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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

PubMedFrontiers in medicine2026-07-17

Identification of key vaginal microbial signatures and immune remodeling associated with HR-HPV clearance following Kushen Gel treatment: a longitudinal analysis.

Wang Ying Y, Pan Shuheng S, Zhang Fengying F, Ma Huimin H et al.

Persistent high-risk human papillomavirus (HR-HPV) infection drives cervical carcinogenesis, often exacerbated by vaginal dysbiosis and localized immune dysfunction. Kushen Gel shows clinical promise, yet its impact on microbial-immune crosstalk during HR-HPV clearance remains unclear. This study elucidates the microbial remodeling and immune shifts associated with Kushen Gel-mediated HR-HPV regression. A retrospective analysis of 230 vaginal swabs (130 pre-treatment, 100 post-treatment) via 16S rRNA sequencing characterized community structural shifts. Subsequently, a prospective cohort of 35 patients with persistent HR-HPV infection (defined as laboratory-confirmed positive HR-HPV DNA for ≥12 months) validated clinical outcomes (HR-HPV clearance, vaginal pH, Nugent scores) alongside paired 16S rRNA sequencing and ELISA-based quantification of cervicovaginal cytokines (IL-8, IL-6, TNF-α, IFN-γ). Kushen Gel intervention significantly decreased microbial alpha diversity and was associated with a distinct beta-diversity shift toward a stable, Lactobacillus-dominant state. Models (LEfSe, Random Forest) identified a marked reduction in pathobionts (Gardnerella, Sneathia, Prevotella) post-treatment. In the prospective cohort, the HR-HPV clearance rate reached 82.9% (29/35) after three menstrual cycles, synchronized with significant reductions in mean vaginal pH (4.85 ± 0.42 to 4.12 ± 0.35, p < 0.001) and an 85.7% Nugent score normalization rate. Crucially, Kushen Gel treatment was associated with a profound shift from a pro-inflammatory to an anti-viral immune microenvironment. Pro-inflammatory markers (IL-8, IL-6, TNF-α) plummeted significantly (p < 0.0001), while anti-viral IFN-γ exhibited a robust increase (3.2 ± 1.1 to 18.6 ± 5.4 pg./mL, p < 0.0001), particularly in responders. Lactobacillus abundance positively correlated with IFN-γ (r = 0.68) and inversely with IL-8 (r = -0.54). Kushen Gel is associated with HR-HPV clearance and concurrent vaginal microenvironment remodeling, marked by suppressed anaerobic-driven inflammation and an enhanced IFN-γ-associated anti-viral niche dominated by Lactobacillus. These findings biologically support using Kushen Gel to manage vaginal dysbiosis and HR-HPV regression.

PMID 42465087
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PubMedAdvanced functional materials2026-07-17

Self-Assembled Nanoclay Gel with Spheroid MSC-Derived Exosome Mimetics to Integrate Demineralized Bone Matrix and Noggin-Targeting miRNA for Synergistic Osteogenesis.

Xu Changlu C, Li Zhi Z, Kang Minjee M, Sheng Ruoyu R et al.

Demineralized bone matrix (DBM) is widely used as an alternative to autografts for repairing bone defects, but its clinical efficacy is limited by poor retention at the defect site and inadequate osteogenic capacity. Here, we developed a multifunctional carrier system aimed at improving the capacity of DBM by utilizing nanoclay-based self-assembly along with cell-derived exosome mimetics (EMs). EMs were derived from mesenchymal stem cells (MSCs) osteogenically induced in spheroids and were functionalized with bisphosphonates (BP) to assemble a stable gel network with laponite nanoclays via BP-nanoclay edge interactions. The resulting self-assembled nanoclay gel exhibited excellent injectability, moldability, and self-healing properties, even when loaded with a high concentration of DBM, and supported MSC osteogenic differentiation. We further enhanced the potency of DBM-mediated osteogenesis and bone morphogenetic protein (BMP) signaling in the nanoclay gel by incorporating BP-functionalized EMs (EM-BPs) loaded with miR-200c that can target BMP antagonist noggin. Lastly, we validated the bone regeneration efficacy of DBM-loaded nanoclay gels in comparison to commercially available DBM putties using a mouse calvarial defect model. This approach presents a versatile nanoclay gel carrier platform that overcomes the limitations of current DBM formulations and provides a promising strategy for improved bone repair.

PMID 42466084
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PubMedPhysiological research2026-07-17

Effects and Mechanisms of Action of Acupuncture on Bone and Lipid Metabolism in a Rat Model of Postmenopausal Osteoporosis.

Zhang S-N SN, Zhang C-C CC, Jiang L-H LH, Ouyang G G

This study investigated the effects of acupuncture on bone and lipid metabolism in a rat model of postmenopausal osteoporosis (PMOP). Thirty-two female Sprague-Dawley rats were randomly assigned to four groups: blank control, sham-operated, model (ovariectomy), and acupuncture treatment (ovariectomy plus acupuncture). Following treatment, bone mineral density (BMD), bone tissue morphological changes with quantitative histomorphometry, serum bone metabolism markers, estradiol (E2) levels at multiple time points, body mass index (BMI), blood lipid indicators, inflammatory factors, and gut microbiota composition were measured in each group. Acupuncture increased femoral BMD after adjusting for femoral shaft thickness (P<0.05) and improved trabecular bone structure, with significant rises in trabecular number, thickness, and bone volume fraction (P<0.05). Serum osteoprotegerin levels increased and osteoclast markers decreased. Serial E2 measurements showed progressive restoration from week 4. Acupuncture reduced BMI (P<0.05), with BMI changes negatively correlating with BMD improvements (r=-0.68, P<0.01). Lipid metabolism and inflammatory markers were significantly improved (P<0.05). Gut microbiota analysis indicated increased abundance of Lactobacillus and Bifidobacterium and decreased pathogenic bacteria (P<0.05). Liquid chromatography-mass spectrometry suggested acupuncture may promote osteogenic differentiation via upregulation of the cAMP-PKA-CREB pathway. Overall, acupuncture effectively enhances bone and lipid metabolism in PMOP rats through hormonal regulation, metabolic modulation, and gut microbiota optimization. Key words Acupuncture " Postmenopausal osteoporosis " Bone metabolism " Lipid metabolism " Estradiol " Gut microbiota " cAMP-PKA-CREB pathway.

PMID 42466703
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PubMedMedical oncology (Northwood, London, England)2026-07-17

Formulation development and preliminary biological evaluation of a menthol modified thermoresponsive tamoxifen sol-gel.

Faheem Saleha S, Hameed Huma H, Al-Hussain Sami A SA, Irfan Ali A et al.

Localized drug delivery strategies offer potential advantages in improving therapeutic concentration at tumor sites while minimizing systemic exposure. In this study, a thermoresponsive poloxamer based sol-gel system incorporating tamoxifen citrate with L-menthol was developed and characterized for potential intratumoral application. The formulation was prepared using the cold method and optimized through response surface methodology\. The optimized system exhibited rapid sol-gel transition at 38.5 °C with gelation time around 37s, acceptable syringeability, pH compatibility with mildly acidic tumor conditions, and uniform drug content (93-96%) with high encapsulation efficiency (88-93%). In vitro release studies demonstrated sustained tamoxifen release over 48 h, best described by the Korsmeyer-Peppas model (n = 0.366), indicating diffusion-controlled release. Physicochemical analyses (FTIR, DSC, XRD, SEM) confirmed drug excipient compatibility and partial amorphization within the polymeric matrix. Molecular docking provided preliminary insight into potential interactions with breast cancer associated proteins. In vitro cytotoxicity in MCF-7 cells showed reduced IC₅₀ values for the menthol containing formulation compared to tamoxifen alone. Acute toxicity evaluation in mice indicated acceptable short-term tolerability. Overall, this system represents a promising localized delivery platform warranting further mechanistic and in vivo efficacy investigations.

PMID 42467342
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PubMedInternational journal of biological macromolecules2026-07-17

The role of intrinsic protein in the structure and gelation of citrus high methoxyl pectin.

Chen Jia-Wen JW, Wang Jin-Mei JM, Liao Jin-Song JS, Qi Jun-Ru JR

The functional properties of pectin are closely related to its molecular structure. In addition to the carbohydrate backbone, non-carbohydrate components such as intrinsic protein also play a significant role in influencing pectin properties both directly and indirectly. In this study, pepsin and papain were used to remove protein in high methoxyl pectin (HMP) extracted from citrus, achieving protein removal rates of 72.59% and 89.40%, respectively. Structural analyses from FTIR, XRD, and NMR confirmed that protein removal did not alter the fundamental functional groups of pectin. However, monosaccharide composition and atomic force microscopy (AFM) revealed that protein was linked to both the homogalacturonan (HG) and rhamnogalacturonan-I (RG-I) domains. Gel analysis showed that protein removal led to a 50°SAG reduction in gel strength at pH 2.5, whereas its impact at pH 6.0 was negligible. Additionally, the rheological characterization further demonstrated the positive role of protein in deformation stability in pectin gels.

PMID 42463085
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PubMedClinical oral implants research2026-07-17

Effect of Hyaluronic Acid on Palatal Wound Healing-A Randomized Crossover Clinical Trial.

Dahi Madeleine M, Amash Sara S, Bertl Kristina K, Beck Florian F et al.

To assess the effect of a hyaluronic acid (HyA) containing gel on patient-related outcomes (PRO) and wound healing after palatal punch-biopsy representing a free gingival graft. A punch-biopsy (6 mm diameter, 2 mm thickness) was harvested from one side of the palate at Day 0 and from the contralateral side at Day 21. Sites were randomly allocated to either 0.3% HyA containing gel (test) or sterile saline solution (control), professionally applied after harvesting and then self-applied three times/day for 7 days. Up to 21 days PRO-related questionnaires were answered and intraoral scans and photographs recorded to assess wound re-epithelialization, tissue refill, and color match. Eighteen of 25 recruited participants were analyzed. Pain perception, difficulties with eating/drinking, and taste alterations significantly decreased over time and were hardly experienced after Day 7 in both groups (p > 0.05). Participants reported significantly more often a positive experience after applying HyA compared to placebo, that is, in 8 versus 1 out of 18 cases. The residual wound area was significantly smaller in the test compared to control group at Day 7, and cases with a thicker palatal tissue showed tendency for faster re-epithelialization. Despite the potential limitations of the present study (i.e., possibility of a carryover effect, questionable blinding of the participants), repeated local application of a 0.3% HyA containing gel appears to only accelerate re-epithelialization in an open palatal wound and provide a positive experience after application, but it did not improve any PRO in such small-sized wounds compared to sterile saline application. ClinicalTrials.gov identifier: NCT05099718.

PMID 42464383
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