Kim Hyo Song, Kim Sung-Moo, Kim Hyunki, Pyo Kyoung-Ho, Sun Jong-Mu, Ahn Myung-Ju, Park Keunchil, Keam Bhumsuk, Kwon Nak-Jung, Yun Hwan Jung, Kim Hoon-Gu, Chung Ik-Joo, Lee Jong Seok, Lee Kyung Hee, Kim Dae Joon, Lee Chang-Geol, Hur Jin, Chung Hyunsoo, Park Jun Chul, Shin Sung Kwan, Lee Sang Kil, Kim Hye Ryun, Moon Yong Wha, Lee Yong Chan, Kim Joo Hang, Paik Soonmyung, Cho Byoung Chul
Division of Medical Oncology, Department of Internal Medicine, Yonsei Cancer Center, Yonsei University College of Medicine, Seoul, Korea.
Yonsei Cancer Research Institute, JE-UK Laboratory of Molecular Cancer Therapeutics, Seoul, Korea.
Oncotarget. 2015 Dec 29;6(42):44971-84. doi: 10.18632/oncotarget.6056.
The purpose of this study was to investigate the clinical activity, safety and predictive biomarkers of dacomitinib, an irreversible pan-HER inhibitor, in patients with recurrent or metastatic esophageal squamous cell carcinoma (R/M-ESCC). Patients, whose diseases were not amenable to curative treatment and had progressed on platinum-based chemotherapy, were treated with dacomitinib 45 mg/day. The primary endpoint was objective response rate by RECISTv 1.1. Predictive biomarker analyses included the characterization of somatic mutations and gene expression using the Ion Torrent AmpliSeq Cancer Hotspot Panel and Nanostring nCounter, and investigation of their relationship with clinical outcomes. Of the 48 evaluable patients, 6 (12.5%) achieved partial responses and 29 (60.4%) had stable disease. The median response duration was 7.1 months. The median progression free survival (PFS) and overall survival (OS) was 3.3 months (95% CI, 2.4-4.3 months) and 6.4 months (95% CI, 4.4-8.4 months). Adverse events were mostly grade 1-2. Gene set enrichment analysis revealed that ERBB signaling pathway is significantly enriched in patients with PFS ≥ 4 months (n = 12) than PFS < 4 months (n = 21) (p < 0.001). Upregulation of ERBB signaling pathway was significantly associated with longer PFS (5.0 vs. 2.9 months, P = 0.016) and OS (10.0 vs. 4.8 months, P = 0.022). The most frequent mutations were TP53 (61%) followed by CDKN2A (8%), MLH1 (8%), FLT3 (8%) and EGFR (8%). Dacomitinib demonstrated clinical efficacy with manageable toxicity in platinum-failed R/M-ESCC. Screening of ERBB pathway-related gene expression profiles may help identify patients who are most likely benefit from dacomitinib.
本研究旨在探讨不可逆泛HER抑制剂达可替尼在复发或转移性食管鳞状细胞癌(R/M-ESCC)患者中的临床活性、安全性及预测生物标志物。疾病无法进行根治性治疗且铂类化疗进展的患者,接受每日45mg达可替尼治疗。主要终点为依据RECISTv 1.1标准的客观缓解率。预测生物标志物分析包括使用Ion Torrent AmpliSeq癌症热点 panel和Nanostring nCounter对体细胞突变和基因表达进行表征,并研究它们与临床结局的关系。48例可评估患者中,6例(12.5%)获得部分缓解,29例(60.4%)疾病稳定。中位缓解持续时间为7.1个月。中位无进展生存期(PFS)和总生存期(OS)分别为3.3个月(95%CI,2.4 - 4.3个月)和6.4个月(95%CI,4.4 - 8.4个月)。不良事件大多为1 - 2级。基因集富集分析显示,与PFS<4个月(n = 21)的患者相比,PFS≥4个月(n = 12)的患者中ERBB信号通路显著富集(p<0.001)。ERBB信号通路的上调与更长的PFS(5.0 vs. 2.9个月,P = 0.016)和OS(10.0 vs. 4.8个月,P = 0.022)显著相关。最常见的突变是TP53(61%),其次是CDKN2A(8%)、MLH1(8%)、FLT3(8%)和EGFR(8%)。达可替尼在铂类治疗失败的R/M-ESCC中显示出临床疗效且毒性可控。筛查ERBB通路相关基因表达谱可能有助于识别最可能从达可替尼治疗中获益的患者。