To Ciric, Kim Eun-Hee, Royce Darlene B, Williams Charlotte R, Collins Ryan M, Risingsong Renee, Sporn Michael B, Liby Karen T
Authors' Affiliations: Departments of Pharmacology, and.
Authors' Affiliations: Departments of Pharmacology, and Medicine, Dartmouth Medical School, Hanover, New Hampshire
Cancer Prev Res (Phila). 2014 Jul;7(7):698-707. doi: 10.1158/1940-6207.CAPR-14-0047. Epub 2014 May 9.
Poly-ADP ribose polymerase (PARP) inhibitors are effective for the treatment of BRCA-deficient tumors. Women with these mutations have an increased risk of developing breast cancer and would benefit from effective chemoprevention. This study examines whether the PARP inhibitors, veliparib and olaparib, delay mammary gland tumor development in a BRCA1-deficient (BRCA1(Co/Co);MMTV-Cre;p53(+/-)) mouse model. In dose de-escalation studies, mice were fed with control, veliparib (100 mg/kg diet), or olaparib (200, 100, 50, or 25 mg/kg diet) continuously for up to 43 weeks. For intermittent dosing studies, mice cycled through olaparib (200 mg/kg diet) for 2 weeks followed by a 4-week rest period on control diet. To examine biomarkers, mice were fed with olaparib using the intermittent dosing regimen and mammary glands were evaluated by immunohistochemistry. In mice treated with veliparib or olaparib (200 mg/kg diet), the average age of the first detectable tumor was delayed by 2.4 and 6.5 weeks, respectively, compared with controls. Olaparib also increased the average lifespan of mice by 7 weeks. In dose de-escalation studies, lower concentrations of olaparib delayed tumor development but were less effective than the highest dose. When fed intermittently, olaparib delayed the onset of the first palpable tumor by 5.7 weeks and significantly reduced proliferation and induced apoptosis in hyperplastic mammary glands. In summary, veliparib and olaparib are effective for delaying tumor development and extending the lifespan of BRCA1-deficient mice, and intermittent dosing with olaparib was as effective as continuous dosing. These results suggest that the use of PARP inhibitors is a promising chemopreventive option.
聚-ADP核糖聚合酶(PARP)抑制剂对治疗BRCA缺陷型肿瘤有效。携带这些突变的女性患乳腺癌的风险增加,有效的化学预防对她们有益。本研究考察了PARP抑制剂维利帕尼和奥拉帕尼是否能延缓BRCA1缺陷(BRCA1(Co/Co);MMTV-Cre;p53(+/-))小鼠模型中乳腺肿瘤的发生。在剂量递减研究中,小鼠连续43周喂食对照、维利帕尼(100毫克/千克饮食)或奥拉帕尼(200、100、50或25毫克/千克饮食)。对于间歇给药研究,小鼠循环服用奥拉帕尼(200毫克/千克饮食)2周,随后在对照饮食上休息4周。为了检测生物标志物,采用间歇给药方案给小鼠喂食奥拉帕尼,并通过免疫组织化学评估乳腺。与对照组相比,用维利帕尼或奥拉帕尼(200毫克/千克饮食)治疗的小鼠首次可检测到肿瘤的平均年龄分别延迟了2.4周和6.5周。奥拉帕尼还使小鼠的平均寿命延长了7周。在剂量递减研究中,较低浓度的奥拉帕尼可延缓肿瘤发生,但效果不如最高剂量。间歇喂食时,奥拉帕尼将首次可触及肿瘤的发生延迟了5.7周,并显著降低了增生性乳腺中的增殖并诱导了凋亡。总之,维利帕尼和奥拉帕尼对延缓BRCA1缺陷小鼠的肿瘤发生和延长其寿命有效,奥拉帕尼间歇给药与连续给药效果相同。这些结果表明,使用PARP抑制剂是一种有前景的化学预防选择。