北京若生智能科技有限公司
Drug Database
ES

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

PubMedCells2026-10-26

Selective Estradiol Sensitivity in 12Z Human Endometriotic Epithelial Cell Line.

Banerjee Shohini S, Chopra Esha E, Smith Ian M IM, Stroka Kimberly M KM

Estradiol (E2) is a potent estrogen molecule that plays a crucial role in regulating numerous healthy and pathophysiological processes. To model estrogen-dependent cellular activities in vitro in a physiologically meaningful way, cells chosen for experimentation should exhibit sensitivity to E2. The 12Z human endometriotic epithelial cell line is gaining attention as a model for estrogen-dependent conditions, but its functional responsiveness to E2 has not been well characterized. For the passage range in the following study, we found that E2 does not statistically significantly influence 12Z proliferation, wound closure, or single-cell migration. However, 12Zs were selectively responsive to E2 in 3D migration models where the cells were physically confined. Upregulating ESR1, the primary mediator of estrogenic action, in the 12Zs did not enhance their functional E2 sensitivity. These results highlight the importance of verifying hormone responsiveness when using 12Z cells to model estrogen-dependent processes and conditions.

PMID 42929847
阅读全文 →
PubMedInternational journal of fertility & sterility2026-10-26

Treatment Approach to Disseminated Peritoneal Leiomyomatosis in A Patient Desiring Future Fertility: A Case Report.

Neal Samantha E SE, Ryles Hannah T HT, Koomson Christabel C, Madueke-Laveaux Obianuju Sandra OS et al.

Disseminated peritoneal leiomyomatosis (DPL) is a rare condition in which fibroids diffusely grow in extrauterine locations. Given its low prevalence, the literature is limited, making evidence-based treatment particularly challenging, especially in premenopausal patients. This case report describes a 34-year-old nulligravid woman with a history of two prior myomectomies who presented with upper abdominal bulk symptoms. Abdominal and pelvic magnetic resonance imaging (MRI) revealed multiple mesenteric and omental masses concerning for recurrent DPL. She underwent exploratory laparotomy with removal of 13 abdominal fibroids ranging from 2 to 12 cm. Postoperatively, her symptoms improved, and she was treated with a gonadotropin-releasing hormone (GnRH) analog (relugolix/estradiol/ norethindrone acetate) with a favorable response and sustained remission on follow up. Our case report demonstrates the efficacy of a novel medical therapy and our scoping review highlights the importance of aggressive surgical management followed by medical therapy for the treatment of DPL in patients with future fertility desires.

PMID 42929007
阅读全文 →
PubMedAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2026-10-26

Plasma Membrane Lipid Asymmetry Dynamically Regulates Passive Diffusion.

Ping Jieming J, Wang Wenliang W, Xu Jinnuo J, Yang Mengyun M et al.

Plasma membrane (PM) phospholipid asymmetry is a fundamental feature of eukaryotic cells that regulates signaling, trafficking, and cell fate. Whether it also controls passive diffusion across the PM remains unknown. Here, we show that phospholipid asymmetry is a critical determinant of PM permeability to hydrophobic molecules. Using genetic and biochemical approaches, we demonstrate that disruption of lipid asymmetry by the Ca2 +-activated scramblase TMEM16F or apoptotic scramblase XKR8 profoundly alters the permeation and intracellular accumulation of diverse hydrophobic compounds, including widely used fluorescent probes, while preserving the barrier to membrane-impermeable molecules. Lipid scrambling is sufficient to remodel membrane permeability to lipophilic molecules, alter membrane biophysical properties, and differentially affect their intracellular accumulation, suggesting selective regulation of passive diffusion rather than nonspecific membrane leakage. Physiological lipid scrambling during T cell activation was also accompanied by altered membrane permeability. Moreover, lipid asymmetry regulates the cellular entry of doxorubicin, 17β-estradiol, and all-trans retinoic acid. Together, our findings identify PM lipid asymmetry as a previously unrecognized regulator of membrane permeability and establish a link between membrane organization and molecular transport.

PMID 42928505
阅读全文 →
PubMedInternational journal of psychophysiology : official journal of the International Organization of Psychophysiology2026-10-25

A behavioral and electrophysiological study on the influence of menstrual cycle, estradiol and progesterone on the social approach-avoidance behavior tendencies of women.

Li Danyang D, Li Xue X, Yuan Yuan Y, Zhu Hao H et al.

It remains unclear whether women's social approach-avoidance behaviors toward different facial expressions are influenced by their menstrual cycles, estradiol and progesterone levels, or what the underlying electrophysiological mechanisms might be. This study collected data on the levels of estradiol and progesterone, social approach-avoidance behavior and electroencephalogram (EEG) recordings from 27 women with natural menstrual cycles during three phases- early follicular phase, late follicular phase, and mid-luteal phase. The results showed that women in the late follicular phase exhibited a faster approach tendency and a smaller LPP amplitude to happy faces compared to the early follicular phase; women in the mid-luteal phase exhibited a faster approach tendency and a smaller LPP amplitude to fearful faces compared to the late follicular phase. Estradiol levels is positively correlated with the efficiency of approach behavior toward happy faces, while progesterone levels is positively correlated with the efficiency of approach behavior toward fearful faces. The results show that women's social approach-avoidance behaviors are specifically regulated by the menstrual cycle, estradiol and progesterone, and exhibit higher cognitive processing efficiency in the late positive potential (LPP) of the brain. These findings are manifestations in social interactions of the characteristics of women's interest pursuit and self-restraint under the influence of different sex hormones formed during evolution, updating established hormone-behavior links in social emotional contexts.

PMID 42926021
阅读全文 →
PubMedJournal of cellular physiology2026-10-25

17β-Estradiol Inhibits Endoplasmic Reticulum Stress and Alleviates Pyroptosis via the NLRP3/Caspase-1/GSDMD Axis in Sheep Theca Cells.

Yang Yahua Y, Yuan Yue Y, Ding Xiaona X, Li Pinshen P et al.

17β-Estradiol (E2) is an important reproductive hormone and exhibits anti-inflammatory properties. To explore the mechanism of estrogen in alleviating inflammation, we used theca cells (TCs) as a model cell type in this study. Lipopolysaccharide (LPS) was used to induce a cell injury model. Protein localization and expression in TCs were assessed by immunofluorescence and Western blotting, organelle morphology was examined by transmission electron microscopy; and target gene expression was analyzed by qRT-PCR. The results showed that E2 significantly enhanced the viability of TCs pretreated with LPS (p < 0.05). E2 treatment alleviated endoplasmic reticulum (ER) and mitochondrial damage. E2 significantly decreased the expression of CHOP and P-PERK/PERK, P-IRE1α/IRE1α and ATF6 (p < 0.05). E2 inhibited pyroptosis via significantly downregulating the expression of GSDMD, NLRP3 and Cleaved caspase-1 (p < 0.05). Following the inhibition of ER stress by 4-PBA, the expression levels of CHOP and GSDMD were significantly reduced in the E2 + LPS + 4-PBA group (p < 0.05). In conclusion, E2 relieved LPS-induced ER stress and pyroptosis in sheep TCs via the CHOP/NLRP3/Caspase-1/GSDMD pathway. This finding provides new insights into the role of estrogen in female reproductive health and suggests a potential therapeutic strategy for improving ovarian immune and reproductive function through the modulation of hormonal homeostasis.

PMID 42927617
阅读全文 →
PubMedJournal of animal science2026-10-25

17β-Estradiol Promotes Goat Granulosa Cell Proliferation via the ERα/NO/Wnt/β-Catenin Signaling Axis.

Tang Yaju Y, Yi Wanting W, Sun Yuting Y, Tang Di D et al.

Ovarian granulosa cells (GCs) are central to follicular development in goats, and their proliferation is tightly regulated by estrogen, yet the downstream signaling cascade mediating this effect in ruminants remains undefined. This study aimed to investigate whether estrogen regulates goat ovarian GC proliferation through the nitric oxide (NO) signaling pathway and to further elucidate the molecular mechanisms by which NO modulates GC proliferation. Primary goat GCs were treated with 17β-estradiol (17β-E2), the NO donor sodium nitroprusside (SNP), the NOS inhibitor NG-monomethyl-L-arginine (L-NMMA), the Wnt inhibitor FH535, and the Wnt agonist SKL2001. Cell viability, proliferation, and protein expression were assessed by CCK‑8, EdU, and Western blotting. 17β-E2 at concentrations of 1, 2, and 10 μg/mL all promoted GC viability (P < 0.05), with maximal effect at 1 μg/mL (P < 0.01), and simultaneously upregulated inducible NOS (iNOS), endothelial NOS (eNOS), and neuronal NOS (nNOS) protein expression via estrogen receptor α (ERα). The NO donor SNP enhanced GC proliferation, whereas the NOS inhibitor L‑NMMA suppressed it; co‑treatment with SNP partially rescued the L‑NMMA‑induced inhibition. Mechanistically, SNP increased β‑catenin and proliferating cell nuclear antigen (PCNA) protein levels, an effect reversed by FH535, whereas L‑NMMA‑induced NO depletion reduced their expression, which was restored by SKL2001, positioning NO upstream of the Wnt/β‑catenin pathway. Collectively, these findings establish that 17β-E2 promotes goat GC proliferation through a signaling cascade involving ERα, NOS, NO, and the Wnt/β‑catenin pathway, providing the functional evidence for this axis in a ruminant model and offering a mechanistic framework for understanding ovarian follicular dynamics with implications for improving reproductive efficiency in goats.

PMID 42921890
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多estradiol + norethisterone