS) models; weighted quantile sum (WQS) regression was used to estimate the association of PFAS mixture exposure with ePWV with additional age-stratified WQS analyses, and ePWVs between high and low mixture exposure groups were compared using doubly robust estimation. Additive and multiplicative interactions between PFAS and sex hormones were evaluated. After covariate adjustment, all the 5 PFAS were positively associated with ePWV. RCS analyses indicated that only PFOS had a significant nonlinear association with ePWV. WQS regression showed a positive association between PFAS mixture exposure and ePWV. Perfluorooctane sulfonate (PFOS) and perfluorohexane sulfonate (PFHS) contributed the most to the WQS index with weights of 47.5% and 24.3%, respectively. Age-stratified WQS analyses showed that positive association was mainly observed in middle-aged and older adults, with PFOS and PFHS retaining high weights across different age groups. In doubly robust analysis, ePWV was 1.284 m/s higher in the high- than in low-mixture exposure group (95%CI:1.078-1.490; P<0.001). Multiplicative interaction analyses suggested weaker positive PFAS-ePWV associations in participants with high estradiol or testosterone levels. Both of the sex hormones showed negative interactions with PFHS; estradiol also interacted negatively with PFOS and PFNA, whereas testosterone interacted negatively with PFOA. PFAS exposure is associated with an elevated ePWV, with PFOS and PFHS as the key driving components. The positive association between PFAS and ePWV is relatively weaker in individuals with high levels of sex hormones.

PMID 42934108
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PubMedCurrent issues in molecular biology2026-10-27

CARTPT and FSH Signaling in Ovarian Follicle Development as an Emerging Link to Oocyte Quality and Female Infertility.

Voros Charalampos C, Chatzinikolaou Fotios F, Papadimas Georgios G, Athanasiou Diamantis D et al.

Not all ovarian follicles respond to follicle-stimulating hormone (FSH) in the same way. This difference is usually attributed to FSH receptor expression and local ovarian factors, but the role of CARTPT has received far less attention. Studies in granulosa cells have shown that cocaine- and amphetamine-regulated transcript (CART) can reduce FSH-induced cAMP production, aromatase expression, and estradiol synthesis. CARTPT expression has also been found to be higher in subordinate and atretic follicles in several animal models. Its regulation by leptin suggests a possible connection between metabolic status and follicular function. Early human findings have linked follicular CART expression with ovarian response and oocyte yield. In cattle and buffalo, CART suppressed FSH-stimulated cAMP production, aromatase expression, and estradiol output in granulosa cells and marked follicles destined for atresia, a pattern not confirmed in the one available porcine study. The receptor mediating these effects in the ovary remains unidentified, though a CART receptor was recently confirmed in another endocrine tissue. Human evidence linking CARTPT to ovarian response and oocyte quality remains preliminary and correlative. CARTPT therefore emerges as a mechanistically well-supported but clinically unproven contributor to FSH resistance and impaired oocyte quality, and this review outlines the loss-of-function and prospective human studies needed to establish its clinical relevance.

PMID 42939561
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PubMedNutrients2026-10-27

Associations Between Gut Microbiota Abundance, Dietary Purine Intake, and Fecal Short-Chain Fatty Acids Across the Clinical Spectrum of Hyperuricemia: A Cross-Sectional Study in Mexican Adults.

Fuentes-Bello Alim Caelli AC, Guevara-Gonzalez Karla Vanessa KV, Granados-Portillo Omar O, Sánchez-Lozada Laura Gabriela LG et al.

Hyperuricemia and gout are closely associated with alterations in gut microbiota function. Short-chain fatty acids (SCFAs) produced by intestinal microorganisms may modulate immune responses and inflammation relevant to gout pathophysiology. This study evaluated fecal SCFA concentrations, their associations with dietary purine intake, and the relationship between Akkermansia spp. and Prevotella spp. abundance and fecal SCFA profiles across the clinical spectrum of hyperuricemia. This cross-sectional study included 380 Mexican adults: normouricemic controls (n = 141), individuals with asymptomatic hyperuricemia (AH; n = 98), and patients with gout (n = 141). Fecal SCFAs were quantified by GC-FID and bacterial abundance by qPCR. Dietary intake was assessed by semi-quantitative food frequency questionnaire and classified by purine content. Between-group differences were evaluated by the Kruskal-Wallis test (Benjamini-Hochberg correction); multivariable linear regression adjusted for age, sex, and BMI was used to assess associations, including a pre-specified dietary purine intake per clinical group interaction term. Fecal acetate and propionate were significantly higher in gout patients than controls, whereas AH individuals had significantly higher butyrate. Moderate-purine food intake showed opposing associations with fecal acetate in controls (β = +3.61, p = 0.019) and gout patients (β = -4.59, p = 0.036), with a significant interaction (p = 0.004). Exploratory analyses revealed a positive association between Prevotella spp. abundance and fecal acetate exclusively in the gout group (β = 0.085, p = 0.020). These findings suggest distinct fecal SCFA profiles across stages of urate-related disease, with a disease-specific gut metabolic response to dietary purine intake potentially contributing to the inflammatory environment of established gout. Longitudinal studies with whole-microbiome profiling are needed to establish causality.

PMID 42942896
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