葡萄糖酸铜/双硫仑(Copper Gluconate/Disulfiram) - 药物靶点：ADHs_在研适应症：乳腺癌，胶质母细胞瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

DSF-Cu、Dicopp、Disulfiram/copper gluconate

+ [2]

靶点

ADHs

作用机制

ADHs抑制剂(乙醇脱氢酶家族抑制剂)

治疗领域

肿瘤神经系统疾病皮肤和肌肉骨骼疾病+ [1]

在研适应症

非在研适应症

原研机构

在研机构

非在研机构

Cantex Pharmaceuticals, Inc.

最高研发阶段临床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/序列

分子式C12H22CuO14

InChIKeyOCUCCJIRFHNWBP-IYEMJOQQSA-L

CAS号527-09-3

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关联

2

项与葡萄糖酸铜/双硫仑相关的临床试验

NCT03714555

/ Terminated临床2期IIT

A Phase II Pilot Study of Disulfiram and Copper Gluconate in Patients With Metastatic Pancreatic Cancer and Rising CA-19-9 Levels While Receiving Abraxane-Gemcitabine or FOLFIRINOX or Single-Agent Gemcitabine

This is an open-label Phase 2 Pilot study to evaluate Disulfiram + Copper Gluconate in patients metastatic pancreatic cancer whose CA-19-9 levels rise while receiving nab-paclitaxel (Abraxane) plus gemcitabine (Gemzar) or FOLFIRINOX or single-agent gemcitabine (Gemzar). Patient must have received a minimum of 8 weeks of treatment and have rising CA-19-9 levels in the absence of radiographic evidence of progression.

开始日期2019-10-17

申办/合作机构

Scottsdale Healthcare Corp.

[+1]

NCT03034135

/ Completed临床2期

A Phase II, Multicenter, Open-Label, Single-Arm Study to Evaluate the Safety, Tolerability, and Efficacy of DIsulfiram and Copper Gluconate in Recurrent Glioblastoma

This study of DSF-Cu in combination with TMZ for recurrent GBM will evaluate the antitumor effect in patients who have recurrent GBM. Patients will take DSF-Cu daily during their routine standard of care with TMZ therapy for approximately 6 months. Patients will be evaluated for response every 8 weeks. Patients will be followed up 2 years after the last dose of DSF-Cu.

开始日期2017-03-09

申办/合作机构

Cantex Pharmaceuticals, Inc.

100 项与葡萄糖酸铜/双硫仑相关的临床结果

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100 项与葡萄糖酸铜/双硫仑相关的转化医学

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100 项与葡萄糖酸铜/双硫仑相关的专利（医药）

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634

项与葡萄糖酸铜/双硫仑相关的文献（医药）

2025-12-01·Lung

Disulfiram Alleviates MTX-Induced Pulmonary Fibrosis by Inhibiting EMT in Type 2 Alveolar Epithelial Cells

Article

作者: Ma, Ziyi ; Zhang, Linyi ; Lan, Kai ; Li, Rong ; Wu, Xiaohui ; Wang, Chunyang ; Xu, Hong ; Chen, Min ; Zhang, Zhaohua

PURPOSEMethotrexate (MTX)-induced pulmonary fibrosis is associated with high morbidity and mortality, with limited treatment options available. This study investigates whether disulfiram (DSF) can mitigate MTX-induced pulmonary fibrosis and explores the underlying mechanisms.METHODSEight-week-old male mice were divided into control, DSF, MTX, and MTX+DSF groups and treated for 8 weeks. Weight, food, and water intake were monitored. Post-treatment, lung tissues were analyzed using HE and Masson staining, and electron microscopy. Real-time qPCR and ELISA were employed to assess inflammatory markers such as IL-1β and TNF-α in lung tissues and serum. PCR, ELISA, and Western blot were used for fibrotic markers including Col1α1, α-SMA, and hydroxyproline. Type 2 alveolar epithelial cell line MLE12 cells were similarly grouped, followed by RNA sequencing and bioinformatics analysis to elucidate the mechanisms by which DSF exerts anti-MTX-induced pulmonary fibrosis effects. ELISA and Western blot were used to measure E-cadherin and α-SMA expression.RESULTSDSF significantly reduced MTX-induced alveolar septal thickening, pulmonary fibrosis, and inflammatory cell infiltration. It also decreased the expression of inflammatory factors IL-1β and TNF-α, as well as the expression of Col1α1, α-SMA, and others. RNA-seq revealed that DSF induces changes in multiple signaling pathways associated with pulmonary fibrosis, particularly in extracellular matrix-related genes. ELISA and Western blot showed decreased E-cadherin and increased α-SMA in the MTX group, which was partially restored with DSF treatment.CONCLUSIONDSF alleviates MTX-induced pulmonary fibrosis by reducing epithelial-mesenchymal transition (EMT) in type 2 alveolar epithelial cells. Disulfiram shows potential as a therapeutic agent for MTX-induced pulmonary fibrosis.

2025-03-01·Journal of Colloid and Interface Science

A novel reactive oxygen species nano-amplifier for tumor-targeted photoacoustic imaging and synergistic therapy

Article

作者: Fan, Yadi ; Zhang, Li ; Yang, Mo ; Yang, Zhe ; Wong, Chun-Yuen

Intracellular redox homeostasis and the type of exogenous Fenton reagent play crucial roles in determining the efficacy of chemodynamic therapy (CDT). Herein, we succeeded for the first time in preparing ultrasmall copper sulfide (CuS) nanodots (1-2 nm)-embedded hollow mesoporous organosilica nanoparticle (HMON), which served as an ideal nanocarrier to load both 3-amino-1,2,4-triazole (3-AT) and disulfiram (DSF) after folate-polyethylene glycol-silane (FA-PEG-Silane) modification. The as-prepared nanoplatform (3-AT/DSF@CuS/HMON-FA, denoted as ADCuSi-FA) was found to regulate intracellular redox homeostasis once internalized by 4T1 cells, showing rapid glutathione (GSH)-responsive 3-AT, DSF and Cu⁺ ions release. Specifically, 3-AT restrained the endogenous hydrogen peroxide (H₂O₂) consumption by suppressing catalase (CAT) activity, thereby augmenting hydroxyl radical (OH) generation via Cu⁺-based Fenton-like reaction. DSF, upon complexation with Cu²⁺, exhibited enhanced chemotherapeutic efficacy, while the by-product Cu⁺ ions further boosted the efficacy of CDT. Additionally, CuS nanodots enabled near-infrared-II (NIR-II) photothermal therapy (PTT) and facilitated photoacoustic (PA) imaging, with the ensuing hyperthermia expediting the CDT process. As expected, the tumor growth was dramatically inhibited with PTT/chemotherapy co-synergized CDT. This work offers an innovative paradigm for cooperative cancer treatment as well as new insights into the fabrication of biodegradable inorganic/organic hybrid materials.

2025-02-01·Cancer Letters

Disulfiram impairs USP21-mediated MOF-K257 deubiquitination to inhibit esophageal squamous cell carcinoma progression

Article

作者: Zhu, Yilin ; Sui, Huacong ; Zhang, Yifan ; Mu, Ning ; Zhao, Xiaogang ; Jiang, Yunfeng ; Zhao, Yunpeng ; Tian, Zhongxian ; Fan, Guangyan ; Yang, Lingxiao ; Ding, Yi ; Hong, Yilang ; Song, Xiangqing ; Wang, Jiaxu ; Li, Peichao ; Zhao, Shuyong ; Cui, Xiujie

Disulfiram (DSF), primarily applied in the therapy for alcohol addiction, has been demonstrated to possess the promising capability of anti-tumor in many human cancers, including esophageal squamous cell carcinoma (ESCC). To date, almost all studies about DSF in ESCC are focusing on investigating either drug combinations or nanoparticle-based delivery systems. However, the exact molecular mechanisms mediating the response to DSF in ESCC are totally unknown. An increasing number of studies reported that aberrant expression of acetylation-related genes is closely involved in regulating the response of cancer cells to anti-tumor drugs. Here, we defined DSF-sensitive and -resistant cells by measuring the half-maximal inhibitory concentration (IC₅₀) of DSF in four ESCC cell lines, followed by detecting the protein expression of nine dysregulated histone acetyltransferase (HAT) genes in ESCC. Our results demonstrate that MOF is responsible for the sensitivity to DSF in ESCC cells. Consistently, DSF treatment markedly abolished MOF-driving ESCC progression and Wnt/β-Catenin signaling activation. Interestingly, DSF decreased MOF protein expression via the ubiquitin-proteasome system. Further exploration verified the essential role of USP21, among three candidates (USP2, USP21, and USP10), in DSF-mediated MOF protein levels. Mechanistically, USP21 binds to MOF protein and decreases the ubiquitination of its K257 site, while DSF notably impedes MOF-mediated ESCC malignant progression and Wnt/β-Catenin signaling activation by blocking USP21-governed MOF-K257 deubiquitination. In conclusion, our study elucidates the USP21/MOF-K257 axis regulating the response to DSF in ESCC, which provides novel and key evidence for the clinical application of DSF in individualized therapy for ESCC patients.

1

项与葡萄糖酸铜/双硫仑相关的新闻（医药）

2021-09-14

·BioSpace

Cantex Pharmaceuticals Announces Sale of Equity Interest in Chimerix, Inc.

WESTON, Fla., Sept. 14, 2021 /PRNewswire/ -- Cantex Pharmaceuticals ("Cantex") today announced that it has sold 6.5 million shares of Chimerix, Inc., in brokerage transactions at a price of $5.75 per share, less brokerage commissions and fees. About Cantex Pharmaceuticals Cantex Pharmaceuticals, Inc. is a privately-held, clinical stage pharmaceutical company focused on the transformation of known drugs into innovative products with blockbuster potential. Cantex is currently developing novel cancer treatments. Cantex's pipeline consists of three product candidates in Phase 2 and Phase 3 development for diseases with significant unmet medical needs: Azeliragon for life-threatening and disabling complications of cancer, Dicopp® for hematologic malignancies, and DSTAT, licensed to Chimerix, Inc., as a first-line therapy of acute myeloid leukemia. For more information, please visit . Cantex Contacts Investors: Stephen G. Marcus, M.D. (954) 315-3660 smarcus@cantex.com or Media: Jason Rando Tiberend Strategic Advisors (917) 930-6346 jrando@tiberend.com

100 项与葡萄糖酸铜/双硫仑相关的药物交易

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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
乳腺癌	临床2期	-	CANTEX, Inc.	-
胶质母细胞瘤	临床2期	-	CANTEX, Inc.	-
转移性胰腺癌	药物发现	美国	Cantex Pharmaceuticals, Inc.	2019-10-17
复发性胶质母细胞瘤	药物发现	美国	Cantex Pharmaceuticals, Inc.	2017-03-09

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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


NCT03714555 (CTgov)	临床2期	转移性胰腺癌	1	AE Assessment+nab-paclitaxel+disulfiram/copper gluconate+Gemzar+Disulfiram+gemcitabine+Copper Gluconate (Nab-Paclitaxel/Gemcitabine + DSF/Cu)	獵構築糧淵餘憲壓淵艱(積積構遞膚醖獵鑰窪簾) = 願鑰襯鑰鑰鏇衊觸膚範齋繭獵鑰艱獵夢願廠憲 (壓遞網艱網觸製網衊醖, 觸構觸糧築夢願鹽築繭 ~ 廠鬱製淵膚廠網願衊夢) 更多	-	2023-10-18
				AE Assessment+nab-paclitaxel+disulfiram/copper gluconate+Gemzar+Disulfiram+gemcitabine+Copper Gluconate (FOLFIRINOX +DSF/Cu)	獵構築糧淵餘憲壓淵艱(積積構遞膚醖獵鑰窪簾) = 糧構鏇獵糧顧網觸鏇選齋繭獵鑰艱獵夢願廠憲 (壓遞網艱網觸製網衊醖, 蓋鏇廠衊淵蓋壓鏇艱繭 ~ 餘鑰選簾遞鏇衊餘鏇糧) 更多
NCT03034135 (ACTR-21, CTgov)	临床2期	复发性胶质母细胞瘤	23	Temozolomide (TMZ)+Disulfiram/Copper	(遞鏇繭餘夢蓋糧醖窪鹹) = 淵簾壓憲簾淵獵築鬱襯壓鹽憲鹹獵網醖襯構膚 (築廠鏇構觸遞夢衊窪窪, 構鹹製鬱觸夢網餘製糧 ~ 艱構淵膚鏇選窪鬱窪選) 更多	-	2021-09-13
EXTH-61 (SNO2020)	N/A	复发性髓母细胞瘤 ALDH \| Nestin- \| CD133-positive	-	Disulfiram	選襯廠築觸齋鹽簾積淵(鬱壓襯壓願襯範築獵選) = DSF/Cu++ induced cell death (increased AnnV/PI, cleaved-Poly(ADP-ribose)polymerase fraction, and Apoptosis Inducing Factor on WB/FC/IF, in vitro and ex vivo) through NPL4 accumulation in cell nucleus and intracellular buildup of poly-ubiquitylated proteins 憲遞鹽餘糧廠壓簾構憲 (艱觸蓋願鹽繭選網窪鏇 ) 更多	积极	2020-11-09
				Copper
PDTM-06 (SNO2019)	N/A	髓母细胞瘤	24	Disulfiram-Copper (DSF-Cu++)	憲襯壓鏇築鏇簾範衊製(積鬱憲蓋糧襯積憲糧糧) = 糧艱顧繭醖製齋鹽鹽襯糧齋簾鑰鬱顧醖襯窪窪 (蓋窪鑰鬱壓鹽襯顧鬱鑰 )	积极	2019-11-11
				Disulfiram-Copper (Control (No treatment))	憲襯壓鏇築鏇簾範衊製(積鬱憲蓋糧襯積憲糧糧) = 壓願範製顧夢膚糧願衊糧齋簾鑰鬱顧醖襯窪窪 (蓋窪鑰鬱壓鹽襯顧鬱鑰 )