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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

PubMedMaturitas2026-06-13

Neurokinin pathway botanical antagonist for menopausal vasomotor symptoms: A randomized, double-blind, placebo-controlled study.

Lederman Samuel S, Minkin Mary Jane MJ, Doyle Audra Lisa AL, Rubio Jevaneeh J et al.

Vasomotor symptoms (VMS) are a prevalent and disruptive manifestation of menopause, and many women prefer nonhormonal, nonpharmacologic treatment options. This study evaluated the efficacy of a patented multi-ingredient botanical neurokinin inhibitor (BNI) on VMS and other patient-reported outcome measures. A randomized, double-blind, placebo-controlled trial was performed in menopausal women with 5 or more moderate to severe hot flashes daily. Participants were enrolled from community medical practices in the United States and randomized to BNI or placebo for 12 weeks. BNI is a novel formulation of plant extracts that attenuates neurokinin receptor signaling in vivo. Primary endpoints were changes in daily VMS frequency and score on the Hot Flash Related Daily Interference Scale (HFRDIS). Secondary endpoints included changes in Menopause-Specific Quality of Life (MENQOL) and Pittsburgh Sleep Quality Index (PSQI). Serum estrogen and liver function were assessed in a subgroup of patients. Of 74 randomized participants, 68 completed the trial (BNI, n = 32; placebo, n = 36). BNI supplementation reduced VMS frequency by 2.2 hot flashes per day more than placebo (p = 0.003), corresponding to a 47.7% relative decrease. HFRDIS was improved in the BNI group (p = 0.037), with significant reduction on all subscales. No significant differences were observed in global menopause symptoms (MENQOL) or sleep quality (PSQI). No changes in serum estradiol or liver function abnormalities were detected. BNI was well tolerated, with no difference in adverse events between groups. A combination of botanically derived neurokinin inhibitors produces significant and sustained relief of vasomotor symptoms in menopausal women. gov registration: NCT05813067.

PMID 42284819
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PubMedBiomedicine & pharmacotherapy = Biomedecine & pharmacotherapie2026-06-13

Steryl glucosides as a novel chemosensitizer: Enhancing doxorubicin response in estrogen receptor-positive breast cancer.

Cavalcanti-Neto Marinaldo Pacífico MP, Brauer Verônica Soares VS, Rella Antonella A, Shamseddine Achraf A et al.

Estrogen receptor-positive (ER+) breast cancer is the most prevalent breast cancer subtype, and doxorubicin is a key systemic therapeutic drug. However, its use is limited by toxicity and mechanisms of drug resistance. Steryl glucosides are bioactive glycolipids with potential anticancer and immunomodulatory properties, but their role as chemotherapy-sensitizing agents remains undefined. Here, we investigated whether a soybean-derived steryl glucoside preparation (SG) enhances doxorubicin activity primarily in the MCF-7 ER+ breast cancer model. SG co-treatment increased doxorubicin-associated cytotoxicity and reduced cell viability of MCF-7. Dose-response matrix analysis and exploratory Bliss independence modeling identified concentration-dependent regions of greater-than-expected combined activity, supporting pharmacological potentiation but not definitive synergy. SG co-treatment also increased γ-H2AX-positive nuclei, consistent with enhanced doxorubicin-associated DNA damage signaling. Fluorescence-based extraction analysis showed increased doxorubicin-associated intracellular fluorescence in SG co-treated cells, while ABCB1 qRT-PCR revealed concentration-dependent transcriptional changes. These findings suggest altered intracellular drug exposure or transport-associated responses, although functional efflux activity was not directly assessed. In an ovariectomized, estradiol-supplemented MCF-7 xenograft model, the SG-doxorubicin group showed the lowest mean tumor-growth trajectory, reduced cumulative tumor burden, lower terminal tumor weight, reduced Ki-67 staining, and increased tumor necrosis. However, the longitudinal tumor-volume analysis did not establish unequivocal superiority over doxorubicin monotherapy. Exploratory T47D data indicated weaker responsiveness, suggesting that the effect may be model-dependent. This study provides proof-of-concept evidence that SG can enhance doxorubicin-associated antitumor activity mainly in the MCF-7 model. Further studies are required to define functional transport mechanisms, model generalizability, toxicity, and formal dose-sparing potential. This study provides proof-of-concept evidence that a soybean-derived steryl glucoside preparation can enhance doxorubicin-associated cytotoxicity, DNA damage signaling, and antitumor activity primarily in the MCF-7 estrogen receptor-positive breast cancer model. The findings support further investigation of SG as a candidate chemotherapy-sensitizing adjuvant, while highlighting the need for functional transport assays, broader model validation, comprehensive toxicity assessment, and formal dose-sparing studies before translational conclusions can be drawn.

PMID 42284886
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PubMedResearch square2026-06-12

Short-term HPV detection dynamics across hormonal contraceptive methods in adolescent girls and young women: a secondary analysis of a randomized trial in South Africa.

Tanko Ramla F RF, Taku Ongeziwe O, Mbulawa Zizipho Z A ZZA, Phohlo Keletso K et al.

Background Human papillomavirus (HPV) is highly prevalent in adolescent girls and young women (AGYW) in sub-Saharan Africa. We evaluated short-term differences in HPV prevalence and early detection dynamics across hormonal contraceptive methods in AGYW. Methods Ninety-eight AGYW (15-19 years) were randomized to receive norethisterone enanthate (Net-EN), combined oral contraceptive pills (COCPs), or a combined contraceptive vaginal ring (CCVR). Cervical samples were collected at baseline and 16-weeks for HPV genotyping. Results Baseline HPV prevalence was high (93/98; 94.9%) and remained high at 16-weeks (87/97; 89.5%), with no significant differences between contraceptive methods. Longitudinal analyses (n = 87 paired samples) showed no statistically significant differences in HPV acquisition, persistence, or clearance. Conclusions No significant differences were observed in HPV outcomes between hormonal contraceptive methods over 16-weeks. Findings should be interpreted as exploratory given the small sample size and short follow-up.

PMID 42281989
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PubMedJournal of clinical medicine2026-06-12

Clinical and Hormonal Determinants of Propofol Requirement During Oocyte Pick-Up: A Prospective Observational Study.

Gürsoy Çirkinoğlu Gözde G, Kuvvet Yoldaş Tuba T, Ateşalp Aylin A, Şahinkaya Halide Hande HH et al.

Objectives: Oocyte pick-up (OPU) is commonly performed under propofol-based sedation during in vitro fertilization (IVF). However, considerable interindividual variability in propofol requirement has been observed. Controlled ovarian hyperstimulation results in supraphysiological levels of ovarian steroid hormones, which may influence anesthetic sensitivity. This study aimed to evaluate the relationship between preprocedural serum estradiol and progesterone levels and propofol requirement during OPU performed under bispectral index (BIS)-guided sedation. Methods: In this prospective observational study, 96 women undergoing OPU were included. Serum estradiol and progesterone levels measured on the day of the procedure were recorded. Sedation was performed using a standardized protocol with midazolam, fentanyl, and propofol titrated to maintain BIS values between 40 and 60. Propofol consumption was normalized to body weight (mg/kg) and procedure duration (μg/kg/min). Correlation analyses and multivariable linear regression models were used to evaluate associations. Results: Mean propofol consumption was 157.3 ± 53.1 mg (2.41 ± 0.83 mg/kg), corresponding to an infusion rate of 125.7 ± 69.6 μg/kg/min. In multivariable analysis, estradiol levels were independently associated with propofol requirement (β = 0.238, p = 0.014), whereas progesterone levels were not significantly associated with anesthetic dosing after adjustment. BMI (β = -0.305, p = 0.002) and procedure duration (β = 0.224, p = 0.021) were also identified as independent predictors. Conclusions: Estradiol levels were associated with propofol requirement during OPU performed under BIS-guided sedation. However, given the observational design and the modest magnitude of the observed associations, these findings should be interpreted cautiously. BMI and procedure duration appeared to be more consistent predictors of propofol administration.

PMID 42279141
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PubMedBreast cancer research and treatment2026-06-12

Three-monthly gonadotropin-releasing hormone agonist for ovarian function suppression in premenopausal breast cancer: a systematic review and meta-analysis.

de Liz Caio Dabbous CD, Reis Pedro C Abrahão PCA, Blanchard-Cavagis Ellen R ER, Diniz Isabela C IC et al.

Ovarian function suppression (OFS) with gonadotropin-releasing hormone agonists (GnRHa) improves outcomes in premenopausal women with hormone receptor-positive (HR +) breast cancer (BC), most commonly using monthly administration. The potential equivalence of 3-monthly (3 M) versus monthly (1 M) schedules has been suggested but remains uncertain. We performed a systematic review and meta-analysis of interventional studies comparing 3 M and 1 M GnRHa regimens in premenopausal women with HR + BC receiving endocrine therapy. Outcomes included ovarian escape (OE), mean estradiol (E2) levels, disease-free survival (DFS), progression-free survival (PFS), and adverse events. Subgroup analyses were performed by estradiol assay type, and a sensitivity analysis restricted to RCTs. Fifteen studies comprising 4,324 patients were included, of whom 2,098 (48%) received a 3 M regimen. The pooled OE was 10% and showed no significant difference between schedules (RR 0.86; 95% CI 0.60-1.22; p = 0.39). Ultrasensitive assays yielded higher OE detection (31%) without inter-regimen differences (RR 0.90; 95% CI 0.38-2.14). Mean E2 concentrations at 12 weeks were similar (MD 1.36 pg/mL; 95% CI -3.66 to 6.38), with consistent findings in RCT-only analyses (MD -1.77 pg/mL; 95% CI -5.71 to 2.17). DFS (RR 1.02; 95% CI 0.67-1.56) and PFS (RR 0.86; 95% CI 0.72-1.04) were also comparable. No clinically relevant differences were observed in reported safety outcomes. 3 M GnRHa achieved OFS efficacy comparable to 1 M regimens, with no meaningful differences in survival or safety. The findings support 3 M GnRHa as a valid and practical alternative for OFS in appropriately selected premenopausal women with HR + BC.

PMID 42283761
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PubMedInternational journal of sports medicine2026-06-12

Trans-inclusion in sports: history, scientific evidence and future directions.

Krishna Ananya M AM, Bauer Carlie C, Way Kimberley L KL, Jones-Freeman Bernadette B et al.

Sport is traditionally organised into male and female categories, but the increasing visibility of transgender athletes has prompted sporting organisations worldwide to develop relevant eligibility regulations. These policies range from hormone thresholds and open categories to puberty-based exclusions and blanket bans yet are rarely based on direct scientific evidence. This review aims to examine the historical evolution of transgender inclusion in sport, map current international regulations and evaluate the evidence underpinning these approaches. First, we outline the temporal evolution of eligibility frameworks. We then review the roles of sex hormones in performance-relevant systems and assess how these mechanisms may result in physiological changes in transgender athletes receiving testosterone or estradiol-based gender affirming hormone therapy (GAHT). Studies demonstrate that GAHT induces physiological changes that may translate to measures of physical fitness, but are limited by cross-sectional designs, small cohorts, short follow-up periods, heterogeneous treatment regimens and outcome measures that are rarely sport specific. Therefore, the certainty of this evidence remains low, and existing data are insufficient to support uniform policies across all disciplines. We therefore recommend that fairness and safety considerations should not be resolved through biology alone and propose a structured, sport-specific framework for policy development and revision under uncertainty.

PMID 42276143
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