University of Colorado Cancer Center, Denver, Colorado 80045, USA.
Cancer Med. 2012 Oct;1(2):207-17. doi: 10.1002/cam4.27. Epub 2012 Aug 16.
Src tyrosine kinases are overexpressed in pancreatic cancers, and the oral Src inhibitor saracatinib has shown antitumor activity in preclinical models of pancreas cancer. We performed a CTEP-sponsored Phase II clinical trial of saracatinib in previously treated pancreas cancer patients, with a primary endpoint of 6-month survival. A Simon MinMax two-stage phase II design was used. Saracatinib (175 mg/day) was administered orally continuously in 28-day cycles. In the unselected portion of the study, 18 patients were evaluable. Only two (11%) patients survived for at least 6 months, and three 6-month survivors were required to move to second stage of study as originally designed. The study was amended as a biomarker-driven trial (leucine rich repeat containing protein 19 [LRRC19] > insulin-like growth factor-binding protein 2 [IGFBP2] "top scoring pairs" polymerase chain reaction [PCR] assay, and PIK3CA mutant) based on preclinical data in a human pancreas tumor explant model. In the biomarker study, archival tumor tissue or fresh tumor biopsies were tested. Biomarker-positive patients were eligible for the study. Only one patient was PIK3CA mutant in a 3' untranslated region (UTR) portion of the gene. This patient was enrolled in the study and failed to meet the 6-month survival endpoint. As the frequency of biomarker-positive patients was very low (<3%), the study was closed. Although we were unable to conclude whether enriching for a subset of second/third line pancreatic cancer patients treated with a Src inhibitor based on a biomarker would improve 6-month survival, we demonstrate that testing pancreatic tumor samples for a biomarker-driven, multicenter study in metastatic pancreas cancer is feasible.
Src 酪氨酸激酶在胰腺癌中过表达,口服Src 抑制剂 saracatinib 在胰腺癌的临床前模型中显示出抗肿瘤活性。我们进行了一项由 CTEP 赞助的 saracatinib 治疗既往治疗过的胰腺癌患者的 II 期临床试验,主要终点是 6 个月的生存率。采用 Simon MinMax 两阶段 II 期设计。saracatinib(每天 175mg)在 28 天的周期内连续口服给药。在研究的未选择部分,18 名患者可评估。只有两名(11%)患者至少存活 6 个月,根据最初的设计,需要 3 名 6 个月的幸存者进入研究的第二阶段。该研究被修改为基于人类胰腺肿瘤外植体模型的临床前数据的生物标志物驱动试验(富含亮氨酸重复蛋白 19[LRRC19]>胰岛素样生长因子结合蛋白 2[IGFBP2]“得分最高的配对”聚合酶链反应[PCR]检测和 PIK3CA 突变)。在生物标志物研究中,检测了存档的肿瘤组织或新鲜的肿瘤活检。生物标志物阳性的患者有资格参加研究。只有一名患者在基因的 3'非翻译区(UTR)部分发生 PIK3CA 突变。该患者被纳入研究,但未达到 6 个月的生存终点。由于生物标志物阳性患者的频率非常低(<3%),该研究被关闭。尽管我们无法得出结论,即根据生物标志物富集接受 Src 抑制剂治疗的二线/三线胰腺癌患者亚组是否会提高 6 个月的生存率,但我们证明在转移性胰腺癌中进行基于生物标志物的多中心研究测试胰腺肿瘤样本是可行的。