Department of Gastrointestinal Oncology, National Cancer Center Hospital East, 6-5-1, Kashiwanoha, Kashiwa, Chiba, 277-8577, Japan.
Department of Gastrointestinal Medical Oncology, National Cancer Center Hospital, Chuo-ku, Tokyo, Japan.
Esophagus. 2022 Oct;19(4):702-710. doi: 10.1007/s10388-022-00928-3. Epub 2022 Jul 29.
PI3K/AKT/mTOR pathway is frequently overactive in esophageal squamous cell carcinoma (ESCC), making it an attractive treatment target. BKM120 is an oral pan-class I PI3K inhibitor with promising activity in several cancers. We prospectively investigated efficacy, safety, and biomarkers of BKM120 in advanced ESCC. We conducted a multicenter phase II study of BKM120 monotherapy in patients with pretreated advanced ESCC.
BKM120 (100 mg/day) was administered orally in a 28-day cycle. The primary end point was disease control rate (DCR). Tumor samples for all patients were collected for gene alteration analysis in a comprehensive genomic profiling assay.
Of 42 patients enrolled, 20 had stable disease and two had confirmed partial response. One ineligible patient was excluded from the primary analysis, which met the primary end point (DCR 51.2%; 95% confidence interval [CI], 35.1-67.1). In the 42 patients, median progression-free survival and overall survival were 2.3 (95% CI 1.8-3.2) and 9.0 (95% CI 6.5-11.4) months, respectively. Common grade 3 or 4 adverse events were rash, anorexia, hyponatremia, and abnormal hepatic function; profiles of these events in this study were similar to those in previous studies of BKM120 monotherapy. No treatment-related deaths occurred. PI3K pathway activation was observed in patients with good clinical response.
BKM120 monotherapy showed promising efficacy and a manageable toxicity profile even in patients with pretreated advanced ESCC. This study showed the potential target PI3K for ESCC, and further confirmatory trial will be necessary to confirm it. Unique ID issued by UMIN: UMIN 000011217.
PI3K/AKT/mTOR 通路在食管鳞癌(ESCC)中经常过度活跃,使其成为有吸引力的治疗靶点。BKM120 是一种口服泛 I 类 PI3K 抑制剂,在几种癌症中具有有前景的活性。我们前瞻性地研究了 BKM120 在晚期 ESCC 中的疗效、安全性和生物标志物。我们进行了一项多中心、II 期研究,评估 BKM120 单药治疗预处理后的晚期 ESCC 患者的疗效。
BKM120(100mg/天)在 28 天的周期内口服给药。主要终点是疾病控制率(DCR)。对所有患者的肿瘤样本进行综合基因组分析检测基因改变。
42 例患者入组,20 例患者疾病稳定,2 例患者确认部分缓解。1 例不合规患者被排除在主要分析之外,该患者符合主要终点(DCR 为 51.2%;95%置信区间[CI],35.1-67.1)。在 42 例患者中,中位无进展生存期和总生存期分别为 2.3(95%CI 1.8-3.2)和 9.0(95%CI 6.5-11.4)个月。常见的 3 级或 4 级不良事件有皮疹、厌食、低钠血症和肝功能异常;本研究中这些事件的发生情况与 BKM120 单药治疗的既往研究相似。无治疗相关死亡事件发生。PI3K 通路的激活与临床反应良好的患者相关。
即使在预处理后的晚期 ESCC 患者中,BKM120 单药治疗也显示出了有希望的疗效和可管理的毒性特征。本研究显示了 ESCC 的潜在靶标 PI3K,需要进一步的确认性试验来证实。
独特 ID 号由 UMIN 颁发:UMIN 000011217。