Delving into the Latest Updates on Amsacrine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

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

+ [22]

Target

Top II

Action

inhibitors

Mechanism

Top II inhibitors(Topoisomerase II inhibitors)

Therapeutic Areas

NeoplasmsHemic and Lymphatic Diseases

Active Indication

Leukemia

Inactive Indication-

Originator Organization-

Active Organization

Searchlight Pharma, Inc.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Canada (31 Dec 1983),

Leukemia

RegulationOrphan Drug (United States)

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Structure/Sequence

Molecular FormulaC21H20ClN3O3S

InChIKeyWDISRLXRMMTXEV-UHFFFAOYSA-N

CAS Registry54301-15-4

View All Structures (2)

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)

Start Date26 Jun 2023

Sponsor / Collaborator

Heinrich-Heine-Universität Düsseldorf

NCT03765541

/ TerminatedPhase 3IIT

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.

Start Date13 Jan 2020

Sponsor / Collaborator

Toulouse University Hospital

100 Clinical Results associated with Amsacrine

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100 Translational Medicine associated with Amsacrine

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100 Patents (Medical) associated with Amsacrine

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2,146

Literatures (Medical) associated with Amsacrine

24 Mar 2025·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

Author: 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.

14 Feb 2025·Organic Letters

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

Article

Author: 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.

01 Jan 2025·Transplantation and Cellular Therapy

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

Article

Author: 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 Deals associated with Amsacrine

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External Link

KEGG	Wiki	ATC	Drug Bank
D02321	Amsacrine	L01XX01	DB00276

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Leukemia	Canada	Searchlight Pharma, Inc.	31 Dec 1983

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


P273 (EBMT2023)	Not Applicable	Neoplasms	41	FLAMSA+Alkylator+Venetoclax	ouqxyirfid(cbbowmjkdi) = xdbkbspbql bdfwyjijpg (grlehapfzt ) View more	-	23 Apr 2023
EBMT2022	Not Applicable	-	11	Venetoclax + FLAMSA + alkylator	cqrqqdusbz(rtfdvbpssv) = hyhkqiujxt mrmwucqgoq (ttwtpwnoxl ) View more	-	19 Mar 2022
NCT00180102 (AML2003, Pubmed \| J Clin Oncol)	Phase 4	Acute Myeloid Leukemia Consolidation	-	Standard high-dose cytarabine consolidation	pmaribianf(fntylmrezw) = fhbwrieyid zjonjsnwzg (bfthgtcuqp ) View more	Negative	10 Jun 2013
NCT00180102 (AML2003, Pubmed \| J Clin Oncol)	Phase 4	Acute Myeloid Leukemia Consolidation	-	Multiagent consolidation with mitoxantrone and amsacrine	pmaribianf(fntylmrezw) = bjrrgdkhtz zjonjsnwzg (bfthgtcuqp ) View more	Negative	10 Jun 2013
Tandem Meetings ASTCT and CIBMTR2012	Not Applicable	Refractory High Risk Myelodysplastic Syndrome	40	FLAMSA sequential chemotherapy	(xypxysaopd) = rvcwtolvij ukhtgdztkd (cmkdhequzb, 17 - 52) View more	Positive	01 Feb 2012
Tandem Meetings ASTCT and CIBMTR2012	Not Applicable	Refractory High Risk Myelodysplastic Syndrome	40	Flamsa (Reduced-Intensity Conditioning (RIC) regimen with TBI)	orjakrwajy(dhllrrphom) = kmdaozrpoc yoppqipkol (paunxhmqxb, 8 - 20)	Positive	01 Feb 2012