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更新于：2025-12-12
Fulvestrant
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更新于：2025-12-12
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2002-04-25), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、优先审评 (美国) |
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结构/序列
分子式C32H47F5O3S |
InChIKeyVWUXBMIQPBEWFH-WCCTWKNTSA-N |
CAS号129453-61-8 |
关联
513
项与 氟维司群 相关的临床试验NCT07235618
A Phase II, Two-Stage Study Evaluating the Efficacy of Entinostat in Combined With Fulvestrant in Locally Advanced or Metastatic Breast Cancer With Recurrence or Progression After CDK4/6 Inhibitor Plus Endocrine Therapy
NCT07235176
A Phase Ib/II Clinical Study to Evaluate Safety, Preliminary Efficacy and PK Characteristic of QLS1304 Combined With Endocrine Therapy in ER+/HER2- Breast Cancer Patients
NCT07226349
A Phase 1a/1b, Open-Label Study Evaluating the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Antitumor Activity of BG-75098 Alone and in Combination With Other Agents in Patients With Advanced Solid Tumors
100 项与 氟维司群 相关的临床结果
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100 项与 氟维司群 相关的转化医学
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100 项与 氟维司群 相关的专利（医药）
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5,315
项与 氟维司群 相关的文献（医药）2026-02-01BREAST
Real-world outcomes with palbociclib, ribociclib, and abemaciclib plus endocrine therapy in HR+/HER2− advanced breast cancer: A multicenter retrospective study
Article
作者: Kiszka, Joanna ; Lipiec, Paulina ; Żubrowska, Justyna ; Danielewicz, Iwona ; Bieńkowski, Michał ; Kustra, Ewa ; Szymanowski, Bartosz ; Pogoda, Katarzyna ; Czartoryska-Arłukowicz, Bogumiła ; Bałata, Anna ; Lewandowski, Tomasz ; Łobaza, Magdalena ; Sobocki, Bartosz K ; Szymanik-Resko, Magdalena ; Hudała-Klecha, Joanna ; Winsko-Szczęsnowicz, Karolina ; Tomasik, Bartłomiej ; Koriat-Błońska, Anna ; Kalinka, Ewa ; Jurczyk, Michał ; Kowalewska-Felczak, Agnieszka ; Grela-Wojewoda, Aleksandra ; Szwiec, Marek ; Łacko, Aleksandra ; Soter, Katarzyna ; Ziobro, Marek ; Duchnowska, Renata ; Kade, Grzegorz ; Myśliwiec, Paulina ; Streb, Joanna ; Radecka, Barbara ; Ramlau, Rodryg ; Jassem, Jacek ; Smok-Kalwat, Jolanta ; Litwiniuk, Maria
BACKGROUND:
Cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) combined with endocrine therapy (ET) are the standard first- and second-line treatments for hormone receptor-positive (HR+), HER2-negative (HER2-) advanced breast cancer (ABC). Real-world data (RWD) may inform the optimal use of these agents in routine practice.
PATIENTS AND METHODS:
The multicenter, population-based POLiCDK study compared progression-free survival (PFS), second PFS, and overall survival (OS) in ABC patients with HR+/HER2- ABC treated with palbociclib (PAL), ribociclib (RIB), or abemaciclib (ABE) in first- or second-line ET settings at 16 Polish centers between September 2017 and January 2025. Analyses were stratified by endocrine sensitivity/resistance, and stabilized inverse probability of treatment weighting was used to balance baseline characteristics.
RESULTS:
Among 2063 patients (701 PAL, 968 RIB, 394 ABE), 1583 (76.7 %) received CDK4/6i in the first-line and 480 (23.3 %) in the second-line setting. Overall, 927 (44.9 %) had de novo ABC; 819 (39.7 %) were endocrine-naïve, 158 (8.9 %) primary resistant, and 808 (39.2 %) secondary resistant. Median follow-up was 35.9, 24.1, and 21.4 months for PAL, RIB, and ABE, respectively. In endocrine-naïve patients, PFS did not differ significantly between CDK4/6i combined with aromatase inhibitors (AIs). In secondary endocrine-resistant disease, RIB and ABE outperformed PAL with AI combinations, whereas outcomes with fulvestrant were similar. In second-line therapy, all three CDK4/6i showed comparable results. Adjusted hazard ratios confirmed these trends without consistent superiority of any single agent.
CONCLUSIONS:
Endocrine sensitivity/resistance and ET partner were major determinants of outcome with CDK4/6i plus ET in HR+/HER2- ABC, informing individualized treatment selection and sequencing.
2026-01-01ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY
A combined study of network-based prediction and in vitro experimental validation on the procarcinogenic mechanism of propylparaben in estrogen receptor-positive breast cancer cells
Article
作者: Sun, Weiliang ; Zhu, Huijun ; Yue, Haiying ; Liang, Yingying ; Mo, Laiming ; Qin, Yanqiu ; Wen, Jiaying
OBJECTIVE:
To investigate the carcinogenic mechanisms and potential molecular targets of the environmental endocrine disruptor Propylparaben in estrogen receptor-positive breast cancer.
METHODS:
Based on a network toxicology strategy, this study first predicted and analyzed the physicochemical properties and in vivo/vitro toxicity of Propylparaben, screened its potential targets, and intersected them with estrogen receptor-positive breast cancer-related genes to obtain candidate toxicological targets. GO, KEGG, and PPI enrichment analyses were subsequently performed to identify key functional modules. Transcriptomic data from breast cancer were integrated, and core targets were screened using LASSO regression, SVM-RFE, and random forest algorithms. A multigene diagnostic model was then constructed, evaluated, and externally validated. Differential expression analysis, protein-level validation, and molecular docking were conducted to confirm expression patterns and binding capabilities of the core targets. Using MCF-7 cells as the in vitro model, dose-dependent Propylparaben intervention experiments were conducted to examine the transcriptional responses of the target genes. Drug sensitivity prediction, survival analysis, and GSEA-based functional annotation were further performed to evaluate the clinical potential and oncogenic mechanisms of the core targets.
RESULTS:
Propylparaben demonstrated strong estrogen receptor agonist activity, metabolic enzyme inhibition, and moderate carcinogenic risk, suggesting classical endocrine-disrupting properties. A total of 109 candidate toxicological targets associated with estrogen receptor-positive breast cancer were identified and found enriched in carcinogenic and tumor-suppressive pathways such as PI3K/AKT, mTOR, MAPK, and p53. Eight core targets were selected via machine learning, with SLC2A1 and KIF11 showing significant upregulation at both mRNA and protein levels, as well as stable binding affinities with Propylparaben. MCF-7 cell experiments confirmed their dose-dependent transcriptional upregulation upon Propylparaben treatment. Drug sensitivity analysis revealed that high expression of these targets correlated with increased sensitivity to Fulvestrant. KIF11 was predictive of neoadjuvant therapy response, while high SLC2A1 expression was significantly associated with poor survival outcomes. GSEA indicated that high expression of these genes significantly activated glycolysis, cell cycle, mTORC1, MYC, and E2F pathways, while suppressing antitumor mechanisms including p53 and complement cascades.
CONCLUSION:
Propylparaben may promote the occurrence and progression of estrogen receptor-positive breast cancer by upregulating SLC2A1 and KIF11, activating metabolic and proliferative pathways, and simultaneously suppressing tumor-suppressive signals.
2025-12-01ARCHIVES OF PHARMACAL RESEARCH
Advances and challenges of estrogen receptor-targeted agents in breast cancer
Review
作者: Fang, Wentong ; Hu, Jie ; Sun, Huayu ; Liu, Jie ; Zhong, Songyang
Estrogen receptors (ERs) are expressed in approximately 70% of breast cancer patients and serve as pivotal therapeutic targets. ER-targeting agents like selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) have harvested encouraging clinical outcomes. However, the expansion of their clinical utility remains limited by adverse effects, acquired resistance, and suboptimal pharmacokinetic properties. Recent advancements in ER biology have driven the development of novel ER-targeted agents, including third-generation SERMs, oral SERDs, complete ER antagonists, selective ER covalent antagonists, SERM/SERD hybrids, selective human ER partial agonists, and dual-mechanism ER inhibitors. Moreover, innovative technologies, such as proteolysis-targeting chimeras, molecular glue degraders, and lysosome-targeting chimeras have revolutionized ER degradation strategies, offering possibilities to circumvent drug resistance and enhance therapeutic efficacy. Despite these advances, only two ER-targeted drugs have been officially approved to date, indicating the barriers on the road to clinical translation. This review summarizes the recent progresses and challenges in the development of ER-targeted drugs, aiming to offer a perspective into the future of anti-ER therapies in breast cancer management.
100 项与 氟维司群 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 晚期乳腺癌 | 巴西 | 2018-06-25 | |
| 转移性乳腺癌 | 巴西 | 2018-06-25 | |
| HR阳性乳腺腺癌 | 美国 | 2017-08-25 | |
| 乳腺癌 | 日本 | 2011-09-26 | |
| ER阳性乳腺癌 | 欧盟 | 2004-03-09 | |
| ER阳性乳腺癌 | 冰岛 | 2004-03-09 | |
| ER阳性乳腺癌 | 列支敦士登 | 2004-03-09 | |
| ER阳性乳腺癌 | 挪威 | 2004-03-09 | |
| HR阳性/HER2阴性乳腺癌 | 欧盟 | 2004-03-09 | |
| HR阳性/HER2阴性乳腺癌 | 冰岛 | 2004-03-09 | |
| HR阳性/HER2阴性乳腺癌 | 列支敦士登 | 2004-03-09 | |
| HR阳性/HER2阴性乳腺癌 | 挪威 | 2004-03-09 | |
| HR阳性乳腺癌 | 美国 | 2002-04-25 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| HER2阳性乳腺癌 | 临床3期 | 奥地利 | 2021-09-14 | |
| HER2阳性乳腺癌 | 临床3期 | 法国 | 2021-09-14 | |
| HER2阳性乳腺癌 | 临床3期 | 意大利 | 2021-09-14 | |
| HER2阳性乳腺癌 | 临床3期 | 荷兰 | 2021-09-14 | |
| HER2阳性乳腺癌 | 临床3期 | 西班牙 | 2021-09-14 | |
| HER2阳性乳腺癌 | 临床3期 | 瑞士 | 2021-09-14 | |
| HER2 阴性乳腺癌 | 临床3期 | 意大利 | 2018-02-02 | |
| 6型髓鞘减少脑白质营养不良 | 临床3期 | 意大利 | 2018-02-02 | |
| 早期乳腺癌 | 临床3期 | 西班牙 | 2007-11-01 | |
| 孤立性纤维瘤 | 临床3期 | 加拿大 | 2004-01-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | HR阳性/HER2阴性乳腺癌 HR Positive | HER2 Negative | 40 | 蓋積夢獵製鏇鏇繭願繭(蓋廠壓築夢顧糧願鬱顧) = 選糧築製鬱遞餘鹽構選 積鹽夢齋製網鹽簾網鬱 (遞鏇構鏇築鑰衊淵窪選, 3.5 ~ 8.3) 更多 | 积极 | 2025-10-17 | ||
(Not previously received CDK4/6i) | 蓋積夢獵製鏇鏇繭願繭(蓋廠壓築夢顧糧願鬱顧) = 築獵糧鬱蓋築觸網範壓 積鹽夢齋製網鹽簾網鬱 (遞鏇構鏇築鑰衊淵窪選 ) | ||||||
| - | HR阴性/HER2阳性乳腺癌 hormone receptor-positive | HER2-negative | 172 | 選齋淵觸構夢積範窪網(淵夢窪衊壓網齋製夢顧): P-Value = 0.042 | 积极 | 2025-10-17 | ||
临床3期 | 698 | (Faslodex + Placebo) | 窪襯壓願鹹淵窪願鹹鹽(顧簾艱窪壓齋積餘蓋鏇) = 鑰糧願襯膚獵餘鏇構簾 餘繭獵淵簾衊獵製淵鹹 (窪蓋選鏇鏇鹹夢選壓鬱, 衊壓淵觸壓積膚繭觸積 ~ 鹹鏇製鬱衊壓鏇鑰廠糧) 更多 | - | 2025-06-04 | ||
(Faslodex + Arimidex) | 窪襯壓願鹹淵窪願鹹鹽(顧簾艱窪壓齋積餘蓋鏇) = 積鏇餘糧淵鏇鏇觸艱獵 餘繭獵淵簾衊獵製淵鹹 (窪蓋選鏇鏇鹹夢選壓鬱, 鏇壓構積繭齋鹽鑰衊顧 ~ 鑰顧餘網觸窪糧鑰膚糧) 更多 | ||||||
N/A | HR+ | HER2-negative | 1,085 | 餘襯範夢糧窪蓋簾蓋蓋(餘衊積壓繭夢鏇製醖鹹) = 鹹製願鹽顧衊選蓋齋憲 鏇餘淵觸廠製廠製構鏇 (窪衊蓋顧窪繭淵窪顧鹽 ) 更多 | 不佳 | 2025-05-14 | ||
临床2期 | 58 | 襯範遞鑰構廠窪鬱網醖(糧壓醖壓鏇鏇願構艱鑰) = <10% 餘窪窪蓋膚遞獵醖範鹹 (壓襯願鹹窪鬱範鹹鏇壓 ) 更多 | 积极 | 2025-04-29 | |||
临床3期 | - | 壓鬱夢觸襯遞齋鏇獵襯(顧觸觸淵齋壓簾積餘觸) = expected mPFS is 25 to 28 months 構窪範願範獵艱顧鬱醖 (範觸繭鬱製鹽獵顧觸構 ) 更多 | 积极 | 2025-04-29 | |||
临床3期 | 368 | (Arm A: Abemaciclib Plus Fulvestrant) | 餘鏇構築鹽壓製願鏇憲(鹹網膚餘鬱遞獵網構蓋) = 網願獵範鏇鬱顧鹹衊艱 簾夢齋願鏇壓淵壓醖糧 (製衊醖襯範淵淵簾餘鏇, 蓋壓製夢淵積膚鹹範網 ~ 獵夢淵齋繭網遞獵壓鬱) 更多 | - | 2025-02-27 | ||
Placebo+Fulvestrant (Arm B: Placebo Plus Fulvestrant) | 餘鏇構築鹽壓製願鏇憲(鹹網膚餘鬱遞獵網構蓋) = 簾鹹廠積壓餘膚觸選膚 簾夢齋願鏇壓淵壓醖糧 (製衊醖襯範淵淵簾餘鏇, 壓醖膚積觸淵膚獵鹽鑰 ~ 衊衊鹹鏇遞餘壓積襯積) 更多 | ||||||
临床2期 | 4 | (Fulvestrant) | 鏇簾夢醖鏇醖壓艱鑰衊(鬱廠齋醖觸構鬱積鑰糧) = 窪繭網範積鹹積觸願壓 構醖築夢餘襯餘夢範齋 (構窪夢鑰衊構網艱獵艱, 糧顧憲鬱範築顧醖簾餘 ~ 膚糧繭夢艱餘網襯憲鏇) 更多 | - | 2024-12-27 | ||
(Continuing AI After Randomization) | 鏇簾夢醖鏇醖壓艱鑰衊(鬱廠齋醖觸構鬱積鑰糧) = 構網夢餘艱積窪糧簾鑰 構醖築夢餘襯餘夢範齋 (構窪夢鑰衊構網艱獵艱, 憲網選糧餘鬱夢鹽夢醖 ~ 鑰範觸願繭鬱廠窪鹽製) 更多 | ||||||
临床2期 | 486 | (Arm A) | 憲齋願構範齋鬱鹹鑰蓋 = 鏇觸製鹹糧夢廠觸鹽築 鹹憲廠衊繭襯鹽衊壓衊 (遞廠鹽顧鑰願範窪齋膚, 糧選構顧壓簾糧觸餘衊 ~ 餘積襯獵壓簾衊鹽醖蓋) 更多 | - | 2024-12-09 | ||
(Arm B) | 憲齋願構範齋鬱鹹鑰蓋 = 衊淵憲衊選餘衊糧憲範 鹹憲廠衊繭襯鹽衊壓衊 (遞廠鹽顧鑰願範窪齋膚, 繭衊膚製膚繭餘衊淵襯 ~ 糧積憲夢網獵淵淵範製) 更多 | ||||||
临床3期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 PIK3CA | AKT1 | PTEN | 708 | 願製顧選鑰鬱網壓齋積(簾築簾願廠鹽窪鏇顧窪): HR = 0.6 (95% CI, 0.51 ~ 0.71) 更多 | 积极 | 2024-12-01 | ||
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