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呋喹替尼在卵巢癌治疗中的概述:背景与未来展望。

Overview of fuzuloparib in the treatment of ovarian cancer: background and future perspective.

机构信息

Department of Gynecologic Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.

Jiangsu Hengrui Pharmaceuticals Co., Ltd. Shanghai, China.

出版信息

J Gynecol Oncol. 2022 Nov;33(6):e86. doi: 10.3802/jgo.2022.33.e86.

DOI:10.3802/jgo.2022.33.e86
PMID:36335989
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9634097/
Abstract

Over the last decade, clinical trials using various poly ADP ribose polymerase (PARP) inhibitors on patients with ovarian cancer have shown promising results. The introduction of PARP inhibitors has changed the treatment landscape and improved outcomes for patients with ovarian cancer. Fuzuloparib, developed by Jiangsu Hengrui Pharmaceuticals Co., Ltd., is a novel orally available small molecule PARP inhibitor. By introducing the trifluoromethyl group into chemical structure, fuzuloparib exhibits higher stability and lower inter-individual variability than other PARP inhibitors. Several clinical trials (FZOCUS series and others) have been carried out to assess the efficacy and safety of fuzuloparib through different lines of treatments for advanced or recurrent ovarian cancer in both treatment and maintenance. Here, we present the most recent data from these studies, discuss current progress and potential future directions.

摘要

在过去的十年中,针对卵巢癌患者的各种多聚 ADP 核糖聚合酶 (PARP) 抑制剂的临床试验取得了可喜的结果。PARP 抑制剂的引入改变了卵巢癌的治疗格局,改善了患者的预后。由江苏恒瑞医药有限公司开发的氟唑帕利是一种新型口服小分子 PARP 抑制剂。通过在化学结构中引入三氟甲基,氟唑帕利比其他 PARP 抑制剂具有更高的稳定性和更低的个体间变异性。几项临床试验(FZOCUS 系列和其他)已经开展,通过不同的治疗线评估氟唑帕利在晚期或复发性卵巢癌中的疗效和安全性,包括治疗和维持治疗。在这里,我们呈现了这些研究的最新数据,讨论了当前的进展和潜在的未来方向。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef04/9634097/ff93f964b2f8/jgo-33-e86-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef04/9634097/44c277d07ebf/jgo-33-e86-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef04/9634097/ff93f964b2f8/jgo-33-e86-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef04/9634097/44c277d07ebf/jgo-33-e86-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef04/9634097/ff93f964b2f8/jgo-33-e86-g002.jpg

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本文引用的文献

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Protein Panel of Serum-Derived Small Extracellular Vesicles for the Screening and Diagnosis of Epithelial Ovarian Cancer.用于上皮性卵巢癌筛查和诊断的血清来源小细胞外囊泡蛋白质组
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Fuzuloparib Maintenance Therapy in Patients With Platinum-Sensitive, Recurrent Ovarian Carcinoma (FZOCUS-2): A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase III Trial.氟唑帕利维持治疗铂敏感复发性卵巢癌患者(FZOCUS-2):一项多中心、随机、双盲、安慰剂对照的 III 期临床试验。
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Poly (ADP-ribose) polymerase inhibitor therapy and mechanisms of resistance in epithelial ovarian cancer.
聚(ADP - 核糖)聚合酶抑制剂疗法及上皮性卵巢癌的耐药机制
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Clinical characterization and genomic landscape of gynecological cancers among patients attending a Chinese hospital.一家中国医院收治的妇科癌症患者的临床特征与基因组图谱
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Major clinical research advances in gynecologic cancer in 2022: highlight on late-line PARP inhibitor withdrawal in ovarian cancer, the impact of ARIEL-4, and SOLO-3.2022 年妇科癌症的主要临床研究进展:重点关注晚期 PARP 抑制剂在卵巢癌中的停药、ARIEL-4 和 SOLO-3 的影响。
J Gynecol Oncol. 2023 Mar;34(2):e51. doi: 10.3802/jgo.2023.34.e51.
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Effect of a moderate CYP3A inducer efavirenz on the pharmacokinetics of fuzuloparib: An open-label, fixed sequence study in Chinese healthy male subjects.中度CYP3A诱导剂依非韦伦对氟唑帕利药代动力学的影响:一项在中国健康男性受试者中开展的开放标签、固定序列研究。
Invest New Drugs. 2023 Apr;41(2):276-283. doi: 10.1007/s10637-023-01331-0. Epub 2023 Feb 17.
Fuzuloparib: First Approval.
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Drugs. 2021 Jul;81(10):1221-1226. doi: 10.1007/s40265-021-01541-x.
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Target Oncol. 2019 Dec;14(6):657-679. doi: 10.1007/s11523-019-00680-2.
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Lancet Oncol. 2019 Oct;20(10):1409-1419. doi: 10.1016/S1470-2045(19)30515-7. Epub 2019 Aug 29.