氟莱哌素(Fluorapacin) - 药物靶点：Tubulin_在研适应症：肺癌，非小细胞肺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

BFBTS、FLP

靶点

Tubulin

作用机制

微管蛋白抑制剂

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

ACEA Therapeutics, Inc.初创企业

非在研机构

杭州艾森医药研究有限公司

安捷伦生物（杭州）有限公司

ACEA BIO

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床2期

特殊审评-

结构

分子式C14H12F2S3

InChIKeyXCOWUOOCXCXCNS-UHFFFAOYSA-N

CAS号869811-23-4

关联

3

项与氟莱哌素相关的临床试验

CTR20130888 / Recruiting临床1期

氟莱哌素注射液联合培美曲赛治疗晚期NSCLC剂量探索I期临床试验

(1)确定联合给药下氟莱哌素注射液的剂量；(2)确定联合方案的MTD、DLT；(3)考察药代动力学行为并计算药代动力学参数。(4)评估耐受性和安全性。(5)初步考察联合给药的疗效。(6)为Ⅱ期临床提供安全有效的合理方案。

开始日期-

申办/合作机构-

CTR20130893 / Completed临床1期

氟莱哌素注射液Ⅰ期临床试验（持续72h给药）

1)确定本品持续72h给药在人体的耐受性及在人体的剂量限制性毒性2)考察氟莱哌素及其代谢物药代动力学行为3)探讨本品剂量、药代动力学参数与药效的关系4)初步考察氟莱哌素疗效5)为Ⅱ期临床研究提供安全有效的合理方案

开始日期-

申办/合作机构-

NCT01361529 / Unknown status临床1期

Phase 1 Study of FLP Injection on Tumor Patients

The purpose of this study is to determine the tolerance and maximum tolerated dose (MTD) for FLP Injection with multiple dose in tumor patients.

开始日期2009-06-01

申办/合作机构

安捷伦生物（杭州）有限公司

100 项与氟莱哌素相关的临床结果

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100 项与氟莱哌素相关的转化医学

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100 项与氟莱哌素相关的专利（医药）

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72

项与氟莱哌素相关的文献（医药）

2023-12-25·Sheng wu gong cheng xue bao = Chinese journal of biotechnology

[Enzyme production mechanism of anaerobic fungus Orpinomyces sp. YF3 in yak rumen induced by different carbon source].

Article

作者: Wang, Lamei ; Cao, Yangchun ; Zhou, Linlin ; Li, Yong ; Zhao, Congcong ; Yao, Junhu ; DU, Xue'er ; Zhang, Fan

In order to investigate the enzyme production mechanism of yak rumen-derived anaerobic fungus Orpinomyces sp. YF3 under the induction of different carbon sources, anaerobic culture tubes were used for in vitro fermentation. 8 g/L of glucose (Glu), filter paper (Flp) and avicel (Avi) were respectively added to 10 mL of basic culture medium as the sole carbon source. The activity of fiber-degrading enzyme and the concentration of volatile fatty acid in the fermentation liquid were detected, and the enzyme producing mechanism of Orpinomyces sp. YF3 was explored by transcriptomics. It was found that, in glucose-induced fermentation solution, the activities of carboxymethyl cellulase, microcrystalline cellulase, filter paper enzyme, xylanase and the proportion of acetate were significantly increased (P < 0.05), the proportion of propionate, butyrate, isobutyrate were significantly decreased (P < 0.05). The results of transcriptome analysis showed that there were 5 949 differentially expressed genes (DEGs) between the Glu group and the Flp group, 10 970 DEGs between the Glu group and the Avi group, and 6 057 DEGs between the Flp group and the Avi group. It was found that the DEGs associated with fiber degrading enzymes were significantly up-regulated in the Glu group. Gene ontology (GO) function enrichment analysis identified that DEGs were mainly associated with the xylan catabolic process, hemicellulose metabolic process, β-glucan metabolic process, cellulase activity, endo-1,4-β-xylanase activity, cell wall polysaccharide metabolic process, carbohydrate catabolic process, glucan catabolic process and carbohydrate metabolic process. Moreover, the differentially expressed pathways associated with fiber degrading enzymes enriched by Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis were mainly starch and sucrose metabolic pathways and other glycan degradation pathways. In conclusion, Orpinomyces sp. YF3 with glucose as carbon source substrate significantly increased the activity of cellulose degrading enzyme and the proportion of acetate, decreased the proportion of propionate, butyrate and isobutyrate. Furthermore, the degradation ability and energy utilization efficiency of fungus in the presence of glucose were improved by means of regulating the expression of cellulose degrading enzyme gene and participating in starch and sucrose metabolism pathway, and other glycan degradation pathways, which provides a theoretical basis for the application of Orpinomyces sp. YF3 in practical production and facilitates the application of Orpinomyces sp. YF3 in the future.

2023-08-31·The European journal of prosthodontics and restorative dentistry

Mechanical Characteristics of Composite Resins Produced by Additive and Subtractive Manufacturing.

Article

作者: Kιlιçarslan, M A ; Sahin, Z ; Yιkιcι, C ; Ozer, N E

INTRODUCTIONThe aim of the study was to evaluate the mechanical characteristics of resin composites produced by additive and subtractive manufacturing.METHODSSix composite resin materials produced by subtractive (Vita Enamic-VE, Cerasmart-CE, Lava Ultimate-LU) and additive manufacturing (Varseo Smile Crown plus-VSC, Saremco Print Crowntec-SPC, Formlabs 3B Permanent crown-FLP) were selected. The three-point bending test was performed, and surface hardness of test specimens was measured.RESULTSThe flexural strength values of CE, SPC and LU test groups were found to be statistically higher when compared to VE, FLP and VSC test groups (p⟨0.0033). The modulus of elasticity values of the test specimens was listed as VE>LU>CE>SPC>FLP>VSC. The FLP group [35.11(4.46)] had the lowest surface hardness values, whereas the VE group [252.50 (21.5)] had the highest values. Other groups were listed as LU⟩CE⟩SPC⟩VSC in terms of surface hardness.CONCLUSIONSAccording to the ISO 6872:2015, the flexural strengths of all resin composites were found to be acceptable for single unit fixed restorations. However, the VSC group's flexural strength is suitable for inlay, onlay, veneer restorations or single-unit anterior fixed dental prostheses. Also, VSC may not be a suitable choice for posterior restorations due to its low flexural strength.

2023-06-01·Computers in Biology and Medicine

Comparison of the molecular mechanisms of Fuzi Lizhong Pill and Huangqin decoction in the treatment of the cold and heat syndromes of ulcerative colitis based on network pharmacology

Article

作者: Zhou, Bingjie ; Hu, Xiyun ; Qiu, Qimiao ; Liu, Ruining ; Liu, Weidong ; Wu, Fengxu ; Huang, Zunnan ; He, Meiqi

OBJECTIVEThe aim of this study was to illuminate the similarities and differences of two prescriptions as "cold" and "heat" drugs for treating ulcerative colitis (UC) with the simultaneous occurrence of heat and cold syndrome via network pharmacology.METHODS(1) Active compounds of Fuzi-Lizhong Pill (FLP) and Huangqin Decoction (HQT) were retrieved from the TCMSP database, and their common active compounds were compared using the Venn diagram. (2) Potential proteins targeted to three sets of compounds either (i) shared by FLP and HQT, (ii) unique to FLP or (iii) unique to HQT were screened from the STP, STITCH and TCMSP databases, and three corresponding core compound sets were identified in Herb-Compound-Target (H-C-T) networks. (3) Targets related to UC were identified from the DisGeNET and GeneCards databases and compared with the FLP-HQT common targets to identify potential targets of FLP-HQT compounds related to UC. (4) Three potential target sets were imported into the STRING database for protein‒protein interaction (PPI) analysis, and three core target sets were defined. (5) The binding capabilities and interacting modes between core compounds and key targets were verified by molecular docking via Discovery Studio 2019 and molecular dynamics (MD) simulations via Amber 2018. (6) The target sets were enriched for KEGG pathways using the DAVID database.RESULTS(1) FLP and HQT included 95 and 113 active compounds, respectively, with 46 common compounds, 49 FLP-specific compounds and 67 HQT-specific compounds. (2) 174 targets of FLP-HQT common compounds, 168 targets of FLP-specific compounds, and 369 targets of HQT-specific compounds were predicted from the STP, STITCH and TCMSP databases; six core compounds specific to FLP and HQT were screened in the FLP-specific and HQT-specific H-C-T networks, respectively. (3) 103 targets overlapped from the 174 predicted targets and the 4749 UC-related targets; two core compounds for FLP-HQT were identified from the FLP-HQT H-C-T network. (4) 103 FLP-HQT-UC common targets, 168 of FLP-specific targets and 369 of HQT-specific targets had shared core targets (AKT1, MAPK3, TNF, JUN and CASP3) based on the PPI network analysis. (5) Molecular docking demonstrated that naringenin, formononetin, luteolin, glycitein, quercetin, kaempferol and baicalein of FLP and HQT play a critical role in treating UC; meanwhile, MD simulations revealed the stability of protein‒ligand interactions. (6) The enriched pathways indicated that most targets were related to anti-inflammatory, immunomodulatory and other pathways. Compared with the pathways identified using traditional methods, FLP-specific pathways included the PPAR signaling pathway and the bile secretion pathway, and HQT-specific pathways included the vascular smooth muscle contraction pathway and the natural killer cell-mediated cytotoxicity pathway etc. CONCLUSION: In this study, we clarified the common mechanisms of FLP and HQT in treating UC and their specific mechanisms in treating cold and heat syndrome in UC through compound, target and pathway distinction and a literature comparison based on network pharmacology; these results provide a new perspective on the detailed mechanism of "multidrugs and single-disease" thought in traditional Chinese medicine.

100 项与氟莱哌素相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
肺癌	临床2期	中国	ACEA Therapeutics, Inc.初创企业	2022-01-30
肿瘤	临床2期	中国	安捷伦生物（杭州）有限公司	2009-06-01
非小细胞肺癌	临床1期	中国	-	2013-11-13
非小细胞肺癌	临床1期	中国	杭州艾森医药研究有限公司	2013-11-13
晚期恶性实体瘤	药物发现	中国	-	2013-11-13
晚期癌症	药物发现	中国	安捷伦生物（杭州）有限公司	2009-06-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASCO2004	N/A	复发性胃癌一线	111	FLP	(構構襯窪壓齋鏇觸範糧) = 築蓋餘夢齋顧襯憲簾鏇願製衊願窪醖繭壓醖製 (襯壓廠蓋壓淵襯顧餘選 ) 更多	-	2004-07-15
				S-1	(構構襯窪壓齋鏇觸範糧) = 顧艱網願蓋積網網艱壓願製衊願窪醖繭壓醖製 (襯壓廠蓋壓淵襯顧餘選 ) 更多
ASCO2006	临床3期	进展期胃腺癌一线	220	FLO	觸膚積遞鹽遞糧齋齋膚(鏇獵網淵遞構選鏇廠壓) = 獵窪觸鹽鹽糧鑰餘製淵餘製範範製艱遞鑰蓋構 (糧繭廠積廠襯願醖顧製 ) 更多	积极	2006-06-20
				FLP	觸膚積遞鹽遞糧齋齋膚(鏇獵網淵遞構選鏇廠壓) = 壓憲膚壓遞壓膚鏇齋顧餘製範範製艱遞鑰蓋構 (糧繭廠積廠襯願醖顧製 ) 更多