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Lurbinectedin

肿瘤

关键词肿瘤 药物 小细胞肺癌

词汇介绍

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解析

Lurbinectedin 

释    义   n. 一种抗癌药物,是海鞘素衍生物,属于RNA聚合酶Ⅱ抑制剂。

例    句   This manuscript describes the efficacy and safety of doxorubicin and lurbinectedin in a subgroup of 27 patients with relapsed SCLC from a phase I trial. 本文描述了阿霉素和lurbinectedin对27例复发性小细胞肺癌I期临床试验的疗效和安全性。

概述

Lurbinectedin(PM1183)是由PharmaMar公司研发的,是海鞘素衍生物,属于RNA聚合酶Ⅱ抑制剂,可选择性地抑制反式激活的RNA聚合酶Ⅱ介导的转录过程,对RNA聚合酶Ⅰ和线粒体RNA聚合酶活性无影响,也不影响mRNA正常转录过程。lubrinectedin的作用机理是与 DNA 双螺旋结构上的小沟相结合,使得肿瘤细胞在有丝分裂过程中畸变、凋亡、最终减少细胞增殖。在有些癌症种类中,癌症细胞依靠高速运转的转录过程支持它们的增殖,这些肿瘤细胞对lurbinectedin尤为敏感

Antitumor activity of lurbinectedin (PM01183) and doxorubicin in relapsed small-cell lung cancer: results from a phase I study复制标题

Lurbinectedin (PM01183) 和阿霉素在复发性小细胞肺癌中的抗肿瘤活性: I期研究结果

发表时间:2017-10-01

影响因子:14.2

作者: E. Calvo

期刊:Ann. Oncol

Lurbinectedin (PM01183) has synergistic antitumor activity when combined with doxorubicin in mice with xenografted tumors. This phase I trial determined the recommended dose (RD) of doxorubicin (bolus) and PM01183 (1-h intravenous infusion) on day 1 every 3 weeks (q3wk), and obtained preliminary evidence of antitumor activity for this combination in small-cell lung cancer (SCLC). Patients with advanced solid tumors received doxorubicin and PM01183 following a standard dose escalation design and expansion at the RD. Twenty-seven patients had relapsed SCLC: 12 with sensitive disease (platinum-free interval ≥90 days) and 15 with resistant disease (platinum-free interval <90 days). RESULTS: Doxorubicin 50 mg/m2 and PM01183 4.0 mg flat dose was the RD. In relapsed SCLC, treatment tolerance at the RD was manageable. Transient and reversible myelosuppression (including neutropenia, thrombocytopenia, and febrile neutropenia) was the main toxicity, managed with dose adjustment and colony-stimulating factors. Fatigue (79%), nausea/vomiting (58%), decreased appetite (53%), mucositis (53%), alopecia (42%), diarrhea/constipation (42%), and asymptomatic creatinine (68%) and transaminase increases (alanine aminotransferase 42%; aspartate aminotransferase 32%) were common, and mostly mild or moderate. Complete (n = 2, 8%) and partial response (n = 13, 50%) occurred in relapsed SCLC, mostly at the RD.

译文

Lurbinectin(PM01183)与多柔比星联用在患有异种移植肿瘤的小鼠中具有协同抗肿瘤活性。这项第一阶段试验每3周(q3wk)第1天确定阿霉素(推注)和PM01183(1-h静脉输注)的推荐剂量(RD),并获得此组合在小细胞肺中的抗肿瘤活性的初步证据癌症(SCLC)。患有晚期实体瘤的患者在标准剂量递增设计和RD扩展后接受了阿霉素和PM01183。二十七例SCLC复发:12例患有敏感疾病(无铂间隔≥90天),15例患有耐药性疾病(无铂间隔≤90天)。结果:阿霉素50μg/ m2和PM01183±4.0μmg单位剂量为RD。在复发性SCLC中,RD的治疗耐受性是可以控制的。短暂和可逆的骨髓抑制(包括嗜中性白血球减少症,血小板减少症和发热性嗜中性白血球减少症)是主要的毒性反应,可通过剂量调整和集落刺激因子来控制。疲劳(79%),恶心/呕吐(58%),食欲下降(53%),粘膜炎(53%),脱发(42%),腹泻/便秘(42%)和无症状的肌酐(68%)和转氨酶增加(丙氨酸氨基转移酶42%;天冬氨酸氨基转移酶32%)是常见的,且多数为轻度或中度。在复发的SCLC中发生完全反应(n = 2,8%)和部分反应(n = 13,50%),大部分发生在RD。