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一项贝洛替康(一种新型喜树碱类似物)治疗未经治疗的广泛期老年小细胞肺癌患者的多中心 II 期研究。

A multicenter phase II study of belotecan, a new camptothecin analogue, in elderly patients with previously untreated, extensive-stage small cell lung cancer.

机构信息

Division of Pulmonology, Department of Internal Medicine, Uijeongbu St. Mary's Hospital, The Catholic University of Korea, Uijeongbu, Republic of Korea.

出版信息

Cancer Chemother Pharmacol. 2013 Oct;72(4):809-14. doi: 10.1007/s00280-013-2256-0. Epub 2013 Aug 6.

DOI:10.1007/s00280-013-2256-0
PMID:23918044
Abstract

PURPOSE

Belotecan is a new camptothecin analogue and a potent topoisomerase I inhibitor. The aim of this phase II study was to investigate the efficacy and toxicity of belotecan in previously untreated elderly patients with small cell lung cancer (SCLC).

METHODS

A total of 26 patients, aged ≥65 years, with previously untreated, extensive-stage SCLC were enrolled in the study. Belotecan was administered by daily intravenous infusion at 0.5 mg/m(2)/day for 5 consecutive days every 3 weeks.

RESULTS

The overall response rate and disease control rate of chemotherapy on an intention-to-treat basis were 35 and 54 %, respectively. The median overall survival was 6.4 months, and the median time to progression was 2.8 months. The most common toxicity was hematologic. Grade 3 or 4 neutropenia occurred in 80.8 % of patients, and grade 3 or 4 thrombocytopenia in 15.3 %. Non-hematologic toxic effects of grade 3 or 4 were uncommon.

CONCLUSION

Belotecan had modest efficacy and well-tolerated toxicity in previously untreated, elderly SCLC patients. Single belotecan could be a promising treatment option, considering its lower toxicity in elderly patients who are unsuitable candidates for platinum plus etoposide chemotherapy.

摘要

目的

贝洛替康是一种新型喜树碱类似物,也是一种有效的拓扑异构酶 I 抑制剂。本 II 期研究旨在评估贝洛替康在未经治疗的老年广泛期小细胞肺癌(SCLC)患者中的疗效和毒性。

方法

共纳入 26 例年龄≥65 岁、未经治疗的广泛期 SCLC 患者,接受贝洛替康 0.5mg/m²/日静脉滴注,连续 5 天,每 3 周 1 次。

结果

根据意向治疗原则,化疗的总缓解率和疾病控制率分别为 35%和 54%。中位总生存期为 6.4 个月,中位无进展生存期为 2.8 个月。最常见的毒性是血液学毒性。80.8%的患者发生 3 或 4 级中性粒细胞减少症,15.3%的患者发生 3 或 4 级血小板减少症。非血液学毒性的 3 或 4 级不良反应不常见。

结论

贝洛替康在未经治疗的老年 SCLC 患者中具有一定的疗效,且毒性可耐受。考虑到老年患者对铂类加依托泊苷化疗不耐受,贝洛替康的低毒性可能使其成为一种有前途的治疗选择。

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Camptothecin (CPT) and its derivatives are known to target topoisomerase I (Top1) as their mechanism of action: did we miss something in CPT analogue molecular targets for treating human disease such as cancer?
喜树碱(CPT)及其衍生物已知以拓扑异构酶I(Top1)为作用靶点:在用于治疗癌症等人类疾病的喜树碱类似物分子靶点方面,我们是否遗漏了什么?
Am J Cancer Res. 2017 Dec 1;7(12):2350-2394. eCollection 2017.