Division of Hematology and Oncology, University Hospitals Cleveland Medical Center, Cleveland, OH, 44106, USA.
Case Comprehensive Cancer Center, Case Western Reserve University, Cleveland, OH, 44106, USA.
Invest New Drugs. 2018 Jun;36(3):435-441. doi: 10.1007/s10637-017-0515-3. Epub 2017 Oct 2.
Introduction Preclinical data suggest quinacrine acts as an inhibitor of FACT (facilitates chromatin transcription) complex, which may play a role in TKI (tyrosine kinase inhibitor) resistance. The aim of this Phase I study was to study the safety and assess the maximum tolerated dose of quinacrine in combination with erlotinib in non small cell lung cancer (NSCLC). Methods This was a phase I study with standard 3 + 3 dose escalation design with the primary aim of determining the maximum tolerated dose. Two of 3 patients enrolled at dose level 1 experienced dose limiting toxicity (DLT). The next 6 patients were enrolled at dose level - 1 and none of these 6 patients experienced DLT. The dose of 50 mg of quinacrine every other day with 150 mg of erlotinib was established as the maximum tolerated and the recommended phase II dose. One of 3 patients treated at dose level 1 had stable disease. One of 6 patients treated at dose level - 1 had partial response for 6 months, the rest had progressive disease at the time of first assessment. Conclusion Combination of quinacrine and erlotinib was well tolerated but showed limited efficacy in advanced NSCLC.
简介
临床前数据表明,吖啶酮可作为 FACT(促进染色质转录)复合物的抑制剂,这可能在 TKI(酪氨酸激酶抑制剂)耐药中发挥作用。本 I 期研究旨在研究吖啶酮联合厄洛替尼治疗非小细胞肺癌(NSCLC)的安全性和评估最大耐受剂量。
方法
这是一项 I 期研究,采用标准的 3+3 剂量递增设计,主要目的是确定最大耐受剂量。在剂量水平 1 入组的 3 例患者中有 2 例出现剂量限制毒性(DLT)。接下来的 6 例患者入组剂量水平-1,这 6 例患者均未出现 DLT。确定 50mg 吖啶酮每两天一次联合 150mg 厄洛替尼作为最大耐受剂量和推荐的 II 期剂量。在剂量水平 1 治疗的 3 例患者中有 1 例病情稳定。在剂量水平-1 治疗的 6 例患者中有 1 例部分缓解 6 个月,其余患者在首次评估时病情进展。
结论
吖啶酮联合厄洛替尼耐受性良好,但在晚期 NSCLC 中的疗效有限。