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estradiol (Estreva oral / Estreva / Estreva gel)

✓ Approved

Merck KGaA · ESR1 · Small Molecule

What is estradiol?

estradiol is a small molecule developed by Merck KGaA. It is approved for therapeutic indications via oral (po) or transdermal.

Drug Profile

Brand NamesEstreva oral, Estreva, Estreva gel
CompanyMerck KGaA
Drug ClassSmall Molecule
Molecular TargetESR1
RouteOral (PO), Transdermal
StatusApproved
Sources: ClinicalTrials.gov, Merck KGaA

Mechanism of Action

Molecular Targets

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

Therapeutic AreaConditionPhase
Surgical and medical proceduresHormone replacement therapy✓ Approved

Related Research Articles

PubMedFood chemistry2026-05-20

Mechanism of pH-driven gelation in Tremella fuciformis polysaccharide-soy protein isolate composite systems.

Zhao Yingting Y, Wang Danni D, Chen Xinyi X, Cheng Lujie L et al.

The gelling properties of soy protein isolate (SPI) are limited, but can be enhanced by adding polysaccharides, with their interactions strongly influenced by pH. This paper explored the effects of pH (5-9) on gel mechanisms of Tremella fuciformis polysaccharide (TFP)-SPI complexes. Results showed that 1) at pH 7, the TFP-SPI composite gels exhibited superior rheological properties, hardness, water-holding behavior, and thermal stability whereas these properties were significantly destroyed under acidic/alkaline conditions, especially under acidic conditions; 2) the hydrophobic interaction of TFP-SPI composite gel was strong at pH 7 but decreased under acidic/alkaline conditions; 3) the hydrophobic and electrostatic interactions mainly drove TFP-SPI gel formation, particularly under neutral and alkaline conditions. In contrast, hydrogen bonds played the smallest role in the composite gels across conditions. Overall, the findings suggest that neutral pH favors TFP-SPI gel formation, offering guidance for designing heat-induced food gel systems, such as plant-based meat analogs or functional puddings.

PMID 42155261
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PubMedImaging neuroscience (Cambridge, Mass.)2026-05-20

Connectivity of the right cerebello-left hippocampal circuit across adulthood.

Hicks Tracey H TH, Magalhães Thamires N C TNC, Bernard Jessica A JA

Direct communication between the hippocampus and cerebellum has been shown via coactivation and synchronized neuronal oscillations in animal models. Further, the cerebello-hippocampal circuit has been under-investigated in the human brain and may be impacted by sex steroid hormones. The cerebellum and hippocampus are dense with estradiol and progesterone receptors relative to other brain regions. Females experience up to a 90% decrease in ovarian estradiol production after the menopausal transition. Postmenopausal women show lower cerebello-cortical functional connectivity (FC) compared to reproductive aged females. Further, sex hormones are established modulators of both memory function and synaptic organization in the hippocampus in non-human animal studies. However, investigation of the cerebello-hippocampal (CB-HP) circuit has been limited to animal studies and small homogeneous samples of young adults as it relates to spatial navigation. Here, we investigate the CB(right)-HP(left) circuit in 138 adult humans (53% female) from 35-86 years of age, to define its FC patterns, and investigate its associations with behavior, hormone levels, and sex differences therein. We demonstrated robust FC patterns between the right CB and left HP in this sample. We predicted and found negative relationships between age and CB-HP FC. As expected, estradiol levels exhibited positive relationships with CB-HP connectivity. We found lower CB-HP FC with higher levels of progesterone. We provide the first characterization of the CB-HP circuit across middle and older adulthood and demonstrate that connectivity is sensitive to sex steroid hormone levels. This work provides the first clear CB-HP circuit functional mapping in the human brain and serves as a foundation for future work in neurological and psychiatric diseases.

PMID 42158340
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PubMedBiological trace element research2026-05-20

Effects of Boron on the Lipid Metabolism, Estradiol Concentration, Uterine Morphology and ERα Expression in Ovariectomized Rats.

Li Ziyan Z, Liu Qinglan Q, Wang Lin L, Wang Chun C et al.

This study aimed to evaluate the effects of boron on the lipid metabolism, estradiol concentration, uterine morphology and ERα expression in ovariectomized rats. Seventy 3-month-old female SD rats were selected and randomly divided into a sham-operated group and an ovariectomized group. After one week of surgical recovery, sham-operated rats were divided into Sham (distilled water) and Sham+B40 (40 mg/L boron) groups. Ovariectomized rats were allocated to OVX (control), OVX + Est (estrogen), OVX+B20 (20 mg/L boron), OVX+B40 (40 mg/L boron) and OVX+B80 (80 mg/L boron) groups. During the 22-week experiment period, body weight was recorded; serum lipid profiles (TC, TG, LDL-C and HDL-C) and estradiol (E2) levels were detected; uterine morphology was observed; uterine ERα expression was analyzed via qRT-PCR and immunohistochemistry. The results showed that the body weight and lipid metabolism levels in the three boron-supplemented groups were generally increased compared to those of the OVX group and the Sham group. The concentration of E2 was increased to a different degree. Uterine area and endometrial thickness increased with 20 mg/L and 40 mg/L boron but decreased at 80 mg/L. Although the expression levels of uterine ERα in the three boron-supplemented groups were different degree increased, the 20 mg/L group was showed the best result. Therefore, that boron demonstrates estrogen-modulatory effects, which can effectively improve the estrogen deficiency symptoms in ovariectomized rats, regulate lipid metabolism disorders, increase E2 concentration, alleviate degree of the uterine atrophy and promote the expression of ERα, especially the low-concentration (20 mg/L) boron has a better effect.

PMID 42159655
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PubMedJournal of controlled release : official journal of the Controlled Release Society2026-05-20

Composite biomaterials of polyelectrolyte complex micelle nanoparticles in hyaluronic acid gels enable local, targeted miR-92a inhibition and enhanced angiogenesis in diabetic wound repair.

Xi Brian J BJ, Wang Siyang S, Lozada Bernice M BM, Alpar Aaron T AT et al.

Diabetic wounds are characterized by various cellular deficiencies, particularly insufficient angiogenesis. MicroRNA 92a (miR-92a) is a known factor in diabetic wounds that perpetuates non-healing wound phenotypes by inhibiting angiogenesis. Therefore, its local inhibition at wound sites has therapeutic potential. To achieve this, we combine a nanoparticle formulation of polyelectrolyte complex micelles (PCMs) delivering miR-92a inhibitors with a hyaluronic acid (HA) gel formulation suitable for topical application to wound sites. The nanoparticles, formed by polyelectrolyte complexation of poly(ethylene glycol)-block-poly(l-lysine) with RNA cargo, are functionalized with targeting peptides against vascular cell adhesion molecule 1 (VCAM-1) to improve affinity for inflamed endothelial cells. We demonstrate effective PCM encapsulation and controlled release from gel formulations in vitro and in vivo. These PCMs are taken up in vivo by endothelial cells and exert functional transcriptional effects on miR-92a and its downstream targets. Furthermore, our composite PCM-gel formulation significantly accelerates wound closure in diabetic mouse models and improves angiogenesis, consistent with the known role of miR-92a inhibition in vascular regeneration. This work demonstrates a highly translatable formulation for improved wound healing, and lays the framework for modular nanoparticle-gel systems that can achieve local, cell-targeted RNA delivery.

PMID 42155602
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PubMedBioscience, biotechnology, and biochemistry2026-05-20

Thymol gel ameliorates anesthesia-related postoperative neuropathic pain: Modulation of inflammatory mediators in a rat model.

Fan Hu H, Xiong Wenfeng W, Liu Liming L, Zhang Chengzhe C et al.

This study investigated the molecular mechanisms and therapeutic efficacy of chitosan-based thymol gels (2.5%, 5%, and 10%) in postoperative neuropathic pain. Gels exhibited pseudoplastic shear-thinning behavior and a biphasic release profile, achieving > 90% cumulative release within 12 h. Using a Wistar rat model of hind paw incision, topical treatment with 5% and 10% thymol gels significantly (p < 0.05) reversed the reduction in paw withdrawal latency and threshold compared to the controls. Thymol gel markedly decreased serum corticosterone, cyclooxygenase-2 (COX-II), and prostaglandin E2 (PGE2) levels. Furthermore, it downregulated the messenger ribonucleic acid (mRNA) expression of interleukins and tumor necrosis factor in the sciatic nerve. Histopathological analysis confirmed reduced inflammation and congestion. Positive correlations were observed between pro-inflammatory cytokine expression and serum corticosterone, PGE2, and COX-II levels. These findings suggest that thymol gel effectively ameliorates anesthesia-related postoperative neuropathic pain by modulating key inflammatory mediators, suggesting its beneficial treatment option for alleviating such pain.

PMID 42159308
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PubMedRSC advances2026-05-20

Ratio-tuned green-synthesized Ag-Fe bimetallic nanoparticles embedded in electrospun gelatin/chitosan nanofibrous scaffolds for antibacterial applications.

Asad Nour Alhuda NA, Erci Fatih F, Bayram Fatma F

Wound and device-associated infections caused by drug-resistant microorganisms are a major global health problem, increasing morbidity, mortality and economic burden. Antimicrobial nanofibrous scaffolds have therefore gained attention as wound dressings capable of reducing infection risk. In this study, gelatin/chitosan (GEL/CTS) nanofibrous scaffolds incorporating silver-iron bimetallic nanoparticles (Ag-FeNPs) synthesized via a green route using Hypericum perforatum (H. perforatum) leaf extract were developed as potential antibacterial wound-dressing materials. Ag-FeNPs were produced at room temperature and characterized by different analytical techniques. Microstructural analysis confirmed that the biogenic nanoparticles were spherical, with an average size of 60.98 ± 18.09 nm, and were uniformly distributed throughout the GEL/CTS fibers. Ag-FeNPs with varying Ag : Fe ratios were subsequently embedded into the polymeric matrix to enhance scaffold wettability and antibacterial performance. FT-IR, XRD, FE-SEM, and water-contact-angle measurements demonstrated that incorporation of CTS and Ag-FeNPs reduced the fiber diameter (171.47 ± 55.96 nm) and improved hydrophilicity, with the GEL/CTS/Ag-Fe (2 : 1) formulation exhibiting the lowest WCA value (60.72°). Antibacterial assays conducted against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli) revealed that the green-synthesized Ag-FeNPs were active against both strains, with stronger inhibition observed for E. coli. Among the nanofibrous scaffolds, the sample containing the highest Ag composition yielded the most pronounced reduction in bacterial colony formation. Overall, these findings indicate that GEL/CTS scaffolds reinforced with Ag-FeNPs possess favorable structural and biological properties, which highlighting their potential as effective antibacterial materials for applications such as wound dressings.

PMID 42158745
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