Department of Pharmacology and Toxicology, Dartmouth Medical School, Hanover, NH, USA.
Chemotherapy. 2012;58(4):321-9. doi: 10.1159/000343165. Epub 2012 Nov 12.
ABT-751 is a novel antimitotic agent that exerted cytotoxic effects in preclinical studies. Carboplatin has efficacy in treating advanced non-small cell lung cancer (NSCLC) in combination with other drugs.
Lung cancer cell lines were treated with ABT-751 and/or carboplatin to investigate their impact on cell growth. A phase I study with an expansion cohort was conducted in previously treated NSCLC patients. The primary objective was the maximum tolerated dose (MTD); secondary objectives were objective response rates, median survival, time to tumor progression, dose-limiting toxicities (DLTs), and pharmacodynamic evaluation of buccal swabs.
Combining ABT-751 with carboplatin significantly reduced growth and induced apoptosis of lung cancer cell lines. Twenty advanced NSCLC patients were enrolled. MTD was ABT-751 125 mg orally twice daily for 7 days with carboplatin AUC 6. DLTs included fatigue, ileus, neutropenia and pneumonitis. Two patients had confirmed partial responses. Median overall survival was 11.7 months (95% CI 5.9-27.0). Time to tumor progression was 2.8 months (95% CI 2.0-2.7). Four of 6 patients showed decreased cyclin D1 protein in posttreatment versus pretreatment buccal swabs.
Combining ABT-751 with carboplatin suppressed growth of lung cancer cell lines and had modest clinical antitumor activity in advanced NSCLC previously treated predominantly with carboplatin. Further studies of this combination are not recommended while investigations of biomarkers in different patient populations, alternative schedules and combinations may be pursued.
ABT-751 是一种新型的抗有丝分裂药物,在临床前研究中显示出细胞毒性作用。卡铂与其他药物联合治疗晚期非小细胞肺癌(NSCLC)具有疗效。
用 ABT-751 和/或卡铂处理肺癌细胞系,以研究它们对细胞生长的影响。对先前治疗的 NSCLC 患者进行了 I 期研究,其中包括扩展队列。主要目的是最大耐受剂量(MTD);次要目标是客观缓解率、中位生存期、肿瘤进展时间、剂量限制性毒性(DLTs)和口腔拭子的药效学评估。
ABT-751 与卡铂联合使用可显著降低肺癌细胞系的生长并诱导其凋亡。共纳入 20 例晚期 NSCLC 患者。MTD 为口服 ABT-751,每日 2 次,每次 125mg,连用 7 天,卡铂 AUC 为 6。DLTs 包括疲劳、肠梗阻、中性粒细胞减少和肺炎。2 例患者有确认的部分缓解。中位总生存期为 11.7 个月(95%CI 5.9-27.0)。肿瘤进展时间为 2.8 个月(95%CI 2.0-2.7)。6 例患者中有 4 例在治疗后与治疗前的口腔拭子中显示出 cyclin D1 蛋白减少。
ABT-751 与卡铂联合使用可抑制肺癌细胞系的生长,并在先前主要用卡铂治疗的晚期 NSCLC 患者中具有适度的临床抗肿瘤活性。不建议进一步研究该联合用药,而可继续研究不同患者人群的生物标志物、替代方案和联合用药。