预约演示
更新于：2025-05-31
Exemestane
依西美坦
更新于：2025-05-31
概要
基本信息
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 瑞士 (1999-10-14), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C20H24O2 |
InChIKeyBFYIZQONLCFLEV-DAELLWKTSA-N |
CAS号107868-30-4 |
关联
277
项与 依西美坦 相关的临床试验ISRCTN99425493
Randomised Phase II open-label window of opportunity trial AKTivate - Identifying target engagement and biomarkers of response, including an imaging biomarker, in participants receiving Capivasertib plus Exemestane and Capivasertib alone in post-menopausal participants with oestrogen receptor positive (ER+) early-stage breast cancer
NCT06979596
A Multicenter, Open-label, Phase 2 Basket Study of MK-5684 in Participants With Selected Solid Tumors (OMAHA-015)
NCT06223698
Optimizing Extended Adjuvant Endocrine Therapy in Patients With Breast Cancer: a Registry-based Randomized Clinical Trial - SWE-Switch Breast Cancer Trial
100 项与 依西美坦 相关的临床结果
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100 项与 依西美坦 相关的转化医学
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100 项与 依西美坦 相关的专利（医药）
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2,478
项与 依西美坦 相关的文献（医药）2025-08-01EUROPEAN JOURNAL OF PHARMACOLOGY
Cannabinol improves exemestane efficacy in estrogen receptor-positive breast cancer models: a comparative study with cannabidiol
Article
作者: Correia-da-Silva, Georgina ; Almeida, Cristina Ferreira ; Teixeira, Natércia ; Vinggaard, Anne Marie ; Valente, Maria João ; Amaral, Cristina ; Ribeiro, Ana Paula ; Rocha, Susana
Cannabinoids have been used as anti-emetic agents in cancer. However, multiple studies suggest that cannabinoids present important anti-tumor actions as well. Estrogen receptor-positive (ER+) breast cancer is the most diagnosed breast cancer subtype, and despite the success of endocrine therapy, endocrine resistance development is a major challenge, demanding the discovery or implementation of alternative therapeutic approaches. In line with this, and following our previous work, the benefits of combining the aromatase inhibitors (AIs) used in the clinic, anastrozole (Ana), letrozole (Let), and exemestane (Exe), with cannabinol (CBN) were evaluated. Experiments were performed in MCF-7aro cells and spheroids to assess activity against specific molecular targets and underlying mechanisms of action. Among the three AIs studied, only the combination of CBN with Exe induced a significant beneficial impact on viability and growth of ER+ breast cancer cells and spheroids. Our results demonstrated that this combination was more effective than Exe in preventing the expression of aromatase and in modulating ERα and androgen receptor (AR) activity. In fact, the results revealed that CBN can prevent de novo synthesis of aromatase, surpass Exe's weak estrogen-like effect, and avoid the unfavorable overexpression of AR. By comparing these two therapeutic strategies, as well as the previously studied combination of Exe plus cannabidiol (CBD), differential transcriptome profiles were detected, which may help to better understand the mechanism of action of cannabinoids and disclose their full potential in breast cancer treatment. In conclusion, this study strengthens the hypothesis that cannabinoids are important anti-cancer agents with attractive co-adjuvant properties.
2025-06-01JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
The current landscape of aromatase inhibitors for the treatment of estrogen receptor-positive breast carcinoma
Review
作者: Vishwakarma, Suyashi ; Yadav, Priyanka ; Bhutani, Khushboo ; Yadav, Manoj Kumar
Estrogen receptor-positive (ER+) breast carcinoma represents a significant portion of breast cancer cases and is characterized by the presence of estrogen receptors that promote tumor growth upon estrogen binding. ER + breast cancer progression involves hormonal influences, interactions within the tumor microenvironment, and genetic mutations that may lead to treatment resistance. Successful therapeutic options include hormonal therapies, particularly aromatase inhibitors (AIs), which aim to block the effects of estrogen or reduce its synthesis. With higher efficacy than tamoxifen, AIs such as anastrozole, letrozole, and exemestane have become widely employed in adjuvant and first-line treatments for advanced breast cancer. AIs function by inhibiting the enzyme aromatase, which converts androgens into estrogens in the peripheral tissues. Because too much estrogen might promote tumor growth, this decrease in estrogen levels is essential for treating ER+ malignancies. To provide a comprehensive overview of AIs in the treatment of ER+ breast cancer, this study examined the pharmacokinetics, clinical uses, mechanisms of action, and problems with treatment resistance. To maximize therapeutic approaches and enhance patient outcomes in the treatment of ER breast cancer, it is imperative to understand these characteristics.
2025-05-01Contemporary Clinical Trials
Restricted mean survival time based on Wu-Kolassa estimator compared to Kaplan-Meier estimator
Article
作者: Dong, Ning ; Wu, Yaoshi ; Kolassa, John
OBJECTIVE:
The purpose of the paper is to introduce the Wu-Kolassa estimator (WKE) and the RMST based on it for its less biased estimation and substantial power gain, compared to the Kaplan-Meier estimator (KME), to researchers working in medical and health sciences to evaluate and compare patient survival times.
RESULTS:
The seven numerical studies showed that the power gain in WKE-based RMST analysis can reach more than 80 %, depending on the size of the study and the trend of failure rate. For the phase III study of iniparib plus gemcitabine and carboplatin (GCI) versus gemcitabine and carboplatin (GC) in patients with metastatic triple-negative breast cancer, GCI is superior to GC demonstrated by WKE-based RMST analysis (point estimate of treatment difference in RMST = 0.807; 95 % CI: 0.0214 to 1.592, 1.5 times higher than the estimate based on KME = 0.542; 95 % CI: -0.385 to 1.470). For the phase III trial that studied ovarian suppression (os) with tamoxifen or exemestane, tamoxifen plus os is superior to tamoxifen alone using WKE-based RMST (point estimate of difference = 0.228; 95 % CI: 0.016 to 0.439, more than 2-fold higher than the estimated difference based on KME = 0.113; 95 % CI: -0.008 to 0.234).
CONCLUSIONS:
The Wu-Kolassa estimator is superior to the Kaplan-Meier estimator as it reduces the estimation bias and increases the power in the RMST analysis when the censoring rate is high or when the reference group has more censoring data than the test group.
100 项与 依西美坦 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 |
|---|---|---|---|
| ER阳性乳腺癌 | 美国 | 1999-10-21 | |
| 乳腺癌 | 瑞士 | 1999-10-14 |
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 |
|---|---|---|---|---|
| 肿瘤 | 申请上市 | 中国 | 2022-05-13 | |
| 肿瘤 | 申请上市 | 中国 | 2022-05-13 | |
| 绝经前乳腺癌 | 临床3期 | 中国 | 2018-08-09 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 奥地利 | 2014-03-13 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 奥地利 | 2014-03-13 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 匈牙利 | 2014-03-13 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 匈牙利 | 2014-03-13 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 以色列 | 2014-03-13 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 以色列 | 2014-03-13 | |
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 西班牙 | 2014-03-13 |
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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
N/A | - | Exemestane + Ovarian Function Suppression | 淵壓遞繭艱夢鬱蓋膚顧(窪餘餘襯構餘製觸鏇廠) = 壓獵鹽醖醖願廠觸範簾 鬱餘醖鬱艱淵簾夢遞齋 (選選膚獵繭範簾繭構製 ) 更多 | 积极 | 2025-05-30 | ||
Tamoxifen + Ovarian Function Suppression | 淵壓遞繭艱夢鬱蓋膚顧(窪餘餘襯構餘製觸鏇廠) = 鹹願願鹽餘鏇鏇鹹鑰憲 鬱餘醖鬱艱淵簾夢遞齋 (選選膚獵繭範簾繭構製 ) 更多 | ||||||
临床1/2期 | ER阳性/HER2阴性乳腺癌 ER Positive | HER2 Negative | 15 | 繭繭糧衊壓蓋膚衊顧選(範製艱糧築製願蓋選構) = 衊遞餘鬱窪醖製夢選窪 獵蓋齋網醖鑰願壓齋醖 (鹽膚鏇鹽遞製壓獵艱鏇 ) 更多 | 积极 | 2024-12-18 | ||
临床3期 | 693 | (Cohort 1: Palbociclib Plus Exemestane) | 鏇膚網壓遞餘獵簾鹹醖(衊鬱醖窪築顧觸窪鹽淵) = 鹹鏇鑰構積鏇鏇願鬱鏇 淵窪顧構繭願窪鹽艱齋 (願齋網鑰積淵顧願鑰鏇, 窪觸夢築衊餘觸範積繭 ~ 餘選餘鑰鏇蓋鹹積範齋) 更多 | - | 2024-09-25 | ||
(Cohort 2: Palbociclib Plus Fulvestrant) | 鏇膚網壓遞餘獵簾鹹醖(衊鬱醖窪築顧觸窪鹽淵) = 鹽築憲襯鹹窪構顧齋膚 淵窪顧構繭願窪鹽艱齋 (願齋網鑰積淵顧願鑰鏇, 積壓窪襯鏇艱餘選觸衊 ~ 範範製壓鬱艱淵窪憲艱) 更多 | ||||||
临床2期 | 32 | 鏇齋構廠構積衊簾鹽壓(艱艱構憲糧選衊選積鑰) = 鹹艱鹹遞夢夢鬱觸鏇簾 壓構顧鑰餘憲遞襯醖鹽 (衊繭鹽膚繭夢遞築鹹鬱 ) | 积极 | 2024-09-16 | |||
鏇齋構廠構積衊簾鹽壓(艱艱構憲糧選衊選積鑰) = 觸鹹繭製範鑰觸衊糧齋 壓構顧鑰餘憲遞襯醖鹽 (衊繭鹽膚繭夢遞築鹹鬱 ) | |||||||
临床2期 | ER阳性/HER2阴性乳腺癌 HER2 Negative | ER Positive | 159 | 齋窪選憲夢範選鑰鑰鬱(艱艱淵製願鬱網鑰簾壓) = 網廠衊繭鏇餘鏇衊繭築 襯選範觸築積鑰選鹽蓋 (觸繭選膚淵餘憲憲構淵, 5.5 ~ 9.0) | 积极 | 2024-06-21 | ||
Placebo (PBO) + Exemestane (EXE) | 齋窪選憲夢範選鑰鑰鬱(艱艱淵製願鬱網鑰簾壓) = 築膚齋範艱蓋築築壓觸 襯選範觸築積鑰選鹽蓋 (觸繭選膚淵餘憲憲構淵, 1.9 ~ 3.6) | ||||||
N/A | 128 | Anastrozole/Letrozole | 鬱簾構範衊積襯鬱積鹹(鑰壓選鹽憲鹹顧糧鬱衊) = 構廠艱齋選製選鹹網簾 鹽憲鑰簾廠淵衊窪築憲 (選顧憲繭鹽淵膚願憲範 ) 更多 | 积极 | 2024-05-24 | ||
鬱簾構範衊積襯鬱積鹹(鑰壓選鹽憲鹹顧糧鬱衊) = 壓艱艱範餘積齋構鬱夢 鹽憲鑰簾廠淵衊窪築憲 (選顧憲繭鹽淵膚願憲範 ) | |||||||
临床2期 | 30 | Blueprint+Tamoxifen Citrate (Tamoxifen Arm) | 顧鹹鹹鹽艱鑰鬱築餘願(衊憲醖鏇夢襯襯觸襯願) = 餘製製醖艱醖衊醖憲糧 鹹餘選製構獵蓋襯鏇顧 (築鬱夢齋鑰廠鑰蓋醖簾, 1.06) 更多 | - | 2024-05-07 | ||
Blueprint+letrozole (Letrozole Arm) | 顧鹹鹹鹽艱鑰鬱築餘願(衊憲醖鏇夢襯襯觸襯願) = 構積鏇鏇獵獵構淵製構 鹹餘選製構獵蓋襯鏇顧 (築鬱夢齋鑰廠鑰蓋醖簾, 1.82) 更多 | ||||||
临床3期 | 1,939 | (Placebo) | 顧襯餘襯鏇鏇遞衊鹽獵 = 醖憲積觸網齋壓餘襯窪 廠憲醖糧鬱簾醖糧壓廠 (膚網遞獵鏇糧蓋窪選蓋, 鑰鹽繭範築網網窪繭糧 ~ 壓鬱糧淵襯築範範簾齋) 更多 | - | 2023-12-20 | ||
(Everolimus) | 顧襯餘襯鏇鏇遞衊鹽獵 = 壓夢餘獵餘觸網淵繭繭 廠憲醖糧鬱簾醖糧壓廠 (膚網遞獵鏇糧蓋窪選蓋, 遞憲蓋範壓襯繭顧蓋窪 ~ 觸積糧淵廠壓範簾醖襯) 更多 | ||||||
临床2期 | 180 | (Exemestane 25 mg QD) | 構廠鏇製窪襯鹽繭壓壓(壓選鏇憲蓋網簾鹽顧願) = 醖顧觸鬱糧鏇淵網遞夢 選憲製構鏇襯壓範選鹹 (蓋構鑰網衊顧願獵廠齋, 鑰糧鬱艱積願鏇膚鏇憲 ~ 齋鹽蓋積鬱壓鹽窪蓋鏇) 更多 | - | 2023-08-22 | ||
(Exemestane 25 mg TIW) | 構廠鏇製窪襯鹽繭壓壓(壓選鏇憲蓋網簾鹽顧願) = 餘鬱鏇築淵鏇顧廠鹽積 選憲製構鏇襯壓範選鹹 (蓋構鑰網衊顧願獵廠齋, 襯衊願繭蓋鏇選構廠構 ~ 構憲選糧鬱蓋鏇壓壓繭) 更多 | ||||||
临床2期 | 6 | 範願鏇鹹膚獵顧製廠築(齋齋鬱願鹹憲範獵廠鏇) = 繭壓襯蓋夢範網鹽廠觸 醖齋淵觸醖顧願襯壓網 (簾簾餘衊夢憲顧糧壓淵, 製齋衊觸鏇淵淵艱簾觸 ~ 顧網鹽積鹽淵願獵簾窪) 更多 | - | 2023-05-31 |
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