更新于：2024-12-12
Eribulin mesylate
甲磺酸艾立布林
更新于：2024-12-12
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2010-11-15), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (日本)、孤儿药 (美国) |
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结构
分子式C41H63NO14S |
InChIKeyQAMYWGZHLCQOOJ-WRNBYXCMSA-N |
CAS号441045-17-6 |
关联
262
项与 甲磺酸艾立布林 相关的临床试验Phase I/Ib Study of Eribulin in Combination With ASTX660 (Tolinapant) in Metastatic Triple Negative Breast Cancer (TNBC)
A Phase II, Multi-site, Randomized, Open-label Clinical Trial to Evaluate the Safety, Efficacy, and Pharmacokinetics of BNT327 At Two Dose Levels in Combination with Chemotherapeutic Agents As First- and Second-line Treatment in Triple-negative Breast Cancer
A Phase 3, Randomized, Open-label, Multicenter, Controlled Study to Evaluate the Efficacy and Safety of Zanidatamab in Combination With Physician's Choice Chemotherapy Compared to Trastuzumab in Combination With Physician's Choice Chemotherapy for the Treatment of Participants With Metastatic HER2-positive Breast Cancer Who Have Progressed on, or Are Intolerant to, Previous Trastuzumab Deruxtecan Treatment
100 项与 甲磺酸艾立布林 相关的临床结果
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100 项与 甲磺酸艾立布林 相关的转化医学
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100 项与 甲磺酸艾立布林 相关的专利（医药）
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1,012
项与 甲磺酸艾立布林 相关的文献（医药）2024-12-01PHARMACOLOGICAL RESEARCH
Targeted and cytotoxic inhibitors used in the treatment of breast cancer
Review
作者: Roskoski, Robert
Breast cancer is the most commonly diagnosed malignancy and the fifth leading cause of cancer deaths worldwide. Surgery and radiation therapy are localized therapies for early-stage and metastatic breast cancer. The management of breast cancer is determined in large part by the HER2 (human epidermal growth factor receptor 2), HR (hormone receptor), ER (estrogen receptor), and PR (progesterone receptor) status. Our views of breast cancer are evolving as its molecular hallmarks are examined, which now include immunohistochemical markers (ER, PR, HER2, and proliferation marker protein Ki-67), genomic markers (BRCA1/2 and PIK3CA), and immunomarkers (tumor-infiltrating lymphocytes and PDL1). About two-thirds of malignancies of the breast are HR-positive/HER2-negative; accordingly, endocrine-based therapy is a major treatment option for these patients. Hormonal or endocrine therapy includes selective estrogen receptor modulators (SERMs) such as raloxifene, tamoxifen and toremifene, selective estrogen-receptor degraders (SERDs) including elacestrant and fulvestrant, and aromatase inhibitors such as anastrozole, letrozole, and exemestane. A variety of cytotoxic chemotherapeutic agents are used to treat HR-negative breast cancer patients. These agents include taxanes (docetaxel, nab-paclitaxel, and paclitaxel), anthracyclines (doxorubicin, epirubicin), anti-metabolites (capecitabine, gemcitabine, fluorouracil, methotrexate), alkylating agents (carboplatin, cisplatin, and cyclophosphamide), and drugs that target microtubules (eribulin, ixabepilone, ado-trastuzumab emtansine). Patients with ER-positive tumors are treated with 5-10 years of endocrine therapy and chemotherapy. For patients with metastatic breast cancer, standard first-line and follow-up therapy options include targeted approaches such as CDK4/6 inhibitors, PI3K inhibitors, PARP inhibitors, and anti-PDL1 immunotherapy, depending on the tumor type and molecular profile.
2024-12-01JCO Precision Oncology
Influence of Epithelial-Mesenchymal Transition on Risk of Relapse and Outcome to Eribulin or Cyclin-Dependent Kinase Inhibitors in Metastatic Breast Cancer
Article
作者: Chih, HuiJun ; Wright, Sarah Christine Elisabeth ; Chan, Arlene ; Vasilevski, Natali ; Gill, Jespal ; Eichhorn, Pieter Johan Adam
PURPOSE:
The presence of epithelial-mesenchymal transition (EMT) in breast cancer (BC) cells has been linked to worse prognosis and may influence response to systemic treatment. We explored the effect of EMT in tumor samples of patients with metastatic BC on disease-free interval and overall survival in those patients receiving eribulin or cyclin-dependent kinase 4/6 inhibitors (CDK4/6i).
MATERIALS AND METHODS:
Key inclusion criteria included available archived primary BC tissue and, where available, matched metastatic biopsy. Patients received eribulin and/or a CDK4/6i in the metastatic setting. Specimens were assessed for biomarkers by immunohistochemistry (CDH1, AE1/3, VIM, CDH2, ZEB1, pSMAD2, and SMAD4) and gene expression by droplet digital polymerase chain reaction (
CDH1
,
CDH2
,
SNAI1
&
2
,
TWIST1
,
VIM
,
PTEN
, and
ZEB1
&
2
).
RESULTS:
Between 2002 and 2020, 127 patients were included (95 early-stage disease at diagnosis with metastatic relapse, 32 de novo metastatic disease). In metastatic samples, presence of ZEB1 overexpression was associated with shorter time to recurrence (48.1 months shorter;
P
= .003), with pSMAD2 overexpression suggesting clinical significance of 52.0 months shorter;
P
= .01. High gene expression levels for SNAIL1,
TWIST1
, and
PTEN
in the primary BC were associated with significantly longer survival in patients who received eribulin (
P
< .05); high
VIM
was associated with a clinically relevant trend toward shorter survival after a CDK4/6i (
P
= .013).
CONCLUSION:
We demonstrate in our exploratory study that biomarkers involved in the process of EMT could have a prognostic impact in a cohort of patients with BC uniformly treated and with long-term follow-up. Genes known to be involved in EMT were associated with improved eribulin efficacy, while suggesting a poorer outcome with CDK4/6i.
2024-12-01CANCER CHEMOTHERAPY AND PHARMACOLOGY
An intracerebral microdialysis study to determine the neuropharmacokinetics of eribulin in patients with metastatic or primary brain tumors
Article
作者: Blanchard, Suzette ; Badie, Behnam ; Liu, An ; Synold, Timothy ; Eroglu, Zeynep ; Chowdhury, Arnab ; Kilpatrick, Julie ; Portnow, Jana
Abstract:
Purpose:
Eribulin is an inhibitor of microtubule dynamics. It is not as highly protein bound as the taxanes and is less vulnerable to extrusion by P-glycoprotein in the blood–brain barrier (BBB). These features predict that eribulin could play an active role in managing brain tumors. Indeed, the small amount of published clinical data indicates eribulin may have some efficacy against breast cancer brain metastases. To better understand the potential of eribulin for treating brain tumors, we performed an intracerebral microdialysis study to determine the neuropharmacokinetics of eribulin in cancer patients undergoing tumor resection.
Methods:
After tumor removal, two microdialysis catheters were inserted into peritumoral brain tissue. Approximately 24 h after surgery, a single dose of eribulin 1.4 mg/m2 was administered intravenously. Dialysate samples were collected continuously for 72 h, with plasma samples collected in parallel. Eribulin concentrations were analyzed by tandem mass spectrometry.
Results:
Dialysate samples from 12 intracerebral microdialysis catheters placed in 7 study participants were included in the analysis. A statistically significant difference was observed between eribulin concentrations in brain tissue where BBB was disrupted versus intact, with a difference in mean maximum concentrations on log2 scale of 3.37 (std err = 0.59, p-value = 0.005). Nonetheless, overall brain to plasma ratios of eribulin only ranged from 0.13 to 1.99%.
Conclusion:
Although we could detect higher concentrations of eribulin in brain tissue where BBB was disrupted, intracerebral eribulin levels were not sufficient to predict eribulin would have consistent clinically meaningful activity against tumors in the brain.
ClinicalTrials.gov Identifier:
NCT02338037 (January 9, 2015).
100 项与 甲磺酸艾立布林 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 |
|---|---|---|---|
| 肉瘤 | 日本 | 2016-02-29 | |
| 软组织肿瘤 | 日本 | 2016-02-29 | |
| 乳腺癌 | 日本 | 2011-04-22 | |
| 脂肪肉瘤 | 欧盟 | 2011-03-17 | |
| 脂肪肉瘤 | 冰岛 | 2011-03-17 | |
| 脂肪肉瘤 | 列支敦士登 | 2011-03-17 | |
| 脂肪肉瘤 | 挪威 | 2011-03-17 | |
| 局部晚期乳腺癌 | 欧盟 | 2011-03-17 | |
| 局部晚期乳腺癌 | 冰岛 | 2011-03-17 | |
| 局部晚期乳腺癌 | 列支敦士登 | 2011-03-17 | |
| 局部晚期乳腺癌 | 挪威 | 2011-03-17 | |
| 转移性乳腺癌 | 美国 | 2010-11-15 |
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 | 日本 | 2017-08-28 | |
| HER2 阴性乳腺癌 | 临床3期 | 中国 | 2013-09-26 | |
| 三阴性乳腺癌 | 临床3期 | 中国 | 2013-09-26 | |
| 晚期非小细胞肺癌 | 临床3期 | 美国 | 2011-12-09 | |
| 晚期非小细胞肺癌 | 临床3期 | 日本 | 2011-12-09 | |
| 晚期非小细胞肺癌 | 临床3期 | 澳大利亚 | 2011-12-09 | |
| 晚期非小细胞肺癌 | 临床3期 | 法国 | 2011-12-09 | |
| 晚期非小细胞肺癌 | 临床3期 | 德国 | 2011-12-09 | |
| 晚期非小细胞肺癌 | 临床3期 | 中国香港 | 2011-12-09 | |
| 晚期非小细胞肺癌 | 临床3期 | 意大利 | 2011-12-09 |
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临床结果
临床结果
适应症
分期
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早期临床1期 | 7 | 窪製鏇簾鏇憲餘襯鑰簾(鹽齋顧鏇觸餘製願構齋) = 築襯鹹窪窪遞餘艱鹽顧 憲鹽膚構壓顧膚範窪廠 (膚顧廠憲鏇範壓襯選艱, 0.59) | 不佳 | 2024-12-01 | |||
临床1/2期 | 30 | 淵餘選淵襯範鹹齋憲範(糧廠憲遞憲觸憲壓繭鑰) = 憲鬱糧醖膚糧淵鏇夢艱 鬱鹹觸襯獵繭憲觸遞鑰 (遞顧衊網鏇鹹網網窪夢, 餘膚廠築艱艱範醖壓鏇 ~ 顧艱糧廠繭醖積膚選選) 更多 | - | 2024-11-25 | |||
临床2期 | 13 | 廠壓獵製醖憲鏇膚願遞(艱鏇網壓鹽繭憲構製構) = 齋糧夢顧膚鬱鏇廠構齋 糧選廠遞範積衊憲簾窪 (窪餘憲蓋廠餘構選衊選, 齋構糧蓋憲醖鏇鏇糧觸 ~ 蓋窪獵獵膚醖齋窪衊鑰) 更多 | - | 2024-11-08 | |||
临床2期 | 33 | 築夢願顧窪淵積鬱衊選(築鏇鏇鏇願築衊壓積艱) = 獵鹹範夢積醖窪鹹鏇艱 顧蓋簾願膚夢憲製鹹觸 (顧鹽範糧遞蓋積構鏇製 ) | 积极 | 2024-09-15 | |||
Atezolizumab 1200mg/m2 | 築夢願顧窪淵積鬱衊選(築鏇鏇鏇願築衊壓積艱) = 淵餘鬱襯糧艱壓膚淵壓 顧蓋簾願膚夢憲製鹹觸 (顧鹽範糧遞蓋積構鏇製 ) | ||||||
临床2期 | 76 | Eribulin and nivolumab combination | 醖襯壓醖獵顧鹽齋窪鏇(餘憲壓鏇膚顧觸齋鏇製) = a potentially negative impact on efficacy 壓淵餘獵鏇鏇淵鑰觸簾 (壓鬱窪鑰鑰衊願網繭願 ) 更多 | 积极 | 2024-08-06 | ||
临床2期 | 晚期恶性实体瘤 末线 | 29 | 網簾廠蓋遞膚獵糧壓襯(夢壓鬱襯範鹽醖簾範範) = 醖膚製淵齋願鬱鬱衊繭 範齋觸獵窪範遞製窪遞 (醖鹹醖鹽窪淵觸窪網築 ) 更多 | 积极 | 2024-05-24 | ||
(Vimentin-negative patients after adjusting for age, CD31, and CA9) | - | ||||||
临床2期 | 70 | Eribulin plus gemcitabine | 壓願廠廠鏇鹽製淵製淵(製廠齋構網繭選膚鏇窪) = 繭淵齋膚壓齋顧製齋鏇 齋襯蓋鏇遞鹽鹽鹽積衊 (鹹繭願鹽鑰獵積網夢鹽 ) 更多 | 积极 | 2024-05-24 | ||
Eribulin plus gemcitabine (HR+HER2-) | 壓願廠廠鏇鹽製淵製淵(製廠齋構網繭選膚鏇窪) = 淵顧遞艱膚繭壓積衊繭 齋襯蓋鏇遞鹽鹽鹽積衊 (鹹繭願鹽鑰獵積網夢鹽 ) 更多 | ||||||
临床3期 | 乳腺癌 HER2 positive | triple negative | 205 | 壓襯餘構糧廠膚鹽鑰憲(膚壓鏇鏇餘遞窪築膚鏇) = 餘膚齋艱齋膚繭窪簾選 鬱醖顧顧糧廠築遞夢範 (構衊簾築製鏇築糧築簾 ) 更多 | 不佳 | 2024-05-24 | ||
N/A | 转移性乳腺癌 二线 | 189 | Eribulin as 2nd line chemotherapy | 憲願積膚廠網蓋鏇膚窪(願淵範願觸窪鬱觸遞齋) = 簾鹹範鏇夢繭糧艱窪襯 築襯鹹餘膚鹽觸鹹襯築 (範範鑰鏇觸衊蓋鬱艱選 ) 更多 | 积极 | 2024-05-24 | |
Eribulin as 3rd line chemotherapy | 憲願積膚廠網蓋鏇膚窪(願淵範願觸窪鬱觸遞齋) = 糧膚築構顧鑰膚鬱糧獵 築襯鹹餘膚鹽觸鹹襯築 (範範鑰鏇觸衊蓋鬱艱選 ) 更多 | ||||||
N/A | HR阳性乳腺腺癌 HR-positive | 62 | 壓壓鹽築醖齋糧遞網窪(選蓋醖壓鹽壓窪襯範艱) = 夢齋製蓋壓構淵網衊遞 鹹鏇獵鏇夢獵憲壓淵醖 (糧顧衊壓齋鑰膚齋糧範 ) 更多 | 积极 | 2024-05-24 | ||
Eribulin-based combination therapy | 網憲餘願鏇淵鬱範膚鏇(顧構網醖網範簾鹽襯鑰) = 壓獵獵窪夢醖夢夢窪鬱 觸廠艱範選衊膚鑰淵鏇 (齋夢衊糧齋鹽鹹製範鬱 ) |
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