Drug Database
ES

estradiol acetate (Menoring / Femring / Estrace VR)

✓ Approved

Actavis · ESR1 · Small Molecule

What is estradiol acetate?

estradiol acetate is a small molecule developed by Actavis. It is approved for therapeutic indications via intravaginal or surgical implantation.

Drug Profile

Brand NamesMenoring, Femring, Estrace VR
CompanyActavis
Drug ClassSmall Molecule
Molecular TargetESR1
RouteIntravaginal, Surgical Implantation
StatusApproved
Sources: ClinicalTrials.gov, Actavis

Mechanism of Action

Molecular Targets

estradiol acetate acts on 1 molecular target:

ESR1estrogen receptor 1 (ER, ESR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

estradiol acetate is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Surgical and medical proceduresHormone replacement therapy✓ Approved

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Contraception Use Differs Across Solid Organ Transplant Types Among Women Transplanted in Reproductive Age.

Cooper Katherine M KM, Mahle Rachael E RE, Joyal Kayla K, Le Mariesa M et al.

There are a growing number of reproductive age solid organ transplant (SOT) recipients, yet comparative data on contraception use across organ types are limited. We performed a retrospective cohort study of women who underwent first-time liver, kidney, heart, or lung transplantation between the ages of 18 and 45 from 2015 and 2025 using TriNetX (n=10,155). Contraception uptake within two years was assessed by organ, including patterns of initial contraceptive choice and subsequent changes in contraception choice, and clinical outcomes, including osteoporosis, thromboembolism, and graft rejection, were compared by contraception type. Among 10,155 eligible SOTR, 19.9% had documented contraception within two years of SOT (heart 27.3%, lung 22.5%, kidney 19.7%, liver 16.8%, p<0.001). Combined oral contraception was the most common initial contraception method, followed by depot medroxyprogesterone acetate (DMPA). However, those who started on DMPA were more likely to switch medications. Compared with no contraception, DMPA was associated with increased osteoporosis, hypertension, thrombosis, and graft rejection, whereas estradiol-containing agents were not. Overall, contraception use after SOT was extremely uncommon with exceedingly low rates of highly effective options, particularly after liver and kidney transplant. Higher switching and adverse associations with DMPA support early, organ-tailored contraceptive counseling and careful method selection post-SOT.

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Oxidative stress caused by production of reactive oxygen species (ROS) due to normal metabolism and/or external environment results in changes in follicular fluid microenvironment, oxidation of oocyte DNA (8‑hydroxy-2'deoxyguanosine levels; 8-OHdG) and poor-quality oocyte. Therefore, the present investigation was designed to evaluate the relationship between oocyte quality and intra-follicular environment (melatonin, 8-OHdG, 17β-estradiol and progesterone concentrations) in different sized follicles during summer and winter in water buffaloes. Slaughterhouse-derived ovaries were subjected for collection of follicular fluid from three (n = 42 each category in summer and winter) different categories of follicle based on diameter (Small: 8-9.9 mm; Medium: 10-11.9 mm; Large: 12-14 mm). Individual follicles were treated as independent observational units and analyzed using a factorial model including effects of season, follicular size, and their interaction. The results revealed higher (P < 0.05) melatonin and 17β-estradiol concentrations were associated with larger follicles and improved oocyte quality. Melatonin was positively associated (P < 0.05) with 17β-estradiol concentrations in different follicular categories during both seasons. Conversely, 8-OHdG followed an inverse association (P < 0.05) with melatonin in different categories of follicles during both seasons. Irrespective of follicles size, data revealed that good-quality oocytes (Grade A) were associated with higher melatonin concentrations, 102.11±3.88 pg/mL and 116.59±3.32 pg/mL in summer and winter, respectively. Ordinal logistic regression analysis identified melatonin concentration as the only significant independent predictor of oocyte quality (β=-0.226, OR=0.798; P < 0.001). Thus, it may be concluded that higher intra-follicular melatonin concentrations were associated with lower oxidative DNA damage and improved oocyte quality in water buffalo.

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Lead is a widespread environmental contaminant that induces multi-organ toxicity primarily through oxidative damage and inflammatory responses. Salivary glands particularly the parotid are increasingly recognized as vulnerable targets of metal-induced injury, with significant implications for oral and digestive health. This study investigated the protective effect of silymarin, a flavonolignan antioxidant extracted from milk thistle seeds, against lead acetate-induced parotid gland damage in rats. Forty adult male Wistar rats were allocated into four groups: untreated controls, silymarin only (100 mg/kg), lead acetate only (50 mg/kg), and a combined treatment group receiving silymarin (100 mg/kg) and lead acetate (50 mg/kg). Treatments were administered orally for six consecutive weeks. Parotid tissues were evaluated using histology, immunohistochemistry, ELISA, qRT-PCR, and transmission electron microscopy (TEM). Lead acetate exposure caused extensive tissue injury, including acinar vacuolation, ductal dilation, and vascular congestion, accompanied by elevated lipid peroxidation, depletion of endogenous antioxidant enzymes, activation of inflammatory signaling pathways, and upregulation of pyroptotic, apoptotic, and ferroptotic markers. TEM revealed swollen mitochondria with fragmented cristae in lead-exposed glands, hallmarks of ferroptosis. Fibrotic remodeling with collagen accumulation was also evident. Silymarin co administration was associated with significant attenuation of these pathological alterations, correlating with enhanced antioxidant defenses, reduced inflammatory mediators, lowered expression of markers linked to multiple programmed cell death pathways, and decreased fibrosis. TEM confirmed silymarin preserved mitochondrial cristae integrity. In summary, these findings suggest that silymarin may exert broad cytoprotective effects against lead induced parotid gland injury, potentially involving coordinated effects on oxidative stress, inflammation, cell death pathways, and fibrotic responses. This points to its potential therapeutic value in heavy metal toxicity, pending further validation.

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The pathophysiological roles of sex hormones in airway inflammation have drawn much attention recently. We aimed to explore the causal effect of sex hormones on chronic rhinosinusitis (CRS) and nasal polyps (NP) via a Mendelian randomization (MR) study. Genetic traits for serum bioavailable testosterone (BioT), total testosterone (ToT), sex hormone-binding globulin (SHBG), and estradiol were extracted from a genome-wide association study (GWAS) containing 425,097 European individuals from the UK Biobank, while outcome data were obtained from the FinnGen data set. Two-sample MR analysis was performed to assess the association of sex hormones and NP or CRS with the inverse variance weighted method as the main analysis, together with sensitivity analyses. Genetically predicted BioT levels showed a possible inverse association with both NP (OR = 0.669, p = 0.009) and CRS (OR = 0.792, p = 0.014) in the overall population, though these associations were marginally above the traditional significance threshold after multiple testing correction (FDR = 0.054). Sex-stratified analyses revealed potentially stronger protective associations in females, with higher BioT associated with lower odds of NP. No significant causal effects of estradiol or SHBG on NP or CRS were identified in the available GWAS data. Our MR analyses suggest a possible inverse relationship between genetically predicted serum BioT levels and the risk of both CRS and NP, with potentially stronger effects in females. Further observational and experimental studies are necessary to validate these genetic associations and explore the potential immunomodulatory mechanisms by which testosterone may influence sinonasal inflammation.

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Megasphaera cerevisiae is a well-known beer spoilage organism, capable of producing undesirable flavours and turbidity. Although the biosynthesis of medium-chain fatty acids (MCFAs) has been extensively studied in different Megasphaera species, the metabolic behaviour of M. cerevisiae in controlled environments remains largely unexplored. This study examines the MCFAs production from diverse substrates and reports flux analyses of core metabolism for the first time using a genome-scale model. The results suggest that acetate stimulates butyrate production but not caproic acid production. Butyrate supplementation, either alone or in combination with acetate, promoted CA synthesis. Lactate supplementation primarily led to the formation of propionic acid and acetic acid. The metabolic network model was manually curated and validated against the different experimental data. The metabolic flux results showed that butyrate production facilitated via the reverse β-oxidation (RBO) pathway, with a minor contribution from the fatty acid synthesis (FAS) pathway. Conversely, CA synthesis was mainly synthesised through the FAS pathway, irrespective of the substrate used. The pathway analyses results highlighted the critical role of hydrogen production in M. cerevisiae metabolism, particularly under conditions where lactate is utilised. Collectively, these findings offer novel insights into the metabolic versatility and pathway preferences of M. cerevisiae.

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Visible-light-promoted catalyst-free benzylic C-H oxidation using molecular oxygen as a green oxidant.

Li Jianing J, Wang Suwen S, Sun Huinan H, Liu Zhunchao Z et al.

Herein, we report a catalyst- and additive-free strategy for the visible-light-promoted carbonylative oxidation of benzylic C-H bonds employing molecular oxygen as the sole oxidant. This operationally simple protocol enables the conversion of a broad range of aromatic alkanes into valuable ketones, including complex drug derivatives and intermediates under mild conditions using ethyl acetate as a green solvent. Mechanistic studies reveal that the reaction proceeds via a substrate-oxygen charge-transfer (CT) complex upon photoexcitation, generating reactive oxygen species (singlet oxygen and superoxide anion) and a key benzylic radical. Interestingly, the carbonyl product can further accelerate the transformation by participating in a separate CT complex with the starting material. To address the scalability limitations, a novel solvent-free continuous-flow photoreactor was developed, which demonstrated a significant efficiency enhancement of over 150-fold compared to batch processes. This work presents a green, practical, and scalable method for benzylic oxidation, underpinned by a detailed mechanistic understanding of the photoinduced CT process.

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