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艾立布林。

Eribulin.

机构信息

Adis, a Wolters Kluwer Business, Auckland, New Zealand.

出版信息

Drugs. 2011 Jul 9;71(10):1321-31. doi: 10.2165/11207520-000000000-00000.

DOI:10.2165/11207520-000000000-00000
PMID:21770478
Abstract

Eribulin (eribulin mesylate) is a non-taxane microtubule dynamics inhibitor with tubulin-based antimitotic activity and chemotherapeutic effects. Eribulin is used in the treatment of patients with locally advanced or metastatic breast cancer who have previously been treated with at least two chemotherapeutic regimens, including an anthracycline and a taxane. In in vitro studies, eribulin displayed antiproliferative activity against human breast cancer cell lines. Regression and elimination of breast tumours were observed in human tumour xenograft models. In the randomized, open-label, multinational, phase III EMBRACE trial in patients with locally recurrent or metastatic breast cancer, median overall survival was significantly longer in patients who received intravenous eribulin (n = 508) [13.1 months] compared with that in patients who received a treatment of physician's choice (n = 254) [10.6 months; hazard ratio 0.81; 95% CI 0.66, 0.99; p = 0.041]. Prior to enrolment, study participants had received between two and five chemotherapeutic regimens, including an anthracycline and a taxane. Consistent with the findings of earlier phase I and II trials, eribulin was reported to have a manageable tolerability profile in the EMBRACE trial. Peripheral neuropathy (incidence 5%) was the most common adverse event resulting in the discontinuation of eribulin treatment. The most common grade 3/4 adverse events in the eribulin group were neutropenia, leukopenia and asthenia or fatigue.

摘要

艾立布林(盐酸艾立布林)是一种非紫杉烷类微管动力学抑制剂,具有基于微管的抗有丝分裂活性和化疗作用。艾立布林用于治疗先前接受过至少两种化疗方案(包括蒽环类药物和紫杉烷类药物)治疗的局部晚期或转移性乳腺癌患者。在体外研究中,艾立布林对人乳腺癌细胞系显示出抗增殖活性。在人肿瘤异种移植模型中观察到乳腺肿瘤的消退和消除。在局部复发或转移性乳腺癌的随机、开放标签、多中心、III 期 EMBRACE 试验中,接受静脉注射艾立布林(n = 508)的患者中位总生存期明显长于接受医生选择治疗(n = 254)的患者[13.1 个月比 10.6 个月;风险比 0.81;95%CI 0.66,0.99;p = 0.041]。入组前,研究参与者接受了 2 至 5 种化疗方案,包括蒽环类药物和紫杉烷类药物。与早期 I 期和 II 期试验的结果一致,在 EMBRACE 试验中,艾立布林被报道具有可管理的耐受性。周围神经病变(发生率为 5%)是导致艾立布林治疗中断的最常见不良事件。艾立布林组最常见的 3/4 级不良事件是中性粒细胞减少、白细胞减少和乏力或疲劳。

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2
Eribulin monotherapy versus treatment of physician's choice in patients with metastatic breast cancer (EMBRACE): a phase 3 open-label randomised study.艾立布林单药治疗与医生选择的治疗方案用于转移性乳腺癌患者(EMBRACE):一项开放标签、3 期随机研究。
Lancet. 2011 Mar 12;377(9769):914-23. doi: 10.1016/S0140-6736(11)60070-6. Epub 2011 Mar 2.
3
Global cancer statistics.
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Acta Neuropathol Commun. 2023 Nov 27;11(1):187. doi: 10.1186/s40478-023-01685-9.
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Eribulin normalizes pancreatic cancer-associated fibroblasts by simulating selected features of TGFβ inhibition.表柔比星通过模拟 TGFβ 抑制的某些特征使胰腺癌相关成纤维细胞正常化。
BMC Cancer. 2022 Dec 2;22(1):1255. doi: 10.1186/s12885-022-10330-y.
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Breaking the Bottleneck in Anticancer Drug Development: Efficient Utilization of Synthetic Biology.突破抗癌药物研发瓶颈:合成生物学的高效利用。
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