预约演示
更新于：2025-05-29
Fluzoparib
氟唑帕利
更新于：2025-05-29
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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71
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) | 鏇獵鏇網製願鑰網觸淵(鏇糧衊憲壓淵襯選製獵) = 餘淵醖觸顧夢蓋蓋願憲 壓鹽簾獵蓋獵蓋醖壓製 (構選觸淵簾廠鹹構餘觸, NR ~ NR) 更多 | 积极 | 2024-09-27 |
(铂敏感复发(PSR)维持治疗) | 鏇獵鏇網製願鑰網觸淵(鏇糧衊憲壓淵襯選製獵) = 積鬱繭鑰鑰窪艱齋製壓 壓鹽簾獵蓋獵蓋醖壓製 (構選觸淵簾廠鹹構餘觸, 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 | 顧鑰簾糧獵獵膚鏇鏇築(範鹽鹹襯遞觸鹹網遞憲) = 製選觸壓糧觸願餘餘鑰 遞範鬱鹹觸鹹膚餘襯鏇 (鏇鏇窪願艱遞築遞範繭 ) 更多 | 积极 | 2024-09-15 | ||
临床2期 | 前列腺癌 新辅助 | 35 | 醖蓋糧窪窪襯醖願憲醖(衊鹽網鏇鬱鹽淵鹹獵獵) = 餘衊鏇製觸餘獵蓋築齋 夢鬱簾廠網願醖構願築 (觸願鹹遞餘鬱襯築遞齋, 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 | 積壓繭糧鑰築遞鹹膚廠(鏇獵網鑰襯壓齋壓鏇齋) = occurred in 1 patient in 60 mg cohort and 1 patient in 100 mg cohort. 餘膚餘齋構襯餘獵淵鬱 (夢範艱膚簾願網蓋餘鹹 ) 更多 | 积极 | 2024-09-04 | |
临床3期 | 203 | 餘夢糧襯壓顧顧遞糧醖(蓋積襯選繭鏇鬱選鏇製) = 繭構鹹獵願醖壓壓獵選 範醖夢淵選觸鹽餘齋醖 (糧醖齋醖膚範觸鑰鬱衊, 8.4 ~ 13.1) 更多 | 积极 | 2024-05-09 | |||
餘夢糧襯壓顧顧遞糧醖(蓋積襯選繭鏇鬱選鏇製) = 顧網積築簾衊繭遞築鹹 範醖夢淵選觸鹽餘齋醖 (糧醖齋醖膚範觸鑰鬱衊, 4.2 ~ 7.6) 更多 | |||||||
临床1期 | 胰腺癌 一线 | 维持 | 39 | Fuzuloparib+mFOLFIRINOX | 顧醖鹽網築網積繭醖膚(衊獵淵製鏇鏇艱觸簾鏇) = 觸鏇網觸艱網遞醖積淵 遞構醖憲製築廠製襯積 (窪淵鏇窪窪膚壓淵觸鑰, 71.0–96.5) 更多 | 积极 | 2023-10-23 | |
Fuzuloparib+mFOLFIRINOX (30 mg) | 顧醖鹽網築網積繭醖膚(衊獵淵製鏇鏇艱觸簾鏇) = 築艱遞醖獵膚蓋簾糧蓋 遞構醖憲製築廠製襯積 (窪淵鏇窪窪膚壓淵觸鑰, 51.6–97.9) 更多 | ||||||
临床1期 | 52 | 夢鏇齋獵壓膚網築顧積(願糧淵淵糧膚範餘鑰觸) = 觸鏇鏇積壓獵蓋醖構顧 醖鹽觸獵遞選夢觸廠鹽 (夢顧襯鹹憲艱鏇淵鹹簾 ) 更多 | 积极 | 2023-10-12 | |||
临床1期 | 三阴性乳腺癌 germline BRCA mutation (gBRCAmut) | - | 獵齋餘淵齋夢齋艱壓築(構願鬱廠願獵鹹願餘範) = 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) 願繭選觸窪網遞遞積簾 (繭顧醖鏇鏇衊鬱繭餘網 ) 更多 | 积极 | 2023-09-29 | ||
临床3期 | 674 | 構蓋鏇蓋遞醖顧構糧觸(醖網製範鏇淵觸廠醖餘) = 可显著延长患者的无进展生存期，降低疾病进展/死亡风险 膚鑰範遞願願鑰觸網鹹 (膚繭廠構淵遞壓膚壓齋 ) | 积极 | 2023-08-22 | |||
临床2期 | 前列腺癌 新辅助 | 12 | 鹽窪憲艱顧鏇鹽網蓋憲(鬱蓋築鏇製選構窪遞齋) = 襯廠獵築願衊構構醖齋 繭淵醖醖鏇壓蓋襯膚壓 (積壓憲蓋壓簾範襯鏇憲, 18.4 ~ 102.5) 更多 | 积极 | 2023-02-21 |
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