Zhen David B, Griffith Kent A, Ruch Joshua M, Camphausen Kevin, Savage Jason E, Kim Edward J, Sahai Vaibhav, Simeone Diane M, Zalupski Mark M
Division of Hematology/Oncology, Department of Internal Medicine, University of Michigan, 3-219 CC, 1500 E Medical Center Dr., SPC 5934, Ann Arbor, MI, 48109-5934, USA.
Department of Biostatistics, University of Michigan, Ann Arbor, MI, USA.
Invest New Drugs. 2016 Dec;34(6):733-739. doi: 10.1007/s10637-016-0376-1. Epub 2016 Jul 21.
Background Cabozantinib and gemcitabine improve tumor control in pancreatic ductal adenocarcinoma (PDAC) in preclinical models through c-Met inhibition. We sought to determine the maximum tolerated dose (MTD) of this combination in patients with advanced PDAC. Methods Patients with ≤1 prior treatment and adequate performance status were eligible. Cabozantinib was given orally once daily, beginning day (-)7 and continued with gemcitabine given intravenously on days 1, 8, and 15 every 28 days. Dose level was assigned using Time to Event Continual Reassessment Method (TITE-CRM). Primary endpoint was MTD, defined as the highest dose level at which ≤25 % of patients incurred a dose-limiting toxicity (DLT). Secondary endpoints included response rate, progression-free survival (PFS), overall survival (OS) and urinary biomarker assessment. Results Twelve patients were enrolled and treated with 10 patients evaluable for DLT. The probability of DLT was >25 % for all dose levels tested, and thus an MTD was not determined. DLTs included grade 3 ALT/AST elevations and thrombocytopenia. Three patients had partial responses, but each discontinued therapy due to toxicity. Median PFS and OS were 4.7 (95 % CI: 1.4-9.7) and 10.1 months (95 % CI: 3.6-20.6). Exploratory biomarker analysis showed correlation of c-Met and VEGF levels with response. Conclusions An MTD for the combination was not established. Cabozantinib and gemcitabine appear impractical for further development due to DLT at low doses and continuing toxicities with ongoing therapy. Acknowledging the small sample size, responses were seen suggesting further investigation of c-Met inhibition in PDAC may be warranted.
在临床前模型中,卡博替尼和吉西他滨通过抑制c-Met改善胰腺导管腺癌(PDAC)的肿瘤控制。我们试图确定这种联合用药方案在晚期PDAC患者中的最大耐受剂量(MTD)。方法:既往接受治疗≤1次且体能状态良好的患者符合入组条件。卡博替尼从第(-)7天开始每日口服一次,并持续联合吉西他滨,每28天的第1、8和15天静脉给药。剂量水平采用事件时间连续重新评估法(TITE-CRM)确定。主要终点是MTD,定义为≤25%的患者发生剂量限制性毒性(DLT)的最高剂量水平。次要终点包括缓解率、无进展生存期(PFS)、总生存期(OS)和尿液生物标志物评估。结果:12例患者入组并接受治疗,其中10例可评估DLT。所有测试剂量水平的DLT发生率均>25%,因此未确定MTD。DLT包括3级谷丙转氨酶/谷草转氨酶升高和血小板减少。3例患者出现部分缓解,但均因毒性而停药。中位PFS和OS分别为4.7个月(95%CI:1.4 - 9.7)和10.1个月(95%CI:3.6 - 20.6)。探索性生物标志物分析显示c-Met和VEGF水平与缓解相关。结论:未确定该联合用药方案的MTD。由于低剂量时出现DLT以及持续治疗存在毒性,卡博替尼和吉西他滨进一步开发似乎不切实际。考虑到样本量小,观察到有缓解情况,提示可能有必要进一步研究PDAC中c-Met抑制作用。