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estradiol + norethisterone (Estrapak 50 / Sequidot / Estrapack)

✓ Approved

Novartis AG · ESR1 · 小分子

什么是 estradiol + norethisterone？

estradiol + norethisterone 是一种小分子，由Novartis AG研发。该药已获批，用于治疗相关适应症，给药途径：Topical、Transdermal。

药物档案

商品名Estrapak 50, Sequidot, Estrapack
公司Novartis AG
药物类别小分子
分子靶点ESR1, PGR
给药途径Topical, Transdermal
状态Approved
来源： ClinicalTrials.gov, Novartis AG

作用机制

分子靶点

estradiol + norethisterone 作用于 2 个分子靶点：

ESR1estrogen receptor 1 (ER, ESR)
PGRprogesterone receptor (NR3C3, PR)
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 + norethisterone 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

PubMedFrontiers in immunology2026-08-04

Priming of human monocytes by β-glucan and obesity-associated factors: modifications to global DNA methylation, gene expression, phenotype and function.

Topham Ben J BJ, Hock Barry D BD, Wiggins George A R GAR, Ashby Louisa V LV et al.

Monocytes play a critical role in regulating immune response to exogenous and endogenous challenge. Recent studies have shown exogenous stimuli can induce metabolic, epigenetic and phenotypic changes in monocytes that reprogramme or 'prime' them to react with an altered response to subsequent stimuli. Obesity is associated with immune dysfunction. However, the ability of endogenous compounds associated with obesity to prime human monocytes and thereby modulate subsequent response remains to be investigated. In this study, human monocytes from non-obese males were utilized. Monocytes exposed to primary exogenous stimuli (β-glucan), but not endogenous stimuli (oxLDL, leptin, 17β-estradiol), demonstrated an altered phenotype (increased CD11b, PD-L1 expression) in response to SK-MEL-28 melanoma cells. In contrast, monocytes primed with oxLDL, but not β-glucan, exhibited an increased rate of superoxide production in response to secondary stimulation with phorbol 12-myristate 13-acetate, and enhanced matrix metalloprotease 9 activity in response to secondary stimulation with lipopolysaccharide. Bulk RNAseq analysis of non-primed monocytes and monocytes primed with 17β-estradiol or oxLDL also showed sustained differential expression of genes related to immune function, metabolism and protein modification. Moreover, mass spectrometry analysis showed that monocytes primed with β-glucan or oxLDL exhibited sustained modifications to global DNA methylation. These results provide the first steps in understanding the functional consequences of monocyte reprogramming by obesity-related factors, and the potential pathways that govern them.

PMID 42548656
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PubMedBiomedical journal2026-08-04

Low-energy extracorporeal shock wave therapy is associated with reduced inflammation and fibrosis in an E2-induced rat model of endometriosis and remains effective under menopause-mimicking conditions.

Lan Kuo-Chung KC, Cheng Yin-Hua YH, Huang Cheng-Rung CR, Weng Pei-Ling PL et al.

Endometriosis is an estrogen-dependent inflammatory disorder marked by ectopic lesions, chronic pelvic inflammation, and frequent recurrence. Extracorporeal shock wave therapy (ESWT) is a non-invasive modality with anti-inflammatory and regenerative potential, but its efficacy under varying estrogen conditions remains unclear. Endometriosis-like lesions were induced in female rats by suturing uterine fragments to the peritoneum, followed by daily 17β-estradiol (E2) or PBS for 28 days. Sprague-Dawley rats were assigned to control, E2, E2 + ESWT (0.1 or 0.25 mJ/mm2), or ovariectomy (OVX) + ESWT groups. ESWT was applied twice weekly for three weeks. Body weight, food intake, lesion morphology, histology, and serum E2 were assessed. Inflammatory and fibrotic markers were analyzed as follows: transforming growth factor beta (TGF-β) and tumor necrosis factor-alpha (TNF-α) were evaluated by both immunohistochemistry (IHC) and quantitative real-time RT-PCR (qRT-PCR), whereas interleukin (IL)-6, nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), cyclooxygenase (COX)-2, vascular endothelial growth factor (VEGF), cytokeratin (CK)-18, superoxide dismutase (SOD), inducible nitric oxide synthase (iNOS), and hypoxia-inducible factor-1 alpha (HIF-1α) were assessed by qRT-PCR only. E2 reduced body weight and food intake and induced cystic peritoneal lesions with upregulated fibrotic and inflammatory markers. ESWT at both energy levels significantly reduced lesion size, cystic formation, the number of endometrial glands (hematoxylin-eosin, H&E staining), fibrosis area ratio (Masson trichrome staining), and expression of fibrosis-, inflammation- oxidative stress-, and hypoxia-related genes and proteins regardless of ovarian status. OVX combined with ESWT produced comparable or slightly enhanced reductions in several markers. ESWT did not alter systemic E2 levels, whereas OVX resulted in reduced serum estrogen levels. Low-energy ESWT attenuated E2-induced endometriotic lesions, accompanied by reductions in proliferation, inflammation, and fibrosis, without altering circulating estrogen levels. These effects were also observed under menopause-mimicking conditions with controlled estrogen exposure. These findings suggest that ESWT may serve as a complementary non-hormonal adjunctive approach and may provide a useful experimental framework for future mechanistic and preclinical studies.

PMID 42546843
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PubMedBiosensors & bioelectronics2026-08-03

Graphdiyne-PtCu hollow nanocubes-cooperated dual-engine hairpin assembler toward amplifiable electrochemical biosensing.

Zhou Yifu Y, Liu Si S, Song Honglin H, Chen Zhixuan Z et al.

Developing graphdiyne-PtCu hollow nanocubes (GPtCu)-cooperated dual-engine hairpin assembler (dEHA) for amplifying electrochemical response of 17β-estradiol (E2) might be intriguing and desirable, particularly in the area of environmental analysis. Herein, we propose the first design of GPtCu-coupled dEHA amplification for constructing electrochemical biosensor sensitively responsive to E2. The modification of GPtCu and AuNPs in the electrode surface aims to enhance electronic conductivity, increase electroactive surface area, and provide more accessible Au-S binding sites for immobilizing electroactive ferrocene (Fc)-labeled signaling hairpin probe. An E2-recognizable strand encoding specific aptamer sequence and a translator strand are designed to form a duplex strand for interpreting the presence and variation of E2. As such, the progressive dEHA operation is executed via consecutive hybridization and strand migration reaction among three functional hairpins. During the process, the translating and recognizing modules are rationally displaced and functioned as two uninterrupted engines to implement repetitive recycling events through cooperatively catalyzing the transient depletion of reactive intermediates, thereby achieving rapid transduction and efficient amplification. As a result, numerous Fc tags in the final duplex products are oriented close in the electrode sensing interface to output linearly E2-dependent current signal, featuring superior reaction kinetics, high specificity and sensitivity. Thus, our strategy would suggest a reliable analytical tool and a universal biosensing paradigm for monitoring diverse trace-level environmental endocrine disruptors (EEDs).

PMID 42546380
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PubMedEuropean journal of applied physiology2026-08-03

Different mucosal immunity and hormonal responses to routine physical training in the follicular and the luteal phases of elite female athletes.

Wang Chung-Kai CK, He Cheng-Shiun CS, Chiang Ming-Ru MR, Li Pei-Ying PY et al.

Fluctuations in sex hormones across the menstrual cycle may influence immune regulation in female athletes; however, evidence regarding phase-specific mucosal immune responses to routine physical training remains limited. This study compared acute changes in salivary immune and hormonal markers induced by routine team-based physical training between the follicular and luteal phases in elite female athletes. Twenty-five athletes completed comparable routine physical training sessions during both menstrual phases. Unstimulated whole saliva was collected before and after each routine physical training session during the mid-follicular (day 10.3 ± 2.7) and mid-luteal (day 23.6 ± 3.7) phases to determine the concentrations of secretory immunoglobulin A (SIgA), lactoferrin (LF), α-amylase (sAA), nitric oxide (NO), estradiol, progesterone, testosterone, and cortisol. Data were analyzed using two-way repeated-measures ANOVA with Bonferroni adjustment. Progesterone and LF concentrations were significantly higher during the luteal phase, whereas the testosterone-to-cortisol ratio at rest was greater during the follicular phase. Following training, SIgA, LF, and cortisol concentrations decreased, while sAA increased, with no significant change observed in NO. These responses were comparable between menstrual phases. Routine physical training acutely altered salivary immune and stress-related markers in elite female athletes irrespective of menstrual phase. Higher LF concentrations during the luteal phase suggest a possible phase-related difference in innate mucosal immune status. The physiological significance of the higher follicular-phase resting T/C ratio requires further investigation.

PMID 42545475
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PubMedToxicology and applied pharmacology2026-08-03

Integrated approaches to testing and assessment (IATA) for the estrogenic response of 14 commonly used chemicals in consumer products.

Lee Hyun Jun HJ, Ortiz Darlene Mae DM, Park Kwangsik K

Human exposure to functional ingredients in consumer products is chronic and often involves complex mixtures; however, integrated assessments of their endocrine-related effects remain limited. This study utilized an adverse outcome pathway (AOP)-informed Integrated Approaches to Testing and Assessment (IATA) framework to evaluate the estrogenic activity of fourteen representative ingredients. A tiered strategy combining in silico receptor-binding predictions, estrogen receptor alpha (ERα) transactivation assays (OECD TG 455), steroidogenesis assays in H295R cells (OECD TG 456), and mixture modeling was implemented. In silico analyses indicated moderate ERα binding affinity, with limited agreement across platforms. Notably, thirteen of fourteen chemicals met OECD positivity criteria in the ERα transactivation assay based on positive control (PC)10 values. Benzisothiazolinone, 2-butyl-1,2-benzothiazol-3-one, propyl paraben, and benzyl benzoate were selected for steroidogenesis assessment due to strong ERα responses. Among these, benzisothiazolinone and propyl paraben increased estradiol production by 5.7- and 5.2-fold, respectively, and significantly upregulated STAR, CYP11A1, and CYP17A1, suggesting stimulation of endogenous hormone synthesis. Whereas the others primarily affected receptor activity without altering steroidogenesis. Binary mixtures representing commonly co-occurring ingredients exhibited predominantly additive effects, as indicated by model deviation ratios. Integration of molecular initiating events, key events, and functional endpoints enabled mechanistic prioritization within the IATA framework. These findings demonstrate that combining standardized in vitro assays with computational approaches provides deeper mechanistic insight than single-endpoint strategies and supports cumulative risk assessment of consumer product ingredients.

PMID 42543081
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PubMedInternational journal of hyperthermia : the official journal of European Society for Hyperthermic Oncology, North American Hyperthermia Group2026-08-03

Comparative study on the effects of high-intensity focused ultrasound (HIFU) and laparoscopic myomectomy on ovarian function and endometrial receptivity in patients with uterine fibroids.

Huang Rui R, Wang Yangyang Y, Song Yuying Y, Duan Xiangling X et al.

To compare the effects of high-intensity focused ultrasound (HIFU) ablation and laparoscopic myomectomy on ovarian function and endometrial receptivity in patients with uterine fibroids. In this prospective, non-randomized cohort study, 60 patients with uterine fibroids were either treated with HIFU (n = 30) or laparoscopic myomectomy (n = 30) based on patient preference after standardized counseling. Ovarian function and endometrial receptivity were evaluated preoperatively and at 1, 3, and 6 months post‑treatment. Ovarian reserve was assessed using anti‑Müllerian hormone (AMH), sex hormone levels of luteinizing hormone (LH), follicle‑stimulating hormone (FSH), estradiol (E2), and antral follicle count (AFC). Endometrial receptivity was evaluated using endometrial thickness and vascular indices, including endometrial artery resistance index (RI), pulsatility index (PI), and the systolic/diastolic velocity ratio (S/D). Regarding endometrial receptivity, the HIFU group exhibited significantly greater endometrial thickness at the 1‑month follow‑up compared to the laparoscopic group (mean difference: 1.5 mm, 95% CI: 0.6 to 2.4 mm; Cohen's d = 0.72, p < 0.05). Both groups showed a reduction in PI after treatment, though the change was not statistically significant. RI and S/D ratios were comparable between the two groups at any time point (p > 0.05). Both HIFU and laparoscopic myomectomy preserved ovarian function in patients with uterine fibroids. HIFU was associated with faster short-term endometrial recovery at 1 month post-treatment, but no differences in ovarian function or other receptivity markers were observed between the two groups of patients. Randomized trials with pregnancy outcomes are needed before clinical recommendations can be made.

PMID 42544600
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