安吖啶(Amsacrine) - 药物靶点：Top II_在研适应症：白血病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

4'-(9-Acridinylamino)-3'-methoxymethanesulfonanilide、4'-(9-Acridinylamino)methanesulfon-m-anisidide、4'-(9-Acridinylamino)methanesulfon-meta-anisidide

+ [22]

靶点

Top II

作用方式

抑制剂

作用机制

Top II抑制剂(拓扑异构酶II抑制剂)

治疗领域

肿瘤血液及淋巴系统疾病

在研适应症

白血病

非在研适应症-

原研机构-

在研机构

Searchlight Pharma, Inc.

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期

加拿大 (1983-12-31),

白血病

最高研发阶段(中国)批准上市

特殊审评孤儿药 (美国)

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结构/序列

分子式C21H20ClN3O3S

InChIKeyWDISRLXRMMTXEV-UHFFFAOYSA-N

CAS号54301-15-4

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关联

10

项与安吖啶相关的临床试验

IRCT20230410057874N1

/ RecruitingN/AIIT

Evaluation of the effectiveness of AMSA injection on patient anesthesia during dental extraction treatment

开始日期2023-07-23

申办/合作机构

Islamic Azad University

NCT05807932

/ Recruiting临床1/2期

Phase-I/II Trial to Assess the Safety and Efficacy of Venetoclax in Addition to Sequential Conditioning With Fludarabine / Amsacrine / Ara-C (FLAMSA) + Treosulfan for Allogeneic Blood Stem Cell Transplantation in Patients With MDS, CMML or sAML (FLAMSAClax

This trial aims to find the MTD of Venetoclax when added to Fludarabin, Amsacrine and Ara-C + Treosulfan and to evaluate whether the addition of Venetoclax to sequential conditioning with FLAMSA + Treosulfan is safe for allogeneic blood stem cell transplantation in patients with high-risk MDS, CMML or sAML (FLAMSAClax)

开始日期2023-06-26

申办/合作机构

Heinrich-Heine-Universität Düsseldorf

NCT03765541

/ Terminated临床3期IIT

Dexamethasone Plus Salvage Chemotherapy Versus Salvage Chemotherapy Alone in Patients With First Relapsed or Refractory Acute Myeloid Leukemia: a Randomized, Controlled, Open-label, Multicenter, Phase III Study

Recent preclinical and retrospective clinical data have suggested that dexamethasone might sensitize leukemic cells to chemotherapy-induced cell death and thus limit the risk of leukemic regrowth and relapse. Moreover, it has been experimentally shown that leukemic cells in acute myeloid leukemia patients who relapse become sensitive to glucocorticoids treatment highlighting a novel potential role for dexamethasone in relapsed or refractory acute myeloid leukemia (R/R).
This study was designed to determine whether adding dexamethasone to standard salvage therapy in the treatment of relapsed/refractory acute myeloid leukemia in adult patients (intensive chemotherapy amsacrine-cytarabine or azacitidine according to investigator's willingness) results in a significant improvement of the overall survival.

开始日期2020-01-13

申办/合作机构

Toulouse University Hospital

100 项与安吖啶相关的临床结果

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100 项与安吖啶相关的转化医学

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100 项与安吖啶相关的专利（医药）

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2,146

项与安吖啶相关的文献（医药）

2025-03-24·Journal of Biomolecular Structure and Dynamics

Inhibition of respiratory syncytial virus by Daclatasvir and its derivatives: synthesis of computational derivatives as a new drug development

Article

作者: Afreen, Shagufta ; Mitra, Debanjan ; Das Mohapatra, Pradeep K. ; Abdalla, Mohnad

The most common cause of respiratory tract illness in newborns and young children is the respiratory syncytial virus (RSV). There is no approved vaccination or specific antiviral medication for RSV infections. Here, an attempt has been made to explore the potential of currently marketed drugs as well as their probable derivatives to improve the possibility of developing stronger medications against RSV. From the 100 synthetic drug compounds library, the best drug molecule was identified through drug-likeness properties, toxicity, molecular docking and molecular dynamics simulations. Molecular Mechanics Generalized Born Surface Area (MM-GBSA) was also a method that was applied in this study. Daclatasvir showed the highest binding energy and appeared as the best drug to inhibit matrix protein and a fusion protein of RSV. Based on Daclatasvir, 40 computational derivatives were made. D28, D34 and D40 showed far better results than the actual drug. Changes in lipophilicity character increase the binding energy of derivatives. Molecular dynamic simulations showed their non-deviated, non-fluctuated and stable complex formation with target proteins. The high number of amino acid contacts throughout the trajectory increases the stability and effectiveness of derivatives. The key to producing a novel medicine to eradicate RSV is provided by derivatives. Daclatasvir will be employed as a potential RSV inhibitor up until that point.

2025-02-14·Organic Letters

Assembly of Biaryl Amines via Mild Copper-Catalyzed Coupling of Anilines with (Hetero)aryl Chlorides/Bromides

Article

作者: Li, Sailuo ; Xu, Lanting ; Ma, Dawei ; An, Bang

CuI/6-hydroxy picolinohydrazide-catalyzed coupling of (hetero)aryl chlorides with anilines proceeded well at 100 °C to afford biaryl amines in a diverse manner, which represents the first example of Cu-catalyzed biaryl amines under milder conditions. The same catalytic system could make the coupling of (hetero)aryl bromides with anilines work at room temperature, giving the corresponding products with an excellent reaction scope.

2025-01-01·Transplantation and Cellular Therapy

Sequential Conditioning With FLAMSA Does Not Improve Outcomes of Allogeneic Stem Cell Transplantation in Chronic Myelomonocytic Leukemia Patients

Article

作者: Steiner, Normann ; Janson, Dietlinde ; Rathje, Kristin ; Wolschke, Christine ; Kröger, Nicolaus ; Massoud, Radwan ; Niederwieser, Christian ; Langebrake, Claudia ; Gagelmann, Nico ; Zeck, Gaby ; Heidenreich, Silke ; Klyuchnikov, Evgeny ; Ayuk, Francis

As with myelodysplastic syndromes (MDS), effective treatment options for chronic myelomonocytic leukemia (CMML) are limited, and the optimal treatment approach remains undefined. Allogeneic stem cell transplantation (allo-SCT) is potentially curative therapy for patients with CMML. Sequential conditioning with FLAMSA was initially developed for refractory acute myeloid leukemia and has since been applied in the treatment of MDS and CMML. Data on optimal allo-SCT conditioning in CMML Patients is scarce. This retrospective study from the Department of Stem Cell Transplantation at the University Medical Center Hamburg, Germany, compared allo-SCT outcomes in CMML patients across three conditioning regimes: Thiotepa-busulfan (TB), sequential FLAMSA-busulfan fludarabine (FLAMSA-FB), and treosulfan-fludarabine (Treo-Flu). Sixty-nine consecutive patients with CMML who underwent allo-SCT between the years 2006 and 2022 were included in the study. Twenty-two received TB, 27 received FLAMSA-FB, and 20 received Treo-Flu conditioning. Transplant sources included matched related donors (8 patients), mismatched related donors (8 all in the TB group), matched unrelated donors (31), and mismatched unrelated donors (22) with significant group variations (P < .001). Most patients received anti-T lymphocyte Globulin for graft versus host disease (GVHD) prophylaxis (TB 68%, FLAMSA-FB 93%, Treo-Flu 85%, P = .08). CPSS-Molecular score was comparable between the groups. One TB patient experienced primary graft failure, but engraftment times were comparable across the groups. Although not statistically significant, the TB group showed a trend toward improved 3-year overall survival (OS) rates (80%) compared to FLAMSA-FB (37%) and Treo-Flu (55%) (P = .05). The TB group also displayed significantly higher 3-year progression-free survival (PFS) rates (80%) compared to FLAMSA-FB (33%) and Treo-Flu (both 39%), (P = .02). No significant differences were observed in 3-year non-relapse mortality across the TB (20%), FLAMSA-FB (30%), and Treo-Flu (26%) groups (P = .8). Interestingly, no TB patients relapsed at 3 years, contrasting with the FLAMSA-FB (41%) and Treo-Flu groups (30%, P = .02). Lastly, cumulative incidences of acute and chronic GVHD were similar across groups. Our analysis suggests FLAMSA-FB does not improve transplant outcomes, however, TB represents the preferred conditioning regimen for CMML patients undergoing allo-SCT. It demonstrates notable advantages in relapse prevention and leads to improved OS and PFS compared to FLAMSA-FB and Treo-Flu protocols.

100 项与安吖啶相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02321	安吖啶	L01XX01	DB00276

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
白血病	加拿大	Searchlight Pharma, Inc.	1983-12-31

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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


P273 (EBMT2023)	N/A	肿瘤	41	FLAMSA+Alkylator+Venetoclax	鹽衊繭鹹艱醖鑰獵築蓋(淵襯鏇夢鹽艱艱構壓構) = 鏇齋製壓艱願齋憲壓襯願壓積願繭廠廠鏇蓋憲 (構醖壓艱醖構餘鏇簾齋 ) 更多	-	2023-04-23
EBMT2022	N/A	-	11	Venetoclax + FLAMSA + alkylator	繭艱鬱遞襯艱鏇鹽艱積(餘繭窪艱膚構壓餘蓋觸) = 憲鹹齋製觸淵糧積衊網蓋蓋壓膚淵齋窪蓋醖蓋 (範壓顧製鬱夢築膚淵築 ) 更多	-	2022-03-19
NCT00180102 (AML2003, Pubmed \| J Clin Oncol)	临床4期	急性髓性白血病巩固	-	Standard high-dose cytarabine consolidation	繭願簾製簾繭廠鬱獵鑰(壓醖憲糧襯衊蓋範襯觸) = 構廠憲網夢鬱網襯鹹鹹窪鏇選範衊襯醖鹹醖餘 (艱廠鑰壓壓醖廠網觸蓋 ) 更多	不佳	2013-06-10
NCT00180102 (AML2003, Pubmed \| J Clin Oncol)	临床4期	急性髓性白血病巩固	-	Multiagent consolidation with mitoxantrone and amsacrine	繭願簾製簾繭廠鬱獵鑰(壓醖憲糧襯衊蓋範襯觸) = 壓遞窪繭衊鬱繭繭鹹顧窪鏇選範衊襯醖鹹醖餘 (艱廠鑰壓壓醖廠網觸蓋 ) 更多	不佳	2013-06-10
Tandem Meetings ASTCT and CIBMTR2012	N/A	难治性高危骨髓增生异常综合征	40	FLAMSA sequential chemotherapy	(膚齋餘網繭簾鑰鏇鏇鹽) = 鑰獵遞餘網廠壓遞夢鹽鬱糧壓築蓋餘獵鑰願醖 (窪襯餘選遞獵鑰壓憲鏇, 17 ~ 52) 更多	积极	2012-02-01
Tandem Meetings ASTCT and CIBMTR2012	N/A	难治性高危骨髓增生异常综合征	40	Flamsa (Reduced-Intensity Conditioning (RIC) regimen with TBI)	觸鏇憲構鬱艱鬱獵製顧(廠廠膚範繭膚遞積醖範) = 鑰糧夢鑰艱鹹壓廠願鹹願襯顧鬱積窪選鹽鬱餘 (範鏇淵醖鏇窪繭蓋夢淵, 8 ~ 20)	积极	2012-02-01