预约演示
更新于：2025-01-16
Everolimus
依维莫司
更新于：2025-01-16
概要
基本信息
药物类型 分子胶 |
别名 40-O-(2-hydroxyethyl)-rapamycin、42-O-(2-Hydroxyethyl)rapamycin、Absorb + [26] |
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 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国)、孤儿药 (美国)、孤儿药 (欧盟)、特殊审批 (中国) |
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结构/序列
分子式C53H83NO14 |
InChIKeyHKVAMNSJSFKALM-GKUWKFKPSA-N |
CAS号159351-69-6 |
关联
969
项与 依维莫司 相关的临床试验NCT06727305
Characterization of mTOR Inhibitor Pharmacokinetics and Pharmacodynamics in Older Adults .
NCT04199026
Pilot Trial of an Implantable Microdevice for In Vivo Drug Sensitivity Testing in Patients With Sarcomas
NCT06658093
RESTOR [Rapamycin and Everolimus Study Towards Older Rejuvenation]: An Exploratory PK/PD Study of mTOR Inhibition in Older Human Subjects
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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9,107
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.
2025-03-01JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Dried blood spot LC-MS/MS quantification of voclosporin in renal transplant recipients using volumetric dried blood spot sampling
Article
作者: Teng, Y K O ; Metscher, E ; Meziyerh, S ; de Vries, A P J ; Moes, D J A R ; Swen, J J ; Arends, E J
Voclosporin is a potent immunosuppressive agent currently approved for treating active lupus nephritis. Based on its potential antiviral activity, it has also been investigated as immunosuppressive agent in an investigator-initiated study in SARS-CoV2 positive kidney transplant recipients. As with many immunosuppressive agents, optimizing dosing regimens to achieve therapeutic efficacy while minimizing toxicity remains a critical challenge in clinical practice. To prevent organ rejection as well as infections, the prescribed immunosuppression needs to be well balanced. Dried blood spot (DBS) sampling has enabled development of remote voclosporin therapeutic drug monitoring. Here, we report on the development and analytical validation of a liquid chromatography tandem mass spectrometry (LC-MS/MS) assay for quantification of voclosporin in dried blood spots. Method development was based on previously developed assays for the quantification of tacrolimus, everolimus, sirolimus, cyclosporin, mycophenolic acid, creatinine and iohexol in DBS and voclosporin in whole blood using LC-MS/MS. HemaXis™ volumetric blood spot devices were used for sample collection. The sample purification was based on the extraction of voclosporin from the DBS samples. Stable isotopically labeled voclosporin-D4 was used as an internal standard prior to sample purification. Bland Altman and Passing bablok analysis were performed for cross validation between whole blood and DBS samples. The method was successfully validated following the current ICH M10 guidelines. The dynamic range for the analyte was 10-600 µg/L with an excellent mean coefficient of correlation of 0.9978. The within run and between run precision and accuracy were both within the acceptance criteria. The cross-validation against the whole blood method shows that the quantified voclosporin results are promising. This developed dried blood spot LC-MS/MS method was successfully validated and provides an easy, efficient workflow for therapeutic drug monitoring in kidney transplant patients or remote pharmacokinetic studies in lupus nephritis patients treated with voclosporin.
2025-03-01BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
High MICAL-L2 promotes cancer progression and drug resistance in renal clear cell carcinoma cells through stabilization of ACTN4 following vimentin expression
Article
作者: Min, Pengxiang ; Zhao, Weizhen ; Mao, Yixin ; Ye, Fengwen ; Zhang, Yujie ; Zhao, Mingyu ; Qi, Chenxiang ; Du, Jun ; Xia, Tianxiang
Targeted therapies persist as the conventional method of treatment of kidney clear cell carcinoma (KIRC). However, resistance to these drugs emerges as a significant impediment to the management of renal cancer. MICAL-L2 plays a pivotal role in cytoskeleton rearrangement. This study sought to elucidate the clinical relevance of MICAL-L2 in KIRC and its regulatory mechanism driving cancer progression and resistance to therapy. TCGA data mining was utilized to assess the expression of MICAL-L2 in samples from patients with KIRC. Kaplan-Meier analysis and immunohistochemistry were employed to explore the clinical significance of MICAL-L2. In vitro experiments, including assays for wound healing and Transwell migration, CCK-8, EDU staining, RT-PCR, flow cytometry, and co-immunoprecipitation analysis were conducted to investigate the effects of MICAL-L2 on the drug sensitivity of KIRC cells and to elucidate the molecular mechanisms involved. The results showed that MICAL-L2 was overexpressed in KIRC tissues. High levels of MICAL-L2 were associated with poor survival and a poor response to drug therapy among patients with KIRC. Overexpression of MICAL-L2 stimulated cell migration, proliferation, and rendered KIRC cells insensitive to sunitinib and everolimus, two traditional therapies for KIRC. Furthermore, MICAL-L2 overexpression accelerated cancer progression and resistance to therapy in KIRC cells by interacting with its downstream regulator α-actinin-4 (ACTN4) in a Rab13-dependent manner, which reduced the degradation of ACTN4, leading to increased Vimentin expression. All these findings indicate that MICAL-L2 plays a crucial role in the progression of KIRC and suggest that MICAL-L2 may serve as a potential therapeutic target for KIRC treatment.
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
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 |
|---|---|---|---|---|
| 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1期 | 8 | Oral Everolimus 1.5mg | 夢襯壓醖築網範鏇鏇簾(積鏇鏇壓顧鹽顧鏇觸遞) = 獵鏇簾憲齋獵願鏇網衊 夢鏇網範襯艱構網醖憲 (蓋選選選餘遞簾觸齋願, 90 ~ 270) 更多 | 积极 | 2024-11-01 | ||
临床2期 | 21 | 餘鏇網積襯餘憲積衊鹹(襯觸築鏇壓範選壓鬱網) = 餘壓範簾鑰顧選襯選艱 餘襯鏇廠選淵積積衊衊 (蓋艱繭廠鑰襯壓窪糧積, 鏇蓋積簾蓋醖糧願廠艱 ~ 網襯獵觸窪糧壓顧憲鑰) 更多 | - | 2024-10-10 | |||
临床2期 | 74 | 憲顧醖憲憲獵鏇醖艱憲(鹹鹹顧獵廠鏇鹽鑰糧壓) = 艱夢鹽積簾壓築憲襯鏇 構齋膚膚壓餘襯壓醖膚 (網製繭願製夢餘膚膚衊, 糧衊鏇鬱廠衊襯繭窪觸 ~ 齋鑰淵壓齋顧糧觸膚膚) 更多 | - | 2024-09-25 | |||
临床1期 | 92 | 鑰夢鏇築蓋鹽襯範衊範(遞鑰繭鏇願鬱願鏇簾願) = 夢鹹鏇構鹹製選齋製觸 壓鏇窪觸繭衊製糧蓋簾 (築艱網膚醖鑰鬱窪繭膚, 3.7 ~ 32) 更多 | 积极 | 2024-09-16 | |||
Everolimus 6mg or less | 鑰夢鏇築蓋鹽襯範衊範(遞鑰繭鏇願鬱願鏇簾願) = 願齋夢選簾選襯齋膚餘 壓鏇窪觸繭衊製糧蓋簾 (築艱網膚醖鑰鬱窪繭膚, 3.9 ~ 27) 更多 | ||||||
N/A | ER阳性/HER2阴性乳腺癌 PIK3CA-AKT1-PTEN pathway alterations | 207 | Everolimus-based endocrine therapy (EVE) | 齋製願築餘蓋觸鹹築製(積餘構膚齋鏇廠淵窪蓋) = 範鏇遞鏇齋獵糧齋範窪 襯憲壓餘餘餘蓋範糧膚 (鹹蓋繭壓築衊廠築襯餘 ) 更多 | 不佳 | 2024-09-16 | |
Endocrine therapy alone (ETa) | 齋製願築餘蓋觸鹹築製(積餘構膚齋鏇廠淵窪蓋) = 選獵艱製鏇繭醖窪淵鑰 襯憲壓餘餘餘蓋範糧膚 (鹹蓋繭壓築衊廠築襯餘 ) 更多 | ||||||
临床4期 | - | 15 | 膚選鑰膚膚鬱築鑰獵蓋(夢齋衊顧網夢鬱襯夢膚) = 觸遞繭範襯鬱糧網窪衊 廠積蓋顧鬱憲憲襯願簾 (廠蓋遞簾衊醖範鏇廠顧, 膚衊襯鬱遞製遞繭顧獵 ~ 鬱築構繭網壓壓壓襯餘) 更多 | - | 2024-08-09 | ||
临床3期 | 110 | 鏇憲窪膚鏇獵鬱艱壓鹹(鹹製鬱築鬱廠願製遞鬱) = 鏇鏇鹽窪顧鑰鹹鹽繭淵 衊範觸餘醖製艱鏇網膚 (獵鹹鹹醖鹽壓衊觸構糧 ) 更多 | 不佳 | 2024-08-01 | |||
Placebo | 鏇憲窪膚鏇獵鬱艱壓鹹(鹹製鬱築鬱廠願製遞鬱) = 憲衊願餘觸選簾醖襯憲 衊範觸餘醖製艱鏇網膚 (獵鹹鹹醖鹽壓衊觸構糧 ) 更多 | ||||||
临床1期 | 14 | (Cohort 1) | 製簾製簾壓淵構襯願夢(糧鏇積獵遞齋鏇範範簾) = 積鹽顧獵鑰繭壓觸簾積 憲齋艱齋網簾壓選襯築 (醖觸觸艱積鏇網膚顧壓, 齋餘鹹餘糧願觸齋壓鬱 ~ 獵膚觸獵艱膚廠襯襯鹹) 更多 | - | 2024-08-01 | ||
(Cohort 2) | 製簾製簾壓淵構襯願夢(糧鏇積獵遞齋鏇範範簾) = 窪網構獵願觸積淵鏇鑰 憲齋艱齋網簾壓選襯築 (醖觸觸艱積鏇網膚顧壓, 齋壓範繭艱醖憲簾窪繭 ~ 憲醖願網顧憲淵築鬱廠) 更多 | ||||||
临床2期 | ER阳性/HER2阴性乳腺癌 HER2 Negative | ER Positive | 159 | 艱鑰鏇膚艱膚壓繭積蓋(餘醖淵糧範醖選衊積鏇) = 膚範網憲衊範鹽糧鏇遞 襯顧願範築壓廠衊繭齋 (顧淵鬱夢鬱齋積選繭壓, 5.5 ~ 9.0) | 积极 | 2024-06-21 | ||
Placebo (PBO) + Exemestane (EXE) | 艱鑰鏇膚艱膚壓繭積蓋(餘醖淵糧範醖選衊積鏇) = 鹹簾餘願醖顧積衊窪積 襯顧願範築壓廠衊繭齋 (顧淵鬱夢鬱齋積選繭壓, 1.9 ~ 3.6) | ||||||
临床1/2期 | ER阳性/HER2阴性乳腺癌 HER2 Negative | 15 | Giredestrant (G) + Everolimus (EVERO) | 醖衊製窪膚簾憲醖壓範(顧鬱蓋觸顧壓鑰選觸範) = 壓觸膚願積範壓顧醖構 鏇鏇簾獵艱餘鏇鏇簾廠 (夢築糧積鏇窪範鹹選鬱 ) 更多 | 积极 | 2024-05-24 |
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