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estradiol (Vagifem)

✓ Approved

Novo Nordisk A/S · ESR1 · 小分子

什么是 estradiol?

estradiol 是一种小分子,由Novo Nordisk A/S研发。该药已获批,用于治疗相关适应症,给药途径:Intravaginal。

药物档案

商品名Vagifem
公司Novo Nordisk A/S
药物类别小分子
分子靶点ESR1
给药途径Intravaginal
状态Approved

作用机制

分子靶点

estradiol 作用于 1 个分子靶点:

ESR1estrogen receptor 1 (ER, ESR)
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 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
Reproductive system and breast disordersAtrophic vulvovaginitis✓ Approved

相关研究文献

PubMedEBioMedicine2026-08-04

Accurate prediction of gain- and loss-of-function missense variants in GABAA receptors.

Boßelmann Christian M CM, Ortiz Sebastian S, Dahl Rebekka R, Liao Vivian W Y VWY et al.

Missense variants in genes encoding GABAA receptors are involved in the pathophysiology of common and rare epilepsies. Variant effects on channel biophysical function are associated with key clinical characteristics and treatment response. Predicting variant effects is therefore key to improving care for individuals with GABAA receptor-related disorders. We collected data from 505 affected individuals with 272 (likely) pathogenic GABAA receptor missense variants (GABRA1, GABRB2, GABRB3, GABRG2). All variants were evaluated with in-vitro electrophysiology. Variants were annotated with features based on sequence, structure, and phenotype. Model performance was estimated using cross-validation and external validation on a further 197 individuals with 138 (likely) pathogenic variants. Our models enable highly accurate prediction of missense variant effects in GABAA (AU-ROC 0.862-0.946), outperforming state-of-the-art models (AU-ROC 0.495-0.756) and clinical decision-making. Model scores correlated with GABA sensitivity and were consistent with expert-based structure-function hypotheses, supporting plausibility. Predictions on population variants were similar to functionally neutral variants, while cases from ClinVar were similar to GOF/LOF variants. Our model may provide additional evidence for 5-25% of variants in ClinVar. Lastly, we show that we can predict likely clinical characteristics from variant information alone (median Lin similarity 0.754 IQR 0.161). We demonstrate accurate missense variant effect prediction in GABAA receptors with rigorous validation across a large dataset of functionally tested variants. These predictions may facilitate timely diagnosis and precision treatment of individuals with GABAA receptor-related disorders, pending prospective clinical validation. A web interface, precomputed scores, and calibrated score thresholds for all possible variants are openly available. Else Kröner-Fresenius-Stiftung; German Federal Ministry of Research, Technology and Space; German Research Foundation; Medical Faculty University of Tübingen; Lundbeck Foundation; Novo Nordisk Foundation.

PMID 42546502
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PubMedThe journal of obstetrics and gynaecology research2026-08-04

Diagnostic Performance of HPV Testing Using Self-Collected Urine and Vaginal Samples for Detecting Cervical Precancer or Worse: A Meta-Analysis.

Hsiao Ke-Yu KY, Lin Hsiu-Ling HL, Chen Cheng-Chieh CC

Self-collection models are regarded as a potential strategy to facilitate HPV testing for cervical cancer screening. HPV testing using urine specimens offers certain advantages, including its noninvasiveness. This characteristic has the potential to eliminate discomfort. Concerns regarding the accuracy of this method persist. Thus, the present meta-analysis aims to verify the accuracy of HPV testing using self-collected urine samples and vaginal samples. A literature search was conducted in the PubMed, Embase, and Cochrane Library databases to identify eligible studies. The inclusion criteria were as follows: studies that evaluated the diagnostic accuracy of HPV testing for high-grade squamous intraepithelial lesion or worse (HSIL+) with self-collected urine samples and vaginal samples. Additionally, studies that provided sufficient data for conducting a meta-analysis were assessed. The meta-analysis was conducted using a bivariate random-effects model. A total of 11 articles were identified. These articles included 3534 self-collected urine specimens and 3523 vaginal specimens. The meta-analysis yielded a pooled sensitivity of 81% for HPV testing with self-collected urine specimens for HSIL+. A further meta-analysis yielded a pooled sensitivity of 88.6% for HPV testing with self-collected vaginal specimens detecting HSIL+. For specimen type, pooled sensitivity was 86.6% in the subgroup of papers using first void urine (FVU) via a standardized device to evaluate HPV testing. Our meta-analysis suggests that HPV testing using both self-collected urine and vaginal specimens achieves high sensitivity for detecting HSIL+. Another potential benefit of HPV testing employing FVU collected with a standardized device is the capacity for heightened sensitivity.

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PubMedClinical research in cardiology : official journal of the German Cardiac Society2026-08-04

Performance of a sirolimus-eluting balloon with phospholipid nanocarriers in the treatment of long de novo coronary artery disease: the prospective GINGER trial.

Ielasi Alfonso A, Gitto Mauro M, Galli Stefano S, Sangiorgi Giuseppe Massimo GM et al.

Sirolimus-coated balloons (SCB) may offer improved antiproliferative efficacy over paclitaxel-coated balloons; however, data regarding their performance in de novo coronary lesions are limited. The GINGER study aimed to evaluate the angiographic efficacy and clinical safety of a SCB (Magic Touch®) in the treatment of long (≥ 25 mm) de novo coronary artery lesions. This observational, prospective, multicenter, single-arm cohort study enrolled patients with at least one long de novo lesion treated with SCB. Co-primary endpoints were late lumen loss (LLL) and net lumen gain at 9 months. Secondary endpoints included: procedural success, periprocedural myocardial infarction, binary restenosis and a device-oriented composite endpoint (DOCE), defined as the composite of cardiac death, target vessel myocardial infarction (TV-MI) and clinically-driven target lesion revascularization (CD-TLR). The study was registered at ClinicalTrials.gov (NCT05471245). A total of 104 patients was enrolled at 8 centers. Mean lesion length was 28.9 ± 16.0 mm and reference vessel diameter was 2.3 ± 0.6 mm. Procedural success was achieved in all cases. At 9-month angiographic follow-up, LLL was 0.28 ± 0.68 mm, net lumen gain 0.62 ± 0.63 mm, and binary restenosis was observed in 33.3% of lesions. Clinical events at 12-month included DOCE in 6.7% of patients, cardiac death in 1.0%, TV-MI in 4.8% and CD-TLR in 3.8%. No lesion thrombosis was reported. In a real-world cohort of patients with long de novo coronary lesions, the Magic Touch SCB was associated with a LLL of 0.28 mm, which should be interpreted in light of the high complexity of treated lesions. Future randomized trials are warranted to evaluate its clinical efficacy in comparison with new-generation drug-eluting stents.

PMID 42550208
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PubMedLung cancer (Amsterdam, Netherlands)2026-08-04

BRAF fusions define therapeutic vulnerability and tyrosine kinase inhibitor resistance in non-small cell lung cancer.

Wang Kai K, Yi Chao C, Ning Xiong X, Xiong Dalin D et al.

BRAF fusions are rare but clinically relevant oncogenic events in non-small cell lung cancer (NSCLC), yet their molecular characteristics and optimal management remain unclear. We retrospectively analyzed 97 patients with NSCLC harboring kinase domain-retaining BRAF fusions, stratified into de novo (N = 43) and acquired (N = 54) groups. Clinical and genomic features were compared across subgroups and comparator driver cohorts. We identified 104 BRAF fusions involving 53 unique partner genes, 29 of which were novel. Common partners included AGK (12.5%), IGR (11.5%), ZC3HAV1 (7.7%), TRIM24 (5.8%), and MKRN1 (5.8%). IGR and DTNB were more commonly observed in de novo cases, whereas AGK-BRAF fusions predominated in acquired cases. Among de novo cases, 65.1% lacked co-occurring drivers. ZNF703 mutations and NRF2 pathway alterations were recurrently enriched in BRAF fusion-only tumors, while CTNNB1 and NKX2-1 mutations were enriched versus ALK-rearranged cases. BRAF fusions co-occurring with other drivers showed enrichment of KMT2C and RTK-RAS pathway mutations, with TP53 mutations enriched compared to RET-rearranged tumors. One patient with TRIM24-BRAF and EGFR exon 19 deletion derived clinical benefit from dual MEK and EGFR inhibition. Acquired BRAF fusions were frequently detected after EGFR-TKI therapy, representing the predominant alteration in 63.0% of cases. Median progression-free survival on prior EGFR-TKIs aligned with clinical trial benchmarks. BRAF fusions in NSCLC are molecularly heterogeneous, with distinct genomic landscapes between de novo and acquired cases. These findings support repeated comprehensive genomic profiling at progression and suggest that pathway-directed combinations, such as MEK plus EGFR inhibition, may offer individualized treatment options for selected patients.

PMID 42546514
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PubMedThe Plant journal : for cell and molecular biology2026-08-04

Inosine monophosphate dehydrogenases are key players for functional development in Arabidopsis.

Dörfer Eva E, Sadeghi Zahra Z, Frick Vincent V, Ebel Katharina K et al.

In plants, nucleotide de novo synthesis is required throughout development to provide building blocks for the synthesis of DNA, RNA and nucleotide-derived cofactors. Inosine Monophosphate Dehydrogenases (IMPDH) are key enzymes in de novo guanylate synthesis. The genome of Arabidopsis thaliana encodes two IMPDHs and we identify IMPDH2 as the major isoform, being enzymatically active in the plant cytosol. Bimolecular fluorescence complementation (BIFC) analysis suggests that IMPDH1 and IMPDH2 interact with themselves and with Cytidine Triphosphate Synthetase (CTPS) isoforms, connecting purine and pyrimidine metabolism. Nucleotide quantification identifies IMPDH2 as a bottleneck in guanylate biosynthesis, and plants lacking this isoform suffer from nucleotide imbalance and limitation, causing reductions in ribosomal RNAs by reducing Target of Rapamycin (TOR) activity. Impaired photosynthesis and growth were further consequences thereof. In contrast, strong overexpression of IMPDH1 supported growth and led to altered organ development in 10% of corresponding plants presumably due to altered auxin metabolism during embryo development.

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PubMedFrontiers in oncology2026-08-04

Long-term risk of gynecologic malignancies in postmenopausal women with vaginal bleeding and benign endometrial lesions: a cohort study.

Lv Chunxiu C, Su Mingrui M, Zheng Xiaojuan X, Li Jinfeng J et al.

This study aims to assess the long-term incidence risk of gynecologic malignancy in postmenopausal women presenting with vaginal bleeding and pathologically confirmed benign endometrial lesions, and to screen for clinical independent risk factors to provide evidence for risk stratification and follow-up management of this population. We conducted a retrospective cohort study of 696 postmenopausal women presenting with vaginal bleeding who underwent diagnostic endometrial curettage. Histopathological evaluation established the initial diagnosis; patients with initially benign endometrial pathology underwent short-term (3-month) histologic re-evaluation, and eligible individuals were enrolled in long-term clinical follow-up. We compared the distribution of pathological subtypes between initial and follow-up diagnoses and performed univariate Cox regression and multivariate Cox proportional hazards regression analyses to identify independent predictors of gynecologic malignancy. The initial diagnosis rates of endometrial malignancy and precancerous lesions were 15.1% (105/696) and 2.9% (20/696), respectively. Among the 118 patients with initially benign endometrial pathology, 5.1% (6/118) and 7.6% (9/118) were diagnosed with malignancy and precancerous lesions, respectively, within 3 months of initial evaluation. Of the 453 patients eligible for long-term follow-up, 338 completed follow-up (25.4% lost to follow-up), during which 16 incident malignancies and 8 incident precancerous lesions were identified. High-grade serous carcinoma constituted a significantly higher proportion of malignancies detected during follow-up (43.8%) than of those diagnosed initially (6.5%; P < 0.001). Patients with high-grade serous carcinoma had a significantly lower BMI compared with those with endometrioid adenocarcinoma or precancerous lesions (P = 0.008); however, median diagnostic delay did not differ significantly across histologic subtypes (P = 0.850). Univariable Cox regression identified RDW, endometrial thickness, and age as factors associated with the risk of subsequent neoplasia. Multivariable Cox proportional hazards regression analysis confirmed baseline red blood cell distribution width (HR = 1.331, 95% CI: 1.086-1.630, P = 0.009) and endometrial thickness (HR = 4.452, 95% CI: 2.111-9.391, P < 0.001) as independent predictors of gynecologic malignancy. Our findings confirm that postmenopausal women with vaginal bleeding and initial benign endometrial lesions carry higher long-term gynecologic malignancy risk. Given their poor tumor prognosis, standardized screening and long-term surveillance are clinically vital for this high-risk cohort.

PMID 42549042
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