硫蒽酮(Lucanthone) - 药物靶点：APE1 x Top II_专利_临床

概要

基本信息

药物类型

小分子化药

别名

1-((2-(Diethylamino)ethyl)amino)-4-methylthioxanthen-9-one、1-diethylaminoethylethylamino-4-methyl-thioxanthenone、1-{[2-(diethylamino)ethyl]amino}-4-methylthioxanthen-9-one

+ [2]

靶点

APE1 x Top II

作用机制

APE1抑制剂(DNA-(无嘌呤或无嘧啶位点)裂合酶抑制剂)、Top II抑制剂(拓扑异构酶II抑制剂)

治疗领域

肿瘤神经系统疾病呼吸系统疾病+ [2]

在研适应症-

非在研适应症

脑癌脑转移瘤乳腺癌+ [2]

原研机构

Arisyn Therapeutics Inc

在研机构-

非在研机构

Spectrum Pharmaceuticals, Inc.Arisyn Therapeutics Inc

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C20H24N2OS

InChIKeyFBQPGGIHOFZRGH-UHFFFAOYSA-N

CAS号479-50-5

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关联

3

项与硫蒽酮相关的临床试验

NCT02014545 / Withdrawn临床2期IIT

Phase II Trial Evaluating the Addition of Lucanthone to Whole Brain Radiation Therapy in Patients With Brain Metastases From Non-Small Cell Lung Cancer

This is a randomized, double blind placebo controlled study to evaluate safety and efficacy of lucanthone administered as an adjunct to patients receiving whole brain radiation therapy (WBRT) as primary treatment for brain metastases secondary to non-small cell lung cancer.

开始日期2016-01-01

申办/合作机构

Wake Forest School of Medicine

[+1]

NCT01587144 / Terminated临床2期

An International, Multi-Center, Randomized, Double Blind Placebo Controlled Phase II Study to Evaluate the Safety and Efficacy of Lucanthone Administered as an Adjunct to Radiation and Temozolomide for Primary Therapy of Glioblastoma Multiforme

The purpose of the study is to determine the effectiveness of an investigational drug called lucanthone, when combined with temozolomide (TMZ) and radiation in the treatment of Glioblastoma Multiforme (GBM).

开始日期2012-06-19

申办/合作机构

Spectrum Pharmaceuticals, Inc.

CTRI/2012/04/002616 / Terminated临床2期

An International, Multi-Center, Randomized, Double Blind Placebo Controlled Phase II Study to Evaluate the Safety and Efficacy of Lucanthone Administered as an Adjunct to Radiation and Temozolomide for Primary Therapy of Glioblastoma Multiforme

开始日期2012-05-15

申办/合作机构

Spectrum Pharmaceuticals, Inc.

100 项与硫蒽酮相关的临床结果

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100 项与硫蒽酮相关的转化医学

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100 项与硫蒽酮相关的专利（医药）

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140

项与硫蒽酮相关的文献（医药）

2024-08-02·Medicine

Investigation of the relationship between COVID-19 and pancreatic cancer using bioinformatics and systems biology approaches

Article

作者: Wu, Xuehu ; Wen, Jing ; Wu, Qian ; Sun, Haiyan ; Zhai, Dongsheng ; Fang, Chengxiang

Background:The coronavirus disease 2019 (COVID-19) pandemic, caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus, poses a huge threat to human health. Pancreatic cancer (PC) is a malignant tumor with high mortality. Research suggests that infection with SARS-CoV-2 may increase disease severity and risk of death in patients with pancreatic cancer, while pancreatic cancer may also increase the likelihood of contracting SARS-CoV-2, but the link is unclear.Methods:This study investigated the transcriptional profiles of COVID-19 and PC patients, along with their respective healthy controls, using bioinformatics and systems biology approaches to uncover the molecular mechanisms linking the 2 diseases. Specifically, gene expression data for COVID-19 and PC patients were obtained from the Gene Expression Omnibus datasets, and common differentially expressed genes (DEGs) were identified. Gene ontology and pathway enrichment analyses were performed on the common DEGs to elucidate the regulatory relationships between the diseases. Additionally, hub genes were identified by constructing a protein–protein interaction network from the shared DEGs. Using these hub genes, we conducted regulatory network analyses of microRNA/transcription factors-genes relationships, and predicted potential drugs for treating COVID-19 and PC.Results:A total of 1722 and 2979 DEGs were identified from the transcriptome data of PC (GSE119794) and COVID-19 (GSE196822), respectively. Among these, 236 common DEGs were found between COVID-19 and PC based on protein–protein interaction analysis. Functional enrichment analysis indicated that these shared DEGs were involved in pathways related to viral genome replication and tumorigenesis. Additionally, 10 hub genes, including extra spindle pole bodies like 1, holliday junction recognition protein, marker of proliferation Ki-67, kinesin family member 4A, cyclin-dependent kinase 1, topoisomerase II alpha, cyclin B2, ubiquitin-conjugating enzyme E2 C, aurora kinase B, and targeting protein for Xklp2, were identified. Regulatory network analysis revealed 42 transcription factors and 23 microRNAs as transcriptional regulatory signals. Importantly, lucanthone, etoposide, troglitazone, resveratrol, calcitriol, ciclopirox, dasatinib, enterolactone, methotrexate, and irinotecan emerged as potential therapeutic agents against both COVID-19 and PC.Conclusion:This study unveils potential shared pathogenic mechanisms between PC and COVID-19, offering novel insights for future research and therapeutic strategies for the treatment of PC and SARS-CoV-2 infection.

2023-01-01·Frontiers in medicine

The influence of COVID-19 on colorectal cancer was investigated using bioinformatics and systems biology techniques.

Article

作者: Wu, Tian ; Du, Ao ; Huang, Tengda ; Zhou, Xinyi ; Xue, Shuai ; Lv, Yue ; Song, Yujia ; Pan, Hongyuan ; Yuan, Kefei ; Lan, Jiang

IntroductionCoronavirus disease 2019 (COVID-19) is a global pandemic and highly contagious, posing a serious threat to human health. Colorectal cancer (CRC) is a risk factor for COVID-19 infection. Therefore, it is vital to investigate the intrinsic link between these two diseases.MethodsIn this work, bioinformatics and systems biology techniques were used to detect the mutual pathways, molecular biomarkers, and potential drugs between COVID-19 and CRC.ResultsA total of 161 common differentially expressed genes (DEGs) were identified based on the RNA sequencing datasets of the two diseases. Functional analysis was performed using ontology keywords, and pathway analysis was also performed. The common DEGs were further utilized to create a protein-protein interaction (PPI) network and to identify hub genes and key modules. The datasets revealed transcription factors-gene interactions, co-regulatory networks with DEGs-miRNAs of common DEGs, and predicted possible drugs as well. The ten predicted drugs include troglitazone, estradiol, progesterone, calcitriol, genistein, dexamethasone, lucanthone, resveratrol, retinoic acid, phorbol 12-myristate 13-acetate, some of which have been investigated as potential CRC and COVID-19 therapies.DiscussionBy clarifying the relationship between COVID-19 and CRC, we hope to provide novel clues and promising therapeutic drugs to treat these two illnesses.

2023-01-01·Frontiers in immunology

Identifying hub genes and common biological pathways between COVID-19 and benign prostatic hyperplasia by machine learning algorithms.

Article

作者: Li, Yuezheng ; Xu, Mingming ; Ren, Congzhe ; Zhou, Hang ; Wang, Shangren ; Pan, Yang ; Li, Muwei ; Hu, Ping ; Liu, Xiaoqiang

BackgroundCOVID-19, a serious respiratory disease that has the potential to affect numerous organs, is a serious threat to the health of people around the world. The objective of this article is to investigate the potential biological targets and mechanisms by which SARS-CoV-2 affects benign prostatic hyperplasia (BPH) and related symptoms.MethodsWe downloaded the COVID-19 datasets (GSE157103 and GSE166253) and the BPH datasets (GSE7307 and GSE132714) from the Gene Expression Omnibus (GEO) database. In GSE157103 and GSE7307, differentially expressed genes (DEGs) were found using the "Limma" package, and the intersection was utilized to obtain common DEGs. Further analyses followed, including those using Protein-Protein Interaction (PPI), Gene Ontology (GO) function enrichment analysis, and the Kyoto Encyclopedia of Genes and Genomes (KEGG). Potential hub genes were screened using three machine learning methods, and they were later verified using GSE132714 and GSE166253. The CIBERSORT analysis and the identification of transcription factors, miRNAs, and drugs as candidates were among the subsequent analyses.ResultsWe identified 97 common DEGs from GSE157103 and GSE7307. According to the GO and KEGG analyses, the primary gene enrichment pathways were immune-related pathways. Machine learning methods were used to identify five hub genes (BIRC5, DNAJC4, DTL, LILRB2, and NDC80). They had good diagnostic properties in the training sets and were validated in the validation sets. According to CIBERSORT analysis, hub genes were closely related to CD4 memory activated of T cells, T cells regulatory and NK cells activated. The top 10 drug candidates (lucanthone, phytoestrogens, etoposide, dasatinib, piroxicam, pyrvinium, rapamycin, niclosamide, genistein, and testosterone) will also be evaluated by the P value, which is expected to be helpful for the treatment of COVID-19-infected patients with BPH.ConclusionOur findings reveal common signaling pathways, possible biological targets, and promising small molecule drugs for BPH and COVID-19. This is crucial to understand the potential common pathogenic and susceptibility pathways between them.

100 项与硫蒽酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	硫蒽酮	-	DB04967

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
非小细胞肺癌	临床2期	美国	Spectrum Pharmaceuticals, Inc.	2016-01-01
多形性胶质母细胞瘤	临床2期	美国	Spectrum Pharmaceuticals, Inc.	2012-06-19
多形性胶质母细胞瘤	临床2期	印度	Spectrum Pharmaceuticals, Inc.	2012-06-19
脑癌	临床2期	-	Arisyn Therapeutics Inc	-
脑癌	临床2期	-	Spectrum Pharmaceuticals, Inc.	-
脑转移瘤	临床2期	美国	-	-
乳腺癌	临床2期	美国	Spectrum Pharmaceuticals, Inc.	-