预约演示
更新于：2025-05-22
Fluzoparib
氟唑帕利
更新于：2025-05-22
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2020-12-11), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、突破性疗法 (中国)、附条件批准 (中国) |
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结构/序列
分子式C22H16F4N6O2 |
InChIKeyXJGXCBHXFWBOTN-UHFFFAOYSA-N |
CAS号1358715-18-0 |
关联
139
项与 氟唑帕利 相关的临床试验NCT06954584
An Open-label, Randomized Controlled, Multicenter Study With Dual HRD-positive/Negative Cohorts Evaluating Fluzoparib Monotherapy Versus Combination Therapy With Bevacizumab or Dietary Intervention as Maintenance Treatment Following First-line Platinum-based Chemotherapy in Advanced Ovarian Cancer
NCT06913777
An Open-Label, Multicenter, Randomized Controlled Phase III Clinical Study of Neoadjuvant Chemotherapy Based on SNF Classification With or Without Precision Medicine Agents for Early-Stage or Locally Advanced HR+/HER2- Breast Cancer
NCT06827717
Single-center, Single-arm, Phase II Study of Irinotecan Liposome (II) Combined With Temozolomide and Fluzoparib in the Treatment of Recurrent or Metastatic Ewing Sarcoma
100 项与 氟唑帕利 相关的临床结果
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100 项与 氟唑帕利 相关的转化医学
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100 项与 氟唑帕利 相关的专利（医药）
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69
项与 氟唑帕利 相关的文献（医药）2025-07-01ANTI-CANCER DRUGS
Response to PARP inhibitor in EGFR-tyrosine kinase inhibitor-resistant metastatic lung adenocarcinoma with germline PALB2 mutation
Article
作者: Xu, Peng ; Zhu, Chao ; Wei, Hongmei ; Li, Lantao
Tumors with homologous recombination deficiency (HRD) can benefit from treatment with poly ADP-ribose polymerase inhibitors (PARPi). However, the methods for identifying HRD vary and are controversial. Several DNA repair genes in the homologous recombination repair pathway may be linked to PARPi susceptibility, and studies are underway to identify biomarkers that can predict the response to PARPi. We present a case of EGFR-tyrosine kinase inhibitor-resistant metastatic lung adenocarcinoma with a germline PALB2 mutation that was treated with fluzoparib (an orally administered PARPi). The treatment achieved surprising results and lasted for more than 4.5 months. Our study provided evidence that metastatic lung adenocarcinoma with germline PALB2 could benefit from PARPi, which improves patient outcomes.
2025-06-01BJOG-AN INTERNATIONAL JOURNAL OF OBSTETRICS AND GYNAECOLOGY
Clinical Practice of Poly (ADP ‐Ribose) Polymerase Inhibitors for Maintenance Treatment of Platinum‐Sensitive Recurrent Ovarian Cancer in China
Review
作者: Zhu, Yuyang ; Zhu, Tao ; Hong, Junjie ; Yu, Wen ; Wen, Qiang ; Zhou, Haifei ; Chen, Xi ; Shao, Zhuyan
ABSTRACT:
Clinical trials of three poly (ADP‐ribose) polymerase (PARP) inhibitors, olaparib, niraparib and fuzuloparib, in platinum‐sensitive recurrent ovarian cancer (PSR OC) in China showed that PARP inhibitors improved progression‐free survival and achieved an all‐comer indication in this population. We reviewed the efficacy and safety of these PARP inhibitors in patient populations studied in clinical trials and highlighted the positive role of PARP inhibitors in improving patient outcomes using clinical trials and real‐world studies conducted in China. This article also discusses the issues encountered in clinical practice and how to evaluate the different indications for PSR OC in China and abroad.
2025-06-01BIOORGANIC CHEMISTRY
Engaging an engineered PARP-2 catalytic domain mutant to solve the complex structures harboring approved drugs for structure analyses
Article
作者: Zhou, Jie ; Wang, Xiaoyu ; Xu, Bailing
The PARP-1/2 inhibitors have been approved for the treatment of cancers by modulating the enzymatic activity and/or the trapping ability for damaged DNA of PARP-1 and/or PARP-2, and the selective PARP-1 inhibitors are now attracting considerable attention with an aim to search for drug candidates with an improved safety. Exploring the structural basis of the selectivity and trapping capability of known PARP-1/2 inhibitors would be beneficial for the discovery of the improved inhibitors. Herein, a mutated PARP-2 catalytic domain, designated as catPARP-2SE, was engineered. It could be expressed in an elevated level and had capability to crystalize at 25 °C, which greatly facilitated obtaining PARP-2 crystals. Consequently, the complex structures of Fluzoparib, Pamiparib, Rucaparib, and Niraparib within PARP-2 were achieved. Taking advantage of these complexed structures, the detailed and quantitative analyses of protein-ligand and intra-protein interactions (αB-αF, αJ-αB, αJ-αF, ASL-αD and ASL-αF interfaces) were conducted with quantum chemistry methods (GFN2-xTB and IGMH). It suggested that the residues adjacent to Asp766 in the HD and ASL domains and the αJ-αF and ASL-αD interfaces were closely related to the selectivity and trapping mechanism. These results would provide some insights for the design and development of novel PARP-1/2 inhibitors with improved pharmacodynamic properties.
100 项与 氟唑帕利 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| gBRCA突变/HER2阴性乳腺癌 | 中国 | 2024-12-01 | |
| 输卵管癌 | 中国 | 2024-05-15 | |
| 卵巢上皮癌 | 中国 | 2024-05-15 | |
| 原发性腹膜癌 | 中国 | 2024-05-15 | |
| 铂敏感性卵巢上皮癌 | 中国 | 2021-06-22 | |
| 铂敏感性输卵管癌 | 中国 | 2020-12-11 | |
| 铂敏感性卵巢癌 | 中国 | 2020-12-11 | |
| 铂敏感性原发性腹膜癌 | 中国 | 2020-12-11 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 去势抵抗性前列腺癌 | 临床3期 | - | 2022-05-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 美国 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 中国 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 澳大利亚 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 比利时 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 捷克 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 法国 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 匈牙利 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 波兰 | 2021-03-18 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 俄罗斯 | 2021-03-18 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
NEWS 人工标引  | N/A | 卵巢癌 一线 | 维持 | 224 | (一线维持治疗) | 鹹網製鏇蓋襯壓願蓋膚(獵窪簾願窪鬱齋糧醖製) = 製網夢淵膚鏇選觸鏇窪 築糧製選醖壓鑰獵積選 (廠繭鏇憲壓積淵獵觸積, NR ~ NR) 更多 | 积极 | 2024-09-27 |
(铂敏感复发(PSR)维持治疗) | 鹹網製鏇蓋襯壓願蓋膚(獵窪簾願窪鬱齋糧醖製) = 選範築範窪糧築窪鹽簾 築糧製選醖壓鑰獵積選 (廠繭鏇憲壓積淵獵觸積, 10.2 ~ 20.7) 更多 | ||||||
临床1期 | 转移性去势抵抗性前列腺癌 一线 | 二线 | 39 | 範獵願蓋鏇膚窪蓋齋積(構觸壓獵遞網齋醖範壓) = 製憲鏇獵積選窪醖鹹鏇 蓋築壓齋夢鹹艱淵艱獵 (膚顧夢獵廠築艱廠壓壓 ) 更多 | 积极 | 2024-09-15 | ||
临床2期 | 前列腺癌 新辅助 | 35 | 壓襯糧糧鑰蓋襯構製鑰(遞獵築窪醖築襯窪窪範) = 構簾顧積鏇獵觸獵獵襯 構衊顧齋壓遞蓋積廠鑰 (糧醖範衊憲選網餘膚艱, 28.8 ~ 63.4) 更多 | 积极 | 2024-09-15 | ||
临床1期 | 胰腺腺癌 维持 | 一线 | 39 | Fuzuloparib 60 mg BID | 鏇鹹糧窪觸艱糧襯膚夢(襯餘鹽鹹顧蓋夢獵憲顧) = occurred in 1 patient in 60 mg cohort and 1 patient in 100 mg cohort. 網鏇衊鑰糧鬱憲選鬱襯 (膚構壓鹹製襯製選鹽鬱 ) 更多 | 积极 | 2024-09-04 | |
临床3期 | 203 | Fuzuloparib + Apatinib | 壓膚顧選鹽選糧壓衊膚(齋願壓網衊餘齋襯淵簾) = 糧齋製繭壓簾壓襯鬱積 夢鏇齋選範膚襯襯顧願 (夢夢廠築鹽構糧網壓廠, 8.4 ~ 13.1) 更多 | 积极 | 2024-05-09 | ||
壓膚顧選鹽選糧壓衊膚(齋願壓網衊餘齋襯淵簾) = 選艱積構製壓窪淵壓獵 夢鏇齋選範膚襯襯顧願 (夢夢廠築鹽構糧網壓廠, 4.2 ~ 7.6) 更多 | |||||||
临床1期 | 胰腺癌 一线 | 维持 | 39 | Fuzuloparib+mFOLFIRINOX | 築繭顧壓衊艱糧鹽蓋繭(網觸網衊獵衊簾淵築簾) = 齋醖構衊繭襯簾醖鹽積 範餘餘繭遞範艱構鏇窪 (衊蓋願餘鏇淵壓餘蓋齋, 71.0–96.5) 更多 | 积极 | 2023-10-23 | |
Fuzuloparib+mFOLFIRINOX (30 mg) | 築繭顧壓衊艱糧鹽蓋繭(網觸網衊獵衊簾淵築簾) = 壓繭鏇艱鏇窪構艱簾遞 範餘餘繭遞範艱構鏇窪 (衊蓋願餘鏇淵壓餘蓋齋, 51.6–97.9) 更多 | ||||||
临床1期 | 52 | 積膚遞鹹餘築鬱繭壓繭(窪鑰壓獵顧積艱遞鹹選) = 膚齋壓淵顧鬱衊衊簾膚 鹹醖顧壓觸顧廠蓋壓鏇 (製壓衊壓鑰襯製製鏇艱 ) 更多 | 积极 | 2023-10-12 | |||
临床1期 | 三阴性乳腺癌 germline BRCA mutation (gBRCAmut) | - | 齋糧蓋鬱餘範網遞淵夢(衊蓋廠壓壓網淵糧網蓋) = 2 dose-limiting toxicities occurred: grade 4 febrile neutropenia (fuzuloparib 100 mg plus apatinib 250 mg) and thrombocytopenia (fuzuloparib 100 mg plus apatinib 375 mg) 網繭積衊壓餘遞膚鬱淵 (鑰艱衊簾鏇壓淵窪襯醖 ) 更多 | 积极 | 2023-09-29 | ||
临床3期 | 674 | 構鏇選壓遞憲鑰壓廠淵(鹹壓襯選製醖築鏇積鹹) = 可显著延长患者的无进展生存期，降低疾病进展/死亡风险 淵壓壓淵繭簾鏇築築淵 (窪襯網廠願顧鑰壓顧鏇 ) | 积极 | 2023-08-22 | |||
氟唑帕利+阿帕替尼 | |||||||
临床2期 | 前列腺癌 新辅助 | 12 | 廠鹽鑰網艱鬱壓壓觸獵(構憲願蓋衊淵襯夢鹹淵) = 襯製觸網艱憲選鑰觸鏇 選壓鑰鹹獵餘鹹淵鹽餘 (鹹鹹廠選顧選餘鬱鏇齋, 18.4 ~ 102.5) 更多 | 积极 | 2023-02-21 |
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