Coleman Robert L, Sill Michael W, Bell-McGuinn Katherine, Aghajanian Carol, Gray Heidi J, Tewari Krishnansu S, Rubin Steven C, Rutherford Thomas J, Chan John K, Chen Alice, Swisher Elizabeth M
Dept. of Gynecologic Oncology & Reproductive Medicine, University of Texas, M.D. Anderson Cancer Center, Houston, TX 77030, USA.
NRG Statistical & Data Center, Roswell Park Cancer Institute, Buffalo, NY 14263, USA.
Gynecol Oncol. 2015 Jun;137(3):386-91. doi: 10.1016/j.ygyno.2015.03.042. Epub 2015 Mar 24.
Veliparib is a potent small molecule inhibitor of PARP-1/2, which is cytotoxic in tumor cells with deficiencies in BRCA1 or BRCA2. We studied the clinical activity and toxicity of veliparib in ovarian cancer patients carrying a germline BRCA1 or BRCA2 mutation (gBRCA).
Eligibility included three or fewer prior chemotherapy regimens, measurable disease and no prior use of a PARP inhibitor. Veliparib was administered at 400mg orally BID with one cycle being 28days. The two-stage Simon design was capable of detecting a 25% response probability with 90% power while controlling alpha=10% (at a 10% assumed null response probability).
The median age of the 50 eligible patients was 57years (range 37-94) and 14, 18, and 18 patients had 1, 2, and 3 prior therapies respectively. Thirty patients (60%) were platinum-resistant. The median number of cycles administered was 6 (1-27). There was one grade 4 thrombocytopenia. Grade 3 adverse events were: fatigue (n=3), nausea (2), leukopenia (1), neutropenia (1), dehydration (1), and ALT (1). Grade 2 events >10% were: nausea (46%), fatigue (26%), vomiting (18%), and anemia (14%). The proportion responding was 26% (90% CI: 16%-38%, CR: 2, PR: 11); for platinum-resistant and platinum-sensitive patients the proportion responding was 20% and 35%, respectively. The most common reason for treatment discontinuation was progression (62%). Twenty-nine patients are alive; two with SD remain on veliparib. The median PFS is 8.18months.
The single agent efficacy and tolerability of veliparib for BRCA mutation-associated recurrent ovarian cancer warrants further investigation.
维利帕尼是一种有效的PARP-1/2小分子抑制剂,对BRCA1或BRCA2缺陷的肿瘤细胞具有细胞毒性。我们研究了维利帕尼在携带种系BRCA1或BRCA2突变(gBRCA)的卵巢癌患者中的临床活性和毒性。
入选标准包括既往化疗方案不超过三种、疾病可测量且未使用过PARP抑制剂。维利帕尼口服给药,剂量为400mg,每日两次,一个周期为28天。两阶段西蒙设计能够在控制α=10%(假设无效反应概率为10%)的情况下,以90%的把握度检测25%的反应概率。
50例符合条件的患者中位年龄为57岁(范围37-94岁),分别有14例、18例和18例患者接受过1次、2次和3次既往治疗。30例患者(60%)对铂类耐药。给药的中位周期数为6个(1-27个)。发生1例4级血小板减少症。3级不良事件包括:疲劳(n=3)、恶心(2例)、白细胞减少(1例)、中性粒细胞减少(1例)、脱水(1例)和谷丙转氨酶升高(1例)。发生率>10%的2级事件包括:恶心(46%)、疲劳(26%)、呕吐(18%)和贫血(14%)。反应率为26%(90%CI:16%-38%,完全缓解:2例,部分缓解:11例);铂类耐药和铂类敏感患者的反应率分别为20%和35%。治疗中断的最常见原因是疾病进展(62%)。29例患者存活;2例病情稳定的患者仍在接受维利帕尼治疗。中位无进展生存期为8.18个月。
维利帕尼单药治疗BRCA突变相关复发性卵巢癌的疗效和耐受性值得进一步研究。