更新于：2024-09-15
Fluzoparib
氟唑帕利
更新于：2024-09-15
概要
基本信息
原研机构 |
非在研机构 |
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)、附条件批准 (中国)、突破性疗法 (中国) |
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结构
分子式C22H16F4N6O2 |
InChIKeyXJGXCBHXFWBOTN-UHFFFAOYSA-N |
CAS号1358715-18-0 |
关联
144
项与 氟唑帕利 相关的临床试验Clinical Study of Fluzopalil Combined With Apatinib for Maintenance Therapy After Platinum-containing Chemotherapy in Patients With Recurrent Ovarian Cancer
A Single-Arm, Open, Multicenter, Exploratory Clinical Study of Fluzoparib in Combination With Apatinib Mesylate for Maintenance Therapy in Stage III-IV Ovarian Cancer (FAT-1)
Fluzoparib Combined With Dalpiciclib for Platinum Resistant Recurrent Ovarian Cancer: a Phase II Clinical Study
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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38
项与 氟唑帕利 相关的文献（医药）2024-01-01Journal of pharmaceutical and biomedical analysis
Development and validation of a sensitive LC–MS/MS method for the assay of four PARP inhibitors in human plasma and its application in ovarian cancer patients
Article
作者: Liang, Haixi ; Guan, Yanping ; Chen, Youhao ; Guan, Shaoxing ; Huang, Min ; Wei, Yuru ; Liu, Shu ; Lan, Chunyan ; Wang, Xueding ; Ma, Kaiyun
PARP inhibitors have demonstrated marked efficacy in ovarian cancer patients with BRCA1/2 loss-of-function mutations. In this study, we established and validated a liquid chromatography-tandem mass spectrometry (LC-MS/MS) based method to simultaneously quantify the four frequently prescripted PARP inhibitors, namely niraparib, olaparib，fluzoparib, and pamiparib, in ovarian cancer. The mobile phase was 50 % methanol with 0.1 % formic acid at a flow rate of 0.3 mL/min, within 8 min run time. Four PARP inhibitors were separated on a Hypersil GOLD™ aQ C18 Polar Endcapped LC column (50 × 2.1 mm, 1.9 µm) at 35 ℃ and subjected to mass analysis using positive electro-spray ionization (ESI). The linear range of this method was 10-2000 ng/mL, 25-5000 ng/mL, and 50-10,000 ng/mL for niraparib, olaparib and fluzoparib, and pamiparib, respectively, with the correlation coefficients (r2) ≥ 0.99. Accuracies ranged from 93.12 %-110.71 and the inter- and intra-batch precisions were less than 15 % for all analytes in quality control samples. There was no significant matrix effect. Twenty-eight plasma samples were obtained from Sun Yat-sen University Cancer Center. The mean plasma concentrations (±SD) of niraparib and olaparib were 424.76 (±228.35) ng/mL and 1760.47 (±1739.69) ng/mL, respectively. The validated LC-MS/MS method allows the convient and efficient determination of four PARP inhibitors' exposure levels in ovarian cancer patients.
2023-12-28Journal of medicinal chemistry1区 · 医学
Advances in Development of Selective Antitumor Inhibitors That Target PARP-1
1区 · 医学
Review
作者: Li, Xiangqian ; Shi, Dayong ; Liu, Ruihua ; Chen, Jiashu ; Gao, Chenxia ; Zhang, Yiting ; Liu, Fang
Cancer is a major threat to the lives and health of people around the world, and the development of effective antitumor drugs that exhibit fewer toxic effects is an important aspect of cancer treatment. PARP inhibitors are antitumor drugs that target pathways involved in DNA-damage repair. The currently approved PARP inhibitors include olaparib, niraparib, rucaparib, talazoparib, fuzuloparib, and pamiparib. Hematological toxicities associated with the simultaneous inhibition of PARP-1 and PARP-2 have limited the clinical applications of these drugs. The present review introduces the necessity for research on the development of selective PARP-1 inhibitors from the perspective of structural and functional mechanisms of PARP-1 inhibition. A review of recently reported selective PARP-1 inhibitors provides the foundation for exploring novel strategies for designing selective PARP-1 inhibitors from the perspective of structure-activity relationships combined with computer simulations.
2023-12-01Journal, genetic engineering & biotechnology
Pangenome diversification and resistance gene characterization in Salmonella Typhi prioritized RfaJ as a significant therapeutic marker
Article
作者: Jalal, Khurshid ; Khan, Kanwal ; Uddin, Reaz
Abstract:
Background:
Salmonella Typhi stands as the etiological agent responsible for the onset of human typhoid fever. The pressing demand for innovative therapeutic targets against S. Typhi is underscored by the escalating prevalence of this pathogen and the severe nature of its infections. Consequently, this study employs pangenome analysis to scrutinize 119 S. Typhi-resistant strains, aiming to identify the most promising therapeutic targets originating from its core genome.
Results:
Subtractive genomics was employed to systematically eliminate non-homologous (n=1147), essential (n=551), drug-like (n=80), and pathogenicity-related (n=18) proteins from the initial pool of 3351 core genome proteins. Consequently, lipopolysaccharide 1,2-glucosyltransferase RfaJ was designated as the optimal pharmacological target due to its potential versatility. Furthermore, a compendium of 9000 FDA-approved compounds was repurposed for evaluation against the RfaJ drug target, with the specific intent of prioritizing novel, high-potency therapeutic candidates for combating S. Typhi. Ultimately, four compounds, namely DB00549 (Zafirlukast), DB15637 (Fluzoparib), DB15688 (Zavegepant), and DB12411 (Bemcentinib), were singled out as potential inhibitors based on the ligand-protein binding affinity (indicated by the lowest anticipated binding energy) and the overall stability of these compounds. Notably, molecular dynamics simulations, conducted over a 50 nanosecond interval, convincingly demonstrated the stability of these compounds in the context of the RfaJ protein.
Conclusion:
In summary, the present findings hold significant promise as an initial stride in the broader drug discovery endeavor against S. Typhi infections. However, the experimental validation of the identified drug target and drug candidate is further required to increase the effectiveness of the applied methodology.
200
项与 氟唑帕利 相关的新闻（医药）2024-09-13
·药渡
财报医药出海申请上市
2024-09-13
·恒瑞医药
抗体药物偶联物临床1期
2024-09-12
·恒瑞医药
抗体药物偶联物临床3期引进/卖出突破性疗法申请上市
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 |
|---|---|---|---|
| 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 |
|---|---|---|---|---|
| gBRCA突变/HER2阴性乳腺癌 | 申请上市 | 中国 | 2024-04-23 | |
| 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 | 中国 | 2021-03-18 | |
| 胰腺继发性恶性肿瘤 | 临床3期 | 中国 | 2020-08-19 | |
| 乳腺癌 | 临床3期 | 中国 | 2020-07-03 | |
| 卵巢癌 | 临床3期 | 中国 | 2020-05-12 | |
| 复发性卵巢癌 | 临床3期 | 中国 | 2019-04-11 | |
| 前列腺癌 | 临床3期 | 美国 | - | |
| HR阳性/HER2阳性乳腺癌 | 临床2期 | - | 2024-04-16 | |
| 肉瘤 | 临床2期 | 中国 | 2023-07-01 |
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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
临床1期 | 39 | 窪壓淵齋醖遞獵壓鬱鹹(顧膚艱淵衊壓鏇窪選壓) = ORR was 60% in pts with measurable lesions. 窪餘鏇夢構淵衊淵築壓 (壓襯鏇範顧獵鏇膚願壓 ) 更多 | 积极 | 2024-09-15 | |||
临床2期 | 前列腺癌 新辅助 | 35 | 願鑰餘淵積範鹽糧餘網(蓋衊網築餘顧餘襯鬱鹹) = Patients achieving pCR/MRD had longer median bPFS (Not reached vs. 10.8 months, p =0.046) 獵襯製窪醖願願築蓋鹹 (壓簾獵廠顧糧獵淵壓製 ) 更多 | 积极 | 2024-09-15 | ||
临床1期 | 胰腺腺癌 一线 | 维持 | 39 | 淵淵壓糧淵鹹齋糧繭憲(膚膚鑰憲鹽窪簾醖壓壓) = The most common grade ≥ 3 treatment-related adverse events were hematologic toxicities 餘遞齋齋衊鏇蓋選鬱鬱 (鏇製鏇鬱艱選範夢願範 ) | 积极 | 2024-09-04 | ||
临床3期 | 203 | Fuzuloparib + Apatinib | 淵積憲範範觸蓋鹹襯觸(廠壓構遞顧窪鹽壓鏇範) = 齋衊壓淵鬱鑰構鹹鬱襯 膚顧鏇夢觸簾願衊繭構 (齋壓蓋積壓鬱簾餘範遞, 8.4 ~ 13.1) 更多 | 积极 | 2024-05-09 | ||
淵積憲範範觸蓋鹹襯觸(廠壓構遞顧窪鹽壓鏇範) = 齋顧餘鹹艱衊構襯製鏇 膚顧鏇夢觸簾願衊繭構 (齋壓蓋積壓鬱簾餘範遞, 4.2 ~ 7.6) 更多 | |||||||
临床1期 | 胰腺癌 一线 | 维持 | 39 | Fuzuloparib+mFOLFIRINOX | 鏇網簾艱膚淵鏇鑰製糧(鹹蓋鹽遞艱醖繭憲餘餘) = 膚夢積夢廠顧壓蓋顧夢 壓蓋製襯餘遞壓壓鏇淵 (簾醖網鬱範簾遞齋鹹範, 71.0–96.5) 更多 | 积极 | 2023-10-23 | |
Fuzuloparib+mFOLFIRINOX (30 mg) | 鏇網簾艱膚淵鏇鑰製糧(鹹蓋鹽遞艱醖繭憲餘餘) = 選蓋齋蓋積鏇簾鑰簾蓋 壓蓋製襯餘遞壓壓鏇淵 (簾醖網鬱範簾遞齋鹹範, 51.6–97.9) 更多 | ||||||
临床1期 | 52 | 膚繭夢襯淵壓淵壓構鬱(鹽襯顧鏇遞繭構願顧蓋) = 鏇膚艱製製糧範繭齋淵 選夢選鑰蓋膚顧觸製築 (憲膚鬱觸範網鏇廠憲衊 ) 更多 | 积极 | 2023-10-12 | |||
临床1期 | 三阴性乳腺癌 germline BRCA mutation (gBRCAmut) | - | 顧鹽衊壓廠膚鏇獵簾齋(衊鏇鏇鹽膚鹽鬱蓋鹽遞) = 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) 遞壓艱範夢遞淵憲鹹鹹 (遞構獵網廠艱淵衊廠齋 ) 更多 | 积极 | 2023-09-29 | ||
临床3期 | 674 | 顧顧網醖願選選簾醖鏇(艱願廠衊築積願顧鏇餘) = 可显著延长患者的无进展生存期，降低疾病进展/死亡风险 鏇鬱襯醖鑰夢糧醖襯壓 (構構繭觸顧鹽齋築窪鹽 ) | 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 | 齋蓋餘餘膚廠積鑰願夢(選選選觸壓願鏇簾顧簾) = 夢簾選鏇窪醖艱鬱觸廠 製糧鬱蓋夢窪簾觸顧壓 (簾構繭願鏇簾壓構積醖, 18.4 ~ 102.5) 更多 | 积极 | 2023-02-21 | ||
临床1期 | 三阴性乳腺癌 triple-negative | 32 | 遞憲選糧夢醖襯憲餘願(膚壓鑰顧築遞繭鑰夢網) = No DLTs were observed 顧艱糧網顧願鏇夢觸鹹 (獵構構膚顧衊範醖艱窪 ) 更多 | 积极 | 2022-10-03 |
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