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一项评估 MET 抑制剂卡马替尼联合西妥昔单抗治疗抗 EGFR 单克隆抗体治疗后进展的 MET 阳性结直肠癌患者的 1b 期研究。

A phase 1b study of the MET inhibitor capmatinib combined with cetuximab in patients with MET-positive colorectal cancer who had progressed following anti-EGFR monoclonal antibody treatment.

机构信息

Department of Medical Oncology, Institut Universitaire du Cancer de Toulouse (IUCT) - Oncopole, 1 avenue Irène Joliot-Curie, 31059, Toulouse Cedex 9, France.

Gastrointestinal Malignancies Division, Vall d'Hebron University Hospital, Barcelona, Spain.

出版信息

Invest New Drugs. 2020 Dec;38(6):1774-1783. doi: 10.1007/s10637-020-00928-z. Epub 2020 May 14.

DOI:10.1007/s10637-020-00928-z
PMID:32410080
Abstract

Background Overcoming resistance to anti-epidermal growth factor receptor (EGFR) monoclonal antibodies (mAbs) in patients with KRAS wildtype (WT) metastatic colorectal cancer (mCRC) could help meet the needs of patients with limited treatment options. Methods In this phase 1b study, patients with N/KRAS WT, MET-positive mCRC who had progressed following anti-EGFR mAb treatment received escalating oral doses of capmatinib (150, 300, and 400 mg) twice daily plus weekly intravenous cetuximab (at the approved dose). The primary objective was to establish a recommended dose for expansion (RDE) of capmatinib in combination with cetuximab. Safety, preliminary activity, pharmacokinetics, and pharmacodynamics were also explored. Results Thirteen patients were enrolled. No patients experienced a dose-limiting toxicity at investigated doses; the RDE was established as capmatinib 400 mg twice daily plus cetuximab. All patients experienced adverse events (AEs) suspected to be related to the study treatment. Five patients (38.5%) reported study-drug-related AEs of grade 3/4 in severity. No patients achieved a complete or partial response according to RECIST v1.1; however, tumor shrinkage of 29-44% was observed in 4 patients. Conclusions Capmatinib plus cetuximab was well tolerated. Preliminary signs of activity were observed. Further investigation is warranted to obtain efficacy data and refine predictive biomarkers of response. Clinical trial registration NCT02205398.

摘要

背景

克服 KRAS 野生型(WT)转移性结直肠癌(mCRC)患者对表皮生长因子受体(EGFR)单克隆抗体(mAb)的耐药性,可以满足治疗选择有限的患者的需求。

方法

在这项 1b 期研究中,既往接受抗 EGFR mAb 治疗后进展的 N/KRAS WT、MET 阳性 mCRC 患者接受卡马替尼(150、300 和 400 mg,每日两次)和每周一次静脉注射西妥昔单抗(批准剂量)递增口服剂量。主要目的是确定卡马替尼联合西妥昔单抗扩展入组(RDE)的推荐剂量。还探索了安全性、初步疗效、药代动力学和药效学。

结果

共纳入 13 例患者。在研究剂量下,无患者发生剂量限制性毒性;确定卡马替尼 400 mg,每日两次联合西妥昔单抗为 RDE。所有患者均发生疑似与研究治疗相关的不良事件(AE)。5 例(38.5%)患者报告有 3/4 级研究药物相关 AE。根据 RECIST v1.1 标准,无患者完全或部分缓解;但 4 例患者的肿瘤缩小 29-44%。

结论

卡马替尼联合西妥昔单抗耐受性良好。观察到初步疗效迹象。需要进一步研究以获得疗效数据并完善反应的预测生物标志物。

临床试验注册

NCT02205398。

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