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PARP抑制剂在卵巢癌中的应用

PARP Inhibitors in Ovarian Cancer.

作者信息

Mittica Gloria, Ghisoni Eleonora, Giannone Gaia, Genta Sofia, Aglietta Massimo, Sapino Anna, Valabrega Giorgio

机构信息

Department of Oncology, University of Torino, Torino, Italy.

Candiolo Cancer Institute-FPO-IRCCS, Candiolo, Torino, Italy.

出版信息

Recent Pat Anticancer Drug Discov. 2018;13(4):392-410. doi: 10.2174/1574892813666180305165256.

Abstract

BACKGROUND

Treatment of Epithelial Ovarian Cancer (EOC), historically based on surgery and platinum doublet chemotherapy, is associated with high risk of relapse and poor prognosis for recurrent disease. In this landscape, the innovative treatment with PARP inhibitors (PARPis) demonstrated an outstanding activity in EOC, and is currently changing clinical practice in BRCA mutant patients.

OBJECTIVES

The study aimed to highlight the mechanism of action, pharmacokinetics, clinical activity, indications and current strategies of development of Olaparib, Niraparib, Rucaparib, Talazoparib and Veliparib, the 5 most relevant PARPis.

METHODS

We performed a review on Pubmed using 'ovarian cancer' and the name of each PARPi (PARP inhibitor) discussed in the review as Medical Subject Headings (MeSH) keywords. The same search was performed on "clinicaltrial.gov" to identify ongoing clinical trials and on "google. com/patents" and "uspto.gov" for recent patents exploring PARPIs in ovarian cancer.

RESULTS

Olaparib, Niraparib and Rucaparib are already approved for the treatment of recurrent EOC and their indications are partially overlapping. Talazoparib and Veliparib are promising PARPis, but currently under investigation in early phase trials. Several studies are evaluating PARPis in monotherapy or in associations, in a wide range of settings (i.e. first line, neoadjuvant, platinum-sensitive and resistant disease).

CONCLUSION

PARPis are valuable options in patients with recurrent ovarian cancer with promising activity in different stages of this disease. Further studies are required to better define optimal clinical settings, predictors of response beyond BRCA mutations and strategies to overcome secondary resistance of PARPis therapy in EOC.

摘要

背景

上皮性卵巢癌(EOC)的治疗历来基于手术和铂类双联化疗,复发风险高,复发疾病预后差。在这种情况下,聚(腺苷酸)核糖聚合酶抑制剂(PARPis)的创新疗法在EOC中显示出卓越活性,目前正在改变BRCA突变患者的临床实践。

目的

本研究旨在突出奥拉帕利、尼拉帕利、鲁卡帕利、他拉唑帕利和维利帕利这5种最相关的PARPis的作用机制、药代动力学、临床活性、适应证及当前研发策略。

方法

我们在PubMed上进行检索,使用“卵巢癌”以及本综述中讨论的每种PARPi(PARP抑制剂)的名称作为医学主题词(MeSH)关键词。在“clinicaltrial.gov”上进行同样的检索以识别正在进行的临床试验,并在“google.com/patents”和“uspto.gov”上检索探索PARPIs用于卵巢癌的近期专利。

结果

奥拉帕利、尼拉帕利和鲁卡帕利已获批用于治疗复发性EOC,其适应证部分重叠。他拉唑帕利和维利帕利是有前景的PARPis,但目前正处于早期试验研究中。多项研究正在评估PARPis在单药治疗或联合治疗中的应用,涉及广泛的治疗场景(即一线、新辅助、铂敏感和耐药疾病)。

结论

PARPis是复发性卵巢癌患者的有价值选择,在该疾病的不同阶段均具有有前景的活性。需要进一步研究以更好地确定最佳临床治疗场景、BRCA突变以外的反应预测指标以及克服EOC中PARPis治疗继发性耐药的策略。

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