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

Related Research Articles

PubMedUrologie (Heidelberg, Germany)2026-09-20

[Gender-affirming hormone therapy: state of the art].

Bischoff Jenny J

Gender incongruence affects approximately 0.6% of the population in Germany and, when accompanied by significant psychological distress, may constitute an indication for gender-affirming hormone therapy (GAHT). The increasing diversity of gender identity has led to a more individualized approach to hormone therapy. The decision to initiate treatment is based on the expected reduction in gender-related dysphoria due to hormonal treatment. Treatment is carried out in accordance with guidelines and is tailored to the wishes and goals of the person seeking treatment. Various estradiol preparations and antiandrogenic substances can be used to achieve feminization. Masculinizing therapy relies primarily on testosterone. For non-binary individuals, GAHT is usually administered at lower doses and typically focuses on specific aspects of gender alignment. The therapeutic effects usually develop slowly but can be irreversible and significant. Risks should be assessed in advance, and patients should be informed about potential adverse effects. Monitoring and adjustment of treatment take place at specified regular intervals. Adjustments and support throughout the course of treatment-ranging from fertility preservation to cancer screening-are key components of comprehensive care in patients undergoing GAHT. Although the evidence regarding GAHT has improved significantly in recent years, large-scale studies are still lacking for many aspects.

PMID 42763335
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PubMedTransplant international : official journal of the European Society for Organ Transplantation2026-09-19

Menopause influences lung inflammatory response and miRNA expression in brain death donors.

Miola Elizabeth Cristina EC, Toneto Nicholas Pietro Agulha NPA, Yamamoto Ricardo-da-Silva Fernanda F, de Freitas Pedro Luis Zonta PLZ et al.

Lungs are highly affected by brain death, with females showing a higher inflammatory response, linked sex hormones acute reduction. With the aging of world population, the number of older donors is increasing. So, the study of menopause associated changes gain importance. Here we investigated menopause's effects in female brain death rats, previously subjected to transitional follicular depletion and aging. Female Wistar rats were divided in young and menopause groups. After follicular depletion, rats aged for 10 weeks. The animals were submitted to brain death and Sham operated rats served as controls. White blood cell counts, bronchoalveolar lavage were analyzed and inflammatory mediators were quantified. Lung tissue was evaluated for myeloperoxidase, intercellular adhesion molecules, miRNA expression, and protein and gene expression of estradiol receptors. In menopause group, there was increase in systemic and tissue leukocyte infiltration, myeloperoxidase expression, inducible nitric oxide synthase, intercellular adhesion molecule-1, lung edema, and loss of IL-10 regulation. Additionally, we found alterations in estradiol receptors along with changes in the expression of miRNAs associated to inflammation, vascular function and senescence. Menopause increases lung inflammation after brain death, by higher leukocyte infiltration and reduction of IL-10 and may impact the outcome of lung transplantation.

PMID 42761501
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PubMedJournal of complementary & integrative medicine2026-09-19

In vitro, in vivo, and computational evaluation of xanthine oxidase inhibitory and antihyperuricemic activities of Piper betle L. ethyl acetate fraction.

Hao Bui Thi BT, Minh Phan Hong PH, Anh Hong Nguyen Thi NT, Nhat Hoang Nam HN et al.

Gout is a metabolic disorder characterized by hyperuricemia and urate crystal deposition. This study evaluated the xanthine oxidase inhibitory, antihyperuricemic, anti-inflammatory, analgesic, and in silico target-binding properties of an EtOAc fraction of Piper betle L. aerial parts. P. betle aerial parts were extracted with ethanol and partitioned to obtain an EtOAc fraction. Xanthine oxidase inhibition was evaluated spectrophotometrically, and antihyperuricemic activity was examined in potassium oxonate-treated mice given the fraction (200 or 600 mg/kg). Carrageenan-induced paw edema and acetic acid-induced writhing were used to assess anti-inflammatory and analgesic effects. Hydroxychavicol was docked with xanthine oxidase, cyclooxygenase-2, and transient receptor potential vanilloid 1, followed by molecular dynamics simulations. The ethyl acetate fraction inhibited xanthine oxidase with an IC50 of 4.28 ± 0.15 μg/mL, whereas allopurinol showed an IC50 of 1.06 ± 0.07 μg/mL. In hyperuricemic mice, serum uric acid showed a decreasing trend, and urinary uric acid was significantly reduced at 600 mg/kg. Paw edema was reduced at 600 mg/kg, whereas writhing responses were not significantly inhibited. Docking predicted favorable hydroxychavicol binding to the three targets, but molecular dynamics indicated weaker ligand retention in the xanthine oxidase complex than in the cyclooxygenase-2 and transient receptor potential vanilloid 1 complexes. The ethyl acetate fraction of P. betle demonstrated preclinical xanthine oxidase inhibitory, urate-lowering, and anti-inflammatory potential. Stronger chemical standardization and mechanistic validation are required before therapeutic relevance can be inferred.

PMID 42762091
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PubMedEndocrine regulations2026-09-19

Estrogens hypersensitivity syndrome in endometriosis.

Rukhliada Nikolai Nikolaevich NN, Dudova Kristina Andreevna KA

Objectives. The aim of the study was to develop a diagnostic method for estrogen hypersensitivity syndrome in proliferative benign diseases of the female reproductive system. Using the example of endometriosis, changes in the activity of the chaperone protein Hsp90α were determined as a diagnostic biomarker. Methods. The study included 60 women aged 30 to 50 years, thirty of whom had a laparoscopically confirmed diagnosis of endometriosis and 30 were included in the control group. After blood sampling to determine the baseline levels of Hsp90α, the patients were prescribed a single oral dose of estradiol valerate 2 mg tablet. The plasma Hsp90α levels were remeasured 6 h later. Results. No significant change (p>0.05) in baseline Hsp90α concentrations was found between the group of patients with endometriosis and the control group. Six hours after estradiol valerate administration, a significant difference (p<0.001) in Hsp90α levels was observed between the group of patients with endometriosis and the control group. The increase in Hsp90α concentration following the test-load was also more pronounced in women with confirmed endometriosis compared to controls (27.29±15.62 ng/ml and 3.16±4.36 ng/ml, respectively) (p<0.001). ROC analysis indicated that the absolute increase in Hsp90α level of more than 8.6 ng/ml in patients with endometriosis has a sensitivity of 0.93 and a specificity of 0.97 (compared to the control group). This change in relative concentration corresponded to an increase of over 28.7%. Conclusion. The increase in Hsp90α plasma level of more than 30% within 6 h after the test-load is a specific criterion for estrogen hypersensitivity syndrome in endometriosis. Further investigation including other nosological forms (myoma, adenomyosis, endometrial hyperplasia) is required.

PMID 42762506
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PubMedFood chemistry: X2026-09-19

Key aroma contributors and perceptual interactions of dried longan-like aroma in lapsang souchong black tea with different natural aging times.

Shi Yutao Y, Zuo Lirong L, Huang Canyang C, Zhou Yanhua Y et al.

This study investigated aroma evolution in Lapsang Souchong black tea (LS) with different natural aging times and the perceptual basis of its dried longan-like aroma. Sensory evaluation, HS-SPME-GC-MS, aroma recombination/omission, S-curve-Feller analysis, and molecular simulations showed that, with increasing natural aging time, LS aroma shifted from pine-smoke, sweet, and fruity aroma dominance to prominent dried longan-like aroma, followed by enhanced woody and aged aromas. LS19 showed the highest dried longan-like aroma intensity. Benzaldehyde, Geranyl acetate, and 2-Acetylfuran were identified as key contributors. Binary mixtures mainly showed additive effects, whereas the ternary system exhibited a synergistic effect. Molecular simulations suggested stable binding of the key aroma compounds with the candidate olfactory receptor OR1A1 (-53.89 kcal/mol), with ILE126 and VAL227 identified as key binding residues. These findings clarify the material basis and perceptual features of dried longan-like aroma and support LS quality evaluation, storage management, and aroma regulation.

PMID 42761899
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PubMedTheriogenology2026-09-19

CPT1A alters granulosa cell proliferation and steroidogenic activity in association with fatty acid oxidation during goat follicular development.

Song Shuaifei S, Yang Mingzhi M, Li Jiayue J, Wang Zihan Z et al.

Follicular development in goats relies on the extensive proliferation and hormone synthesis of granulosa cells (GCs), processes that require an adequate energy supply. Fatty acid oxidation (FAO) represents a primary energy source for granulosa cells. However, how its rate-limiting enzyme, carnitine palmitoyltransferase 1A (CPT1A), modulates granulosa cell function remains unclear. This study examined CPT1A expression in healthy and atretic follicles and investigated its association with FAO-associated gene expression, ATP generation, proliferation, steroidogenesis, and palmitic acid (PA)-induced ferroptosis-associated responses in goat granulosa cells. Compared with healthy follicles, CPT1A protein expression was significantly higher in atretic follicles. In vitro experiments demonstrated that CPT1A overexpression upregulated the expression of FAO-associated genes and elevated intracellular ATP levels, whereas CPT1A knockdown produced the opposite effects. Moreover, CPT1A expression was positively associated with granulosa cell proliferation and steroidogenesis, as evidenced by increased PCNA expression, EdU-positive rates, the expression of steroidogenesis-associated proteins, and the secretion of estradiol and progesterone. Conversely, CPT1A knockdown inhibited cell proliferation and reduced steroidogenic activity. Additionally, PA treatment increased CPT1A expression, which was accompanied by ferroptosis-associated changes, including elevated lipid peroxidation and ROS accumulation, alongside reduced GSH levels. In summary, this study reveals the critical role of CPT1A as a potential metabolic regulator in goat granulosa cells, providing new insights into the metabolic mechanisms underlying follicular development and suggesting that CPT1A may serve as a key molecular target for understanding reproductive regulation in goats.

PMID 42762603
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