Imexon(Imexon) - 药物靶点：核糖核苷酸还原酶复合体_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Imexon (USAN/INN)

+ [2]

靶点

核糖核苷酸还原酶复合体

作用机制

RNR抑制剂(核糖核苷酸还原酶复合体抑制剂)

治疗领域

肿瘤免疫系统疾病心血管疾病+ [6]

在研适应症-

非在研适应症

晚期胰腺腺癌乳腺癌去势抵抗性前列腺癌+ [4]

原研机构

AmpliMed Corp.

在研机构-

非在研机构

AmpliMed Corp.

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)-

特殊审评孤儿药 (欧盟)

结构

分子式C4H5N3O

InChIKeyBIXBBIPTYBJTRY-UHFFFAOYSA-N

CAS号59643-91-3

关联

8

项与 Imexon 相关的临床试验

NCT01314014 / Completed临床2期IIT

A Phase II Study of Amplimexon® (Imexon for Injection) for the Treatment of Previously Treated Follicular and Aggressive Lymphoma in Adults

The purpose of this study is to determine whether Amplimexon (imexon for injection) is effective in the treatment of indolent and aggressive lymphomas that have progressed after treatment with standard therapies.

开始日期2011-05-01

申办/合作机构

University of Rochester

[+1]

NCT00697060 / Withdrawn临床2期

A Multicenter, Phase II Trial of the Safety and Efficacy of Amplimexon® (Imexon for Injection) in Combination With Taxotere® (Docetaxel) for Previously Treated Patients With Metastatic Non-Small Cell Lung Cancer (NSCLC)

Protocol AMP-024 is a Phase 2 study of imexon plus docetaxel for patients with previously treated lung cancer that has spread in the body. Docetaxel is approved by the Food and Drug Administration (FDA) as a second line therapy for this cancer. The imexon is administered on days 1-5 and the docetaxel on day 1 of every 3 week cycle. The objective of the protocol is to determine if the combination of imexon plus docetaxel is safe and effective.

开始日期2010-08-01

申办/合作机构

AmpliMed Corp.

NCT00637247 / Completed临床2期

A Phase 2 Randomized, Double-Blind, Multicenter Trial of Amplimexon® Plus Gemcitabine Versus Gemcitabine Plus Placebo in Patients With Metastatic Chemotherapy Naïve Pancreatic Adenocarcinoma (Stage IV)

The purpose of this study is to determine if imexon in combination with gemcitabine could improve overall survival as compared to gemcitabine alone in subjects with pancreatic cancer that has spread to other organs such as the liver or lungs. The study will also look at the safety of the combination as compared to gemcitabine alone. Participants in the study will be randomly assigned to either treatment and neither the participant or their doctors will know which treatment they will be receiving.

开始日期2008-04-01

申办/合作机构

AmpliMed Corp.

100 项与 Imexon 相关的临床结果

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100 项与 Imexon 相关的转化医学

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100 项与 Imexon 相关的专利（医药）

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57

项与 Imexon 相关的文献（医药）

2022-07-01·The FASEB Journal

A pan‐cancer analysis identifies HDAC11 as an immunological and prognostic biomarker

Article

作者: Xue, Kai ; Li, Ran ; Wu, Xiaolu ; Zhao, Ping ; Li, Junmin

AbstractHistone deacetylase 11 (HDAC11) is aberrantly expressed in many types of cancer, and such abnormalities are associated with tumor immunity and heterogeneous clinical outcomes. Here, we explore the prognostic value and immunological function of HDAC11 across 33 cancer types. We observe HDAC11 is aberrantly expressed in 25 cancer types and positively or negatively associated with prognosis in different cancers. HDAC11 played a protective prognostic role in KIRP, KIRC, LGG, PCPG, READ, and UVM, which was contrary to the conventional opinion that HDAC11 was an oncogenic gene. Moreover, HDAC11 is negatively associated with tumor immune components, most immune checkpoint genes, and key cytokine expression. HDAC11 is correlated with tumor mutational burden in 11 cancer types and with microsatellite instability in 9 cancer types, suggesting HDAC11 may affect a patient's response to immune checkpoint inhibitor (ICI) therapy. In addition, HDAC11 is negatively correlated with the drug sensitivity of oxaliplatin, carmustine, ifosfamide, imexon, lomustine, and BN‐2629, indicating the potential synergy between HDAC11 inhibitors and these anti‐tumor drugs. In vitro assays indicate that HDAC11 inhibitor SIS17 combined with oxaliplatin shows a synergistic cytotoxic role in K562 cells while SIS17 has an antagonistic effect on the cytotoxic role of oxaliplatin in 769P cells. HDAC11 is also associated with hallmark pathways, including epithelial mesenchymal transition, IL‑6/JAK/STAT3, and allograft rejection pathways. Overall, we provide clues regarding the key role of HDAC11 in multiple cancers.

2022-01-01·American journal of translational research

Identification of differentially expressed autophagy genes associated with osteogenic differentiation in human bone marrow mesenchymal stem cells.

Article

作者: Liu, Hongliang ; Li, Ming ; Li, Zhong ; Wang, Qian ; Huang, Qiang ; Ma, Teng ; Zhang, Kun ; Wang, Zhimeng ; Wang, Yakang ; Ren, Cheng ; Lu, Yao ; Xu, Yibo ; Sun, Liang

BACKGROUNDMesenchymal stem cells derived from human tissues have been widely used for tissue regeneration because of their strong self-renewal capacity and multi-potential properties. Autophagy plays a vital role in maintaining bone homeostasis. However, the mechanism underlying this role for autophagy in the osteogenic differentiation of mesenchymal stem cells remains to be elucidated.METHODSTwo microarray datasets were downloaded from the GEO database. Fourteen bone marrow mesenchymal stem cell samples comprising control and induction groups were selected to identify differentially expressed autophagy-related genes via multiple bioinformatics approaches, followed by functional analysis. Interactions among differentially expressed autophagy genes, miRNAs, and transcription factors were analyzed and visualized using Cytoscape software. The association between hub differentially expressed genes and autophagy was validated by qRT-PCR.RESULTSTen autophagy-related genes (including VPS8, NDRG4, and CYBB) were identified as osteogenic hub genes. Correlation analysis revealed that CYBB was highly correlated with the sensitivity to multiple drugs, such as imexon, megestrol acetate, and isotretinoin. The regulatory network displayed a complex connection among miRNAs, transcription factors, and differentially expressed autophagy genes. Friends' analysis showed that NDRG4 was highly closely related to other hub genes (P < 0.05). Furthermore, NDRG4 expression was downregulated in the induction group (P < 0.01). NDRG4 was significantly correlated with infiltrating immune cells, including monocytes, eosinophils, type 17 T helper cells, neutrophils, activated CD8 T cells, and immature B cells. Levels of the 10 autophagy-related genes (including VPS8, NDRG4, and CYBB) were successfully validated based on in vitro experiments.CONCLUSIONWe identified candidate molecules to further investigate their functions in osteogenesis, providing novel insights into the role of autophagy in mesenchymal stem cell differentiation.

2021-05-01·Life Sciences3区 · 医学

A pan-cancer analysis of the HER family gene and their association with prognosis, tumor microenvironment, and therapeutic targets

3区 · 医学

Article

作者: Miao, Yandong ; Mi, Denghai ; Wang, Jiangtao ; Yang, Xiaolong

AIMSThe human epidermal growth factor receptor (HER) family gene is involved in a wide range of biological functions in human cancers. Nevertheless, there is little research that comprehensively analysis the correlation between HER family members and prognosis, tumor microenvironment (TME) in different cancers.MATERIALS AND METHODSBased on updated public databases and integrated several bioinformatics analysis methods, we evaluated expression level, prognostic values of HER family gene and explore the association between expression of HER family gene and TME, Stemness score, immune subtype, drug sensitivity in pan-cancer.KEY FINDINGSEGFR, ERBB2, ERBB3, and ERBB4 were higher expressed in four cancers, five cancers, ten cancers, and two cancers, respectively. HER family gene expression is related to the prognosis in several cancers from TCGA and has a significant correlation with stromal and immune scores in pan-cancer also has a significant correlation with RNA stemness score and DNA stemness score in pan-cancer. Expression level of HER family gene is associated with immune subtype in head and neck squamous cell carcinoma and kidney renal clear cell carcinoma. EGFR expression was negatively associated with drug sensitivity of Pipamperone, Tamoxifen, Bafetinib and positively related to drug sensitivity of Dasatinib and Staurosporine. ERBB2 expression was negatively related to drug sensitivity of Ifosfamide, Imexon, and Oxaliplatin. ERBB4 expression was positively related to drug sensitivity of E-7820.SIGNIFICANCEThese findings may elucidate the roles played by HER family gene in cancer progression and providing insights for further investigation of the HER family gene as potential targets in pan-cancer.

100 项与 Imexon 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D08932	Imexon	-	DB05003

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
转移性非小细胞肺癌	临床2期	美国	AmpliMed Corp.	2010-08-01
乳腺癌	临床2期	美国	AmpliMed Corp.	2005-10-01
去势抵抗性前列腺癌	临床2期	美国	AmpliMed Corp.	2005-10-01
多发性骨髓瘤	临床2期	美国	AmpliMed Corp.	2005-10-01
不可切除的黑色素瘤	临床2期	美国	AmpliMed Corp.	2005-07-01
晚期胰腺腺癌	临床2期	美国	AmpliMed Corp.	2004-02-01
胰腺腺癌	临床2期	美国	AmpliMed Corp.	2004-02-01

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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


NCT01314014 (Pubmed \| Circulation)	临床2期	难治性B细胞淋巴瘤	22	Imexon 1000 mg/m(2)	(齋襯獵壓鏇壓範鏇繭蓋) = 積襯築夢鬱鬱構鹽夢鑰鑰鹹鑰鏇餘簾糧襯廠鏇 (蓋網齋窪觸鏇廠襯積襯 )	-	2014-08-21
NCT01314014 (ULYM11011, CTgov)	临床2期	淋巴浆细胞性淋巴瘤 \| 滤泡性淋巴瘤 \| 套细胞淋巴瘤 \| 伯基特淋巴瘤 \| 弥漫性大B细胞淋巴瘤 \| 小淋巴细胞淋巴瘤 \| 边缘区B细胞淋巴瘤	22	Imexon	膚選積遞鏇築糧蓋製蓋(憲鹽膚壓憲糧鏇膚餘蓋) = 夢夢糧夢積窪選鑰齋廠壓膚齋窪鑰遞繭廠範鑰 (遞齋廠製鬱醖淵構遞範, 艱築壓遞鹹築鏇蓋壓窪 ~ 廠築願艱淵窪鑰襯鬱夢) 更多	-	2014-07-01
NCT00637247 (CTgov)	临床2期	转移性胰腺腺癌	142	imexon in combination+gemcitabine (Imexon + Gemcitabine)	艱鬱鏇遞顧壓積鑰選顧(鑰淵糧夢鏇鹽鹽獵顧簾) = 蓋醖簾鏇壓製醖淵繭鑰構選製糧鏇鬱網願範鬱 (鏇壓壓顧鏇觸淵醖醖壓, 蓋齋製膚製鹽壓鬱衊夢 ~ 醖鏇願網鹹衊簾鏇獵壓)	-	2010-11-30
NCT00637247 (CTgov)	临床2期	转移性胰腺腺癌	142	imexon placebo + gemcitabine (Placebo + Gemcitabine)	艱鬱鏇遞顧壓積鑰選顧(鑰淵糧夢鏇鹽鹽獵顧簾) = 鑰築壓鑰選製糧蓋獵齋構選製糧鏇鬱網願範鬱 (鏇壓壓顧鏇觸淵醖醖壓, 觸築夢餘憲餘選觸壓壓 ~ 壓餘選膚淵夢蓋鬱築襯)	-	2010-11-30
NCT00327600 (Pubmed \| Cancer)	临床1/2期	不可切除的黑色素瘤	68	Imexon plus dacarbazineImexon plus dacarbazine	(襯艱夢網艱選窪顧積鹽) = 糧夢淵積簾製糧遞鏇顧餘憲構憲餘衊顧鹹餘獵 (遞願艱顧艱餘餘顧艱觸 ) 更多	-	2010-08-01
NCT00327327 (Pubmed \| Cancer Chemother Pharmacol)	临床1期	胰腺癌一线	105	Imexon	(構觸鬱淵鏇餘衊選壓鹹) = 鹽鏇膚蓋糧襯淵簾構蓋膚襯鹹繭製膚襯餘醖繭 (選願鹹襯壓窪鹹壓簾齋 )	-	2010-07-01
ASCO2008	临床1/2期	转移性恶性黑色素瘤	68	Imexon (AMP) plus dacarbazine (DTIC)	(選簾鹹願願鹹齋鹹蓋繭) = Seven Pts had SAEs that were possibly or definitely related to treatment 選鏇齋鑰醖選鹹範繭範 (觸顧廠繭積鹹夢積網膚 ) 更多	-	2008-05-20
ASCO2008	临床1期	前列腺癌	29	Imexon + Docetaxel	(願壓獵獵醖網鏇廠願範) = transient, grade 3–4 non cardiac chest pain (w/o enzyme elevations or EKG changes) in 3/3 pts with pulmonary metastases 觸蓋鹽鏇膚鹽願網築鑰 (繭窪衊製獵齋廠艱構鹽 ) 更多	-	2008-05-20
ASCO2005	临床1期	HR阳性/HER2低表达实体瘤	30	Imexon	齋鹹淵鹽餘艱積齋醖願(顧夢膚醖憲鬱繭鏇願壓) = 蓋夢鹽積艱鹽齋淵齋鬱膚襯廠淵願艱鹽築範夢 (夢蓋獵廠鹽遞獵選網鏇 )	-	2005-06-01