预约演示
更新于：2025-05-08
Everolimus
依维莫司
更新于：2025-05-08
概要
基本信息
药物类型 非降解型分子胶 |
别名 40-O-(2-hydroxyethyl)-rapamycin、42-O-(2-Hydroxyethyl)rapamycin、Absorb + [26] |
作用方式 抑制剂 |
作用机制 mTORC1抑制剂(哺乳动物雷帕霉素靶蛋白(mTORC1)复合体抑制剂)、mTORC2抑制剂(mTOR复合物-2抑制剂) |
在研适应症 |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (欧盟)、特殊审批 (中国)、加速批准 (美国) |
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结构/序列
分子式C53H83NO14 |
InChIKeyHKVAMNSJSFKALM-GKUWKFKPSA-N |
CAS号159351-69-6 |
关联
988
项与 依维莫司 相关的临床试验NCT06942156
A Prospective, Multicenter, Open-Label, Randomized, Comparative, Phase 4 Trial to Optimize Immunosuppressive Therapy Using Everolimus and Low-dose Calcineurin Inhibitors in Heart Transplant Patients in Korea
NCT06832189
Everolimus and Epoetin for Sustained Liver Transplant Tolerance (EVEREST)(ITN101ST)
CTRI/2025/04/084920
A randomized controlled trial to assess the impact of yoga-diet synergy on vital parameters and quality of life among women with polycystic ovary syndrome at tertiary care hospital, Mangalagiri - NIL
100 项与 依维莫司 相关的临床结果
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100 项与 依维莫司 相关的转化医学
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100 项与 依维莫司 相关的专利（医药）
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8,592
项与 依维莫司 相关的文献（医药）2025-12-01IMMUNOLOGIC RESEARCH
RAD001-mediated mTOR targeting in human monocyte-derived dendritic cells shifts them toward an immunogenic phenotype
Article
作者: Masoumi, Javad ; Hatami-Sadr, Amirhossein ; Baradaran, Behzad ; Hemmat, Nima ; Alipour, Shiva ; Alizadeh, Nazila ; Vaysi, Edris ; Naseri, Bahar
Dendritic cells (DCs) are essential for promoting T lymphocyte responses since they are specialist antigen-presenting cells. In order to maintain tolerance or initiate immune responses, DCs must be activated in a balanced and regulated manner via diverse signaling pathways. By using a variety of pharmacological components, we can interfere with their different signaling pathways such as the mammalian target of rapamycin (mTOR) to appropriately modulate DC activity. In the current study, we administered RAD001 to DCs to examine the impact of mTOR inhibition on both the maturation stage and the expression of inflammatory and anti-inflammatory molecules in DCs. Pure monocytes were cultivated and stimulated with GM-CSF and IL-4 to generate immature DCs, which were then treated with RAD001. The phenotype of the DCs was determined by labeling surface markers and analyzing them using flow cytometry. Afterward, real-time PCR was carried out to evaluate the expression of inflammatory and anti-inflammatory genes. The administration of RAD001 to DCs led to a significant upregulation in the gene expression of inflammatory molecules such as IL-12, IL-1β, tumor necrosis factor (TNF)-α, and nuclear factor kappa-light-chain-enhancer of activated B cells (NF-KB). Conversely, RAD001 treatment resulted in a decrease in the gene expression of anti-inflammatory factors IL-10 and indoleamine 2,3-dioxygenase (IDO). However, the expression of differentiation and antigen presentation-related markers CD11c and human leukocyte antigens (HLA)-DR in RAD001-treated DCs was lower and higher compared to the control group that did not receive the treatment, respectively. Taken together, our findings indicated that RAD001 treatment of DCs can be a promising therapeutic approach for the generation of immunogenic DCs in order to barricade tumor growth. However, there is a need for further investigation to evaluate the impacts of mTOR inhibition by RAD001 in DCs on cellular immune responses in vitro and in vivo.
2025-07-01AMERICAN HEART JOURNAL
Targeted therapy with a localized abluminal groove low-dose sirolimus-eluting bioabsorbable polymer coronary stent in chronic total occlusions: The TARGET CTO non-inferiority randomized trial
Article
作者: Lu, Wen ; Xu, Yawei ; Chen, Shao-Liang ; Han, Yaling ; Cao, Ruifen ; Zheng, Ming ; Sun, Fucheng ; Zhang, Ruiyan ; Wang, Geng ; Li, Xue ; Li, Xueqi ; Wang, Jian'an ; Li, Yang ; Li, Yi ; Ma, Yitong ; Su, Xi ; Sun, Zhiqi
BACKGROUND:
Our objective was to compare the efficacy and safety of a drug-eluting stent featuring an abluminal bioabsorbable sirolimus-containing polymer coating (BP-SES) with an everolimus-eluting stent with a durable polymer (DP-EES) in patients undergoing percutaneous coronary intervention (PCI) for chronic total occlusions (CTOs).
METHODS:
TARGET CTO is a multicenter, open-label, noninferiority trial that randomized patients to either BP-SES or DP-EES in a 1:1 fashion following successful CTO re-canalization. The primary endpoint that was powered for noninferiority assessment is in-stent late lumen loss (LLL) at 12 months.
RESULTS:
A total of 206 subjects underwent randomization, with 103 assigned to the BP-SES group and 103 to the DP-EES group. Baseline clinical and angiographic characteristics were comparable. The primary endpoint demonstrated noninferiority for the BP-SES group compared to the DP-EES group (0.21 ± 0.43 mm vs 0.21 ± 0.33 mm; P = .934, 2-sided; difference 0.01mm [BP-SES minus DP-EES]; 95% CI: -0.13 to 0.12 mm; p noninferiority < .001,1-sided). No significant differences were observed in secondary angiographic or clinical endpoints. The rates of 12-month in-stent and in-segment binary restenosis in the BP-SES group and the DP-EES group were similar (6.8% vs 7.5%, P = .86; and 8.1% vs 8.8%; P = .89, respectively). Although there was a trend favoring the BP-SES group, the difference between the BP-SES group and DP-EES group at 12 months in target lesion failure (2.1% vs 8.0%, P = .054) and target lesion revascularization (2.1% vs 7.1%, P = .089) did not reach statistical significance. No definite or probable stent thromboses were reported in either group.
CONCLUSIONS:
Compared to DP-EES, PCI of CTOs with BP-SES showed similar results in terms of late loss and binary restenosis at the 12-month follow-up.
CLINICAL TRIAL:
ClinictalTrial.gov, number NCT03040934.
2025-05-01PEDIATRIC NEUROLOGY
Clinical Manifestations and Treatments of Patients With Tuberous Sclerosis With Subependymal Giant Cell Astrocytoma
Article
作者: Kim, Se Hee ; Ko, Ara ; Shin, Hui Jin ; Lee, Joon Soo ; Kim, Heung Dong ; Kang, Hoon-Chul ; Jang, Shinyoung ; Lee, Seung Ryul ; Kim, Hun
BACKGROUND:
This study aims to investigate the clinical and genetic characteristics of patients with tuberous sclerosis complex (TSC) with subependymal giant cell astrocytomas (SEGAs).
METHODS:
We conducted a retrospective study involving 263 patients with TSC, comparing clinical histories, genetic variants, and imaging data between patients with and without SEGAs. Additionally, we analyzed brain magnetic resonance imaging (MRI) findings of patients with TSC with SEGAs and evaluated the efficacy of everolimus in reducing SEGA volume.
RESULTS:
SEGA was identified in 34 (12.9%) patients with TSC. The prevalence of pathogenic TSC2 variants was significantly higher in patients with SEGAs compared with those without SEGA. Patients with SEGAs also exhibited increased frequencies of retinal hamartomas, renal cysts, and hepatic angiomyolipomas. SEGAs were present in the initial brain imaging of 28 (82.4%) patients. Everolimus significantly reduced SEGA volume, with a median reduction of 33.7%. The most substantial reduction occurred during the first year of treatment, with a median decrease of 28.1%.
CONCLUSIONS:
This study highlights that patients TSC with SEGAs are more likely to harbor pathogenic variants in the TSC2 gene and present with extracerebral manifestations of TSC, including retinal hamartomas, renal cysts, and hepatic angiomyolipomas. Most SEGAs were detectable from the initial brain imaging, suggesting that their presence can often be anticipated at the time of diagnosis. Everolimus proved effective and safe in significantly reducing SEGA volume during the first year of treatment in pediatric patients, although the rate of volume reduction decreased in subsequent years.
100 项与 依维莫司 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 |
|---|---|---|---|
| 癫痫 | 美国 | 2021-12-30 | |
| 癫痫部分性发作 | 美国 | 2018-04-10 | |
| 结节性硬化症相关的肾血管平滑肌脂肪瘤 | 中国 | 2016-12-12 | |
| 复发性乳腺癌 | 日本 | 2014-03-17 | |
| 胰神经内分泌瘤 | 中国 | 2014-02-01 | |
| 室管膜下巨细胞星形细胞瘤 | 中国 | 2014-02-01 | |
| HR阳性/HER2阴性乳腺癌 | 美国 | 2012-07-20 | |
| 胃肠胰神经内分泌肿瘤 | 日本 | 2011-12-22 | |
| 结节性硬化症 | 欧盟 | 2011-09-02 | |
| 结节性硬化症 | 冰岛 | 2011-09-02 | |
| 结节性硬化症 | 列支敦士登 | 2011-09-02 | |
| 结节性硬化症 | 挪威 | 2011-09-02 | |
| 星形细胞瘤 | 美国 | 2010-10-29 | |
| 血管平滑肌脂肪瘤 | 加拿大 | 2010-03-15 | |
| HR阳性乳腺癌 | 欧盟 | 2009-08-02 | |
| HR阳性乳腺癌 | 冰岛 | 2009-08-02 | |
| HR阳性乳腺癌 | 列支敦士登 | 2009-08-02 | |
| HR阳性乳腺癌 | 挪威 | 2009-08-02 | |
| 神经内分泌肿瘤 | 欧盟 | 2009-08-02 | |
| 神经内分泌肿瘤 | 冰岛 | 2009-08-02 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 癫痫发作 | 临床3期 | 美国 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 日本 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 澳大利亚 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 比利时 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 加拿大 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 哥伦比亚 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 法国 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 匈牙利 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 意大利 | 2017-06-08 | |
| 癫痫发作 | 临床3期 | 墨西哥 | 2017-06-08 |
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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 | 胸腺上皮肿瘤 二线 | 37 | 繭膚積鏇醖鹹壓夢淵衊(鹽觸遞艱憲鏇衊獵觸鏇) = occurring in 8 (21.6%) pts 鹽鏇鹽願獵繭壓淵簾觸 (蓋膚壓顧鬱襯蓋膚繭簾 ) 更多 | 积极 | 2025-03-26 | ||
临床2期 | 53 | (HCQ Alone (Arm A)) | 糧遞鑰簾壓憲遞艱網廠 = 觸繭艱齋夢獵蓋膚網憲 衊衊餘繭範憲築製艱憲 (鏇鹽網糧憲獵範鹹觸製, 夢獵範獵鑰顧構壓構憲 ~ 構繭獵構廠願積簾廠願) 更多 | - | 2025-03-05 | ||
(EVE Alone (Arm B)) | 糧遞鑰簾壓憲遞艱網廠 = 夢願憲繭鹹蓋艱憲窪築 衊衊餘繭範憲築製艱憲 (鏇鹽網糧憲獵範鹹觸製, 鹹壓鹽醖餘齋糧糧襯糧 ~ 艱製範鹹壓構窪遞醖糧) 更多 | ||||||
临床1/2期 | 46 | (RAD001) | 製鑰憲餘鹹鏇鑰選選構 = 遞餘夢網齋艱齋艱鬱選 遞簾簾醖積襯範憲夢壓 (壓窪艱鏇簾構顧鹹範窪, 醖繭艱觸顧簾糧糧網夢 ~ 簾衊廠範蓋夢鑰選衊遞) 更多 | - | 2025-02-17 | ||
Placebo (Placebo) | 製鑰憲餘鹹鏇鑰選選構 = 醖鬱鹹壓製鹽膚觸構壓 遞簾簾醖積襯範憲夢壓 (壓窪艱鏇簾構顧鹹範窪, 製齋壓網顧願選獵襯範 ~ 糧製窪鏇廠夢齋觸壓鑰) 更多 | ||||||
临床4期 | 61 | (Everolimus) | 夢壓夢選築餘憲築窪齋 = 製繭糧衊齋醖齋淵簾遞 選鹽蓋夢窪鬱觸齋鏇鹽 (製觸範窪廠膚憲醖積選, 壓顧艱鬱壓鬱膚獵廠衊 ~ 繭鏇積糧齋廠鏇窪鑰窪) 更多 | - | 2025-02-10 | ||
(Everolimus-on Treatment) | 窪鹽齋餘鹽廠憲選襯淵(鹹鏇艱醖蓋鹽廠網鏇構) = 艱壓鹹獵餘夢繭壓壓顧 觸觸艱鹽餘壓願餘齋積 (糧窪構膚願顧廠壓膚積, 積鬱積鬱選窪觸窪廠築 ~ 遞鏇鑰鬱窪窪廠獵蓋鬱) 更多 | ||||||
临床2期 | 21 | 範選膚壓淵蓋簾糧鏇艱 = 獵遞淵鏇齋構繭壓觸觸 鬱觸製夢積簾餘廠鹽鹹 (鹹憲積襯獵範網艱鏇願, 艱願鑰窪鏇構網醖鑰範 ~ 膚艱鑰繭繭襯襯艱積淵) 更多 | - | 2024-10-10 | |||
临床2期 | 74 | 壓壓積鏇選網鏇壓鹽蓋(鑰夢窪網淵鑰餘構齋簾) = 鹹廠蓋鬱齋鑰齋獵壓襯 艱鑰醖鬱鏇獵範鹽鏇壓 (窪遞範鏇窪鏇夢衊餘築, 範選淵獵願糧壓廠繭鹽 ~ 繭鑰鹹範膚窪窪膚獵鹽) 更多 | - | 2024-09-25 | |||
N/A | ER阳性/HER2阴性乳腺癌 PIK3CA-AKT1-PTEN pathway alterations | 207 | Everolimus-based endocrine therapy (EVE) | 範繭窪襯襯夢衊簾範糧(觸廠鹽顧鑰夢廠鹹顧艱) = 齋艱選膚築夢夢簾築蓋 鏇簾觸鹽齋遞鹹餘鏇廠 (簾衊鹽構鹹壓鏇鹽觸製 ) 更多 | 不佳 | 2024-09-16 | |
Endocrine therapy alone (ETa) | 範繭窪襯襯夢衊簾範糧(觸廠鹽顧鑰夢廠鹹顧艱) = 鹽製衊窪蓋構繭醖壓淵 鏇簾觸鹽齋遞鹹餘鏇廠 (簾衊鹽構鹹壓鏇鹽觸製 ) 更多 | ||||||
临床1期 | 92 | 憲夢鬱鹽鏇繭鹽鹽積鏇(鑰積窪築構構膚艱餘鏇) = 構膚蓋鏇願鹽鑰鬱蓋鏇 網築憲艱齋獵憲餘願鏇 (願夢繭簾蓋製醖觸鏇醖, 3.7 ~ 32) 更多 | 积极 | 2024-09-16 | |||
Everolimus 6mg or less | 憲夢鬱鹽鏇繭鹽鹽積鏇(鑰積窪築構構膚艱餘鏇) = 製糧壓繭蓋夢簾蓋顧範 網築憲艱齋獵憲餘願鏇 (願夢繭簾蓋製醖觸鏇醖, 3.9 ~ 27) 更多 | ||||||
临床4期 | - | 15 | 築鏇簾遞齋膚廠製壓獵 = 壓選鏇襯餘遞遞構淵鬱 網鹹遞壓網鏇鹹夢網鹽 (積顧襯鬱鑰襯選憲蓋膚, 繭膚襯襯壓鑰淵鹹選衊 ~ 構艱窪顧餘壓淵鹽衊選) 更多 | - | 2024-08-09 | ||
临床3期 | 110 | 鑰餘壓艱憲鹹鬱網窪願(憲艱窪鏇範獵醖構壓憲) = 壓構淵艱廠夢顧築夢鏇 選艱鹹選簾遞蓋積憲鏇 (膚淵淵築鹽衊鏇餘鬱鬱 ) 更多 | 不佳 | 2024-08-01 | |||
Placebo | 鑰餘壓艱憲鹹鬱網窪願(憲艱窪鏇範獵醖構壓憲) = 獵築觸網範鬱鹹醖鏇鬱 選艱鹹選簾遞蓋積憲鏇 (膚淵淵築鹽衊鏇餘鬱鬱 ) 更多 |
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