更新于：2024-06-30
Dexrazoxane Hydrochloride
右雷佐生
更新于：2024-06-30
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国)、孤儿药 (美国)、孤儿药 (澳大利亚) |
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结构
分子式C11H17ClN4O4 |
InChIKeyBIFMNMPSIYHKDN-FJXQXJEOSA-N |
CAS号149003-01-0 |
关联
51
项与 右雷佐生 相关的临床试验ANTICIPATE: Prevention of ANThracycline-Induced Cardiac Dysfunction by Dexrazoxane In PATients With diffusE Large B-cell Lymphoma: a Phase III National Multicenter Prospective Randomized Open-label Trial
A Phase II, Single Arm, Open Label, Study on the Safety, Efficacy, Pharmacokinetics & Pharmacodynamics of Quizartinib + Chemotherapy and as Single-agent After High Dose Therapy in Newly Diagnosed Pediatric FLT3-ITD+ and NPM1wt AML Patients
A Phase I Study of Venetoclax in Combination With Cytotoxic Chemotherapy, Including Calaspargase Pegol, for Children, Adolescents and Young Adults With High-Risk Hematologic Malignancies
100 项与 右雷佐生 相关的临床结果
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100 项与 右雷佐生 相关的转化医学
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100 项与 右雷佐生 相关的专利（医药）
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821
项与 右雷佐生 相关的文献（医药）2024-04-01Redox biology
Pharmacological activation of GPX4 ameliorates doxorubicin-induced cardiomyopathy
Article
作者: Guo, Yishan ; Wang, Li ; Xiang, Ying ; Sun, Guogen ; Yang, Jinru ; Jin, Min ; Zhang, Tao ; Han, Bing ; Li, Jiao ; Huang, Chuying ; Wu, Bo ; Li, Tuo ; Zhou, Yong ; Wei, Yumiao ; Mao, Yong ; Hu, Jiaxing ; Qiu, Jiao ; Tan, Yong ; Li, Shuijie ; Wang, Yongsheng ; Wang, Yuqi ; Lei, Lingshan ; Huang, Rui ; Song, Xiusheng
Due to the cardiotoxicity of doxorubicin (DOX), its clinical application is limited. Lipid peroxidation caused by excessive ferrous iron is believed to be a key molecular mechanism of DOX-induced cardiomyopathy (DIC). Dexrazoxane (DXZ), an iron chelator, is the only drug approved by the FDA for reducing DIC, but it has many side effects and cannot be used as a preventive drug in clinical practice. Single-nucleus RNA sequencing (snRNA-seq) analysis identified myocardial and epithelial cells that are susceptible to DOX-induced ferroptosis. The glutathione peroxidase 4 (GPX4) activator selenomethione (SeMet) significantly reduced polyunsaturated fatty acids (PUFAs) and oxidized lipid levels in vitro. Consistently, SeMet significantly decreased DOX-induced lipid peroxidation in H9C2 cells and mortality in C57BL/6 mice compared to DXZ, ferrostatin-1, and normal saline. SeMet can effectively reduce serum markers of cardiac injury in C57BL/6 mice and breast cancer patients. Depletion of the GPX4 gene in C57BL/6 mice resulted in an increase in polyunsaturated fatty acid (PUFA) levels and eliminated the protective effect of SeMet against DIC. Notably, SeMet exerted antitumor effects on breast cancer models with DOX while providing cardiac protection for the same animal without detectable toxicities. These findings suggest that pharmacological activation of GPX4 is a valuable and promising strategy for preventing the cardiotoxicity of doxorubicin.
2024-01-09Advances in pharmacological and pharmaceutical sciences
Alkaloidal Extracts from Avicennia africana P. Beauv. (Avicenniaceae) Leaf: An Antiplasmodial, Antioxidant, and Erythrocyte Viable
Article
作者: Ahmed, Mustapha A ; Zoiku, Felix K ; Adokoh, Christian K ; Armah, Francis A ; Ghartey-Kwansah, George ; Fynn, Patrick M ; Ameyaw, Elvis O ; Asiamah, Isaac ; Ofori-Attah, Ebenezer
Background. The emergence of drug-resistant parasites impedes disease management and eradication efforts. Hence, a reinvigorated attempt to search for potent lead compounds in the mangroves is imperative. Aim. This study evaluates in vitro antiplasmodial activity, antioxidant properties, and cytotoxicity of A. africana leaf alkaloidal extracts. Methods. The A. africana leaves were macerated with 70% ethanol to obtain a total crude extract. Dichloromethane and chloroform-isopropanol (3 : 1, v/v) were used to extract the crude alkaloids and quaternary alkaloids from the total crude. The antiplasmodial activities of the alkaloidal extracts were performed against 3D7 P. falciparum chloroquine-sensitive clone via the SYBR Green I fluorescence assay with artesunate serving as the reference drug. The alkaloidal extracts were further evaluated for antioxidant properties via the total antioxidant capacity (TAC), the total glutathione concentration (GSH), the DPPH (2,2-diphenyl-1-picrylhydrazyl) assay, and the ferric-reducing antioxidant power (FRAP) methods. The cytotoxic activity of the alkaloidal extracts was tested on erythrocytes using a 3-(4,5-dimethylthiazol-2-yl)-5-diphenyltetrazolium bromide-MTT assay with little modification. The phytocompounds in the alkaloidal extracts were identified via gas chromatography-mass spectrometry (GC-MS) techniques. Results. The total crude extract showed good antiplasmodial activity (IC50 = 11.890 µg/mL). The crude and quaternary alkaloidal extracts demonstrated promising antiplasmodial effects with IC50 values of 6.217 and 6.285 µg/mL, respectively. The total crude and alkaloidal extracts showed good antioxidant properties with negligible cytotoxicity on erythrocytes with good selectivity indices. The GC-MS spectral analysis of crude alkaloidal extracts gave indole and isoquinoline alkaloids and several other compounds. Dexrazoxane was found to be the main compound predicted, with an 86% peak area in the quaternary alkaloidal extract. Conclusion. The crude and quaternary alkaloidal extracts exhibited antiplasmodial activities and ability to inhibit oxidative stress with negligible toxicity on erythrocytes. This may be good characteristics to avoid oxidative stress related to Plasmodium infection in the treatment of malaria.
2024-01-01British journal of pharmacology
Novel metallo‐β‐lactamases inhibitors restore the susceptibility of carbapenems to New Delhi metallo‐lactamase‐1 (NDM‐1)‐harbouring bacteria
Article
作者: Gao, Yawen ; Yang, Mengge ; Wang, Jianfeng ; Ding, Rui ; Qiu, Jiazhang ; Niu, Xiaodi ; Liu, Hongtao ; Feng, Haihua ; Guo, Yan ; Deng, Xuming
Abstract:
Background and purpose:
The production of metallo‐β‐lactamases is a major mechanisms adopted by bacterial pathogens to resist carbapenems. Repurposing approved drugs to restore the efficacy of carbapenems represents an efficient and cost‐effective approach to fight infections caused by carbapenem resistant pathogens.
Experimental approach:
The nitrocefin hydrolysis assay was employed to screen potential New Delhi metallo‐lactamase‐1 (NDM‐1) inhibitors from a commercially available U.S. Food and Drug Administration (FDA) approved drug library. The mechanism of inhibition was clarified by metal restoration, inductively coupled plasma mass spectrometry (ICP‐MS) and molecular dynamics simulation. The in vitro synergistic antibacterial effect of the identified inhibitors with meropenem was determined by the checkerboard minimum inhibitory concentration (MIC) assay, time‐dependent killing assay and combined disc test. Three mouse infection models were used to further evaluate the in vivo therapeutic efficacy of combined therapy.
Key results:
Twelve FDA‐approved compounds were initially screened to inhibit the ability of NDM‐1 to hydrolyse nitrocefin. Among these compounds, dexrazoxane, embelin, candesartan cilexetil and nordihydroguaiaretic acid were demonstrated to inhibit all tested metallo‐β‐lactamases and showed an in vitro synergistic bactericidal effect with meropenem against metallo‐β‐lactamases‐producing bacteria. Dexrazoxane, embelin and candesartan cilexetil are metal ion chelating agents, while the inhibition of NDM‐1 by nordihydroguaiaretic acid involves its direct binding to the active region of NDM‐1. Furthermore, these four drugs dramatically rescued the treatment efficacy of meropenem in three infection models.
Conclusions and implications:
Our observations indicated that dexrazoxane, embelin, candesartan cilexetil and nordihydroguaiaretic acid are promising carbapenem adjuvants against metallo‐β‐lactamases‐positive carbapenem resistant bacterial pathogens.
100 项与 右雷佐生 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 诊断和治疗物质外渗 | 欧盟 | 2006-07-27 | |
| 诊断和治疗物质外渗 | 冰岛 | 2006-07-27 | |
| 诊断和治疗物质外渗 | 列支敦士登 | 2006-07-27 | |
| 诊断和治疗物质外渗 | 挪威 | 2006-07-27 | |
| 细胞保护佐剂 | 中国 | 2006-05-29 | |
| 心肌疾病 | 美国 | 1995-05-26 | |
| 转移性乳腺癌 | 美国 | 1995-05-26 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 出血 | 临床3期 | 丹麦 | 2002-04-01 | |
| 出血 | 临床3期 | 德国 | 2002-04-01 | |
| 出血 | 临床3期 | 意大利 | 2002-04-01 | |
| 出血 | 临床3期 | 荷兰 | 2002-04-01 | |
| 出血 | 临床3期 | 波兰 | 2002-04-01 | |
| 支气管炎 | 临床3期 | 丹麦 | 2001-06-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 142 | Anthracycline + Dexrazoxane | 願積蓋淵選築選觸範鏇(選觸衊蓋糧壓糧膚構壓) = 獵憲餘壓鹹築鹽築積積 蓋膚選選艱夢構顧蓋齋 (膚壓窪簾選繭構積築鏇 ) | 积极 | 2023-05-31 | ||
Anthracycline only | 願積蓋淵選築選觸範鏇(選觸衊蓋糧壓糧膚構壓) = 齋蓋網遞鑰衊憲遞簾鬱 蓋膚選選艱夢構顧蓋齋 (膚壓窪簾選繭構積築鏇 ) 更多 | ||||||
N/A | - | 195 | 繭選夢蓋顧鹹範醖壓艱(顧簾選艱範鹹淵選衊鏇) = 廠憲築鹹憲餘淵鑰製簾 鏇遞簾夢鏇壓衊鹽製簾 (鑰鏇襯淵鹹膚蓋夢網膚 ) | - | 2023-01-20 | ||
- | |||||||
N/A | 263 | 廠蓋鹽網衊鏇蓋鹽遞壓(鏇蓋網製醖觸鹹顧鹽壓) = 鹹繭繭積鹽構獵窪鹹衊 鏇憲壓遞糧襯鬱繭衊遞 (網繭獵鏇積製齋獵顧蓋 ) 更多 | - | 2022-12-03 | |||
廠蓋鹽網衊鏇蓋鹽遞壓(鏇蓋網製醖觸鹹顧鹽壓) = 繭蓋壓積網積襯蓋顧艱 鏇憲壓遞糧襯鬱繭衊遞 (網繭獵鏇積製齋獵顧蓋 ) 更多 | |||||||
N/A | - | 1,308 | Doxorubicin with dexrazoxane | 艱憲齋遞艱顧構構網願(膚鏇醖範衊淵糧憲鹹夢): HR = 1.07 (95% CI, 0.78 ~ 1.47) 更多 | - | 2022-02-15 | |
Doxorubicin without dexrazoxane | |||||||
临床3期 | 236 | Therapeutic Conventional Surgery (Very Low-risk Group) | 鏇糧窪蓋遞蓋選淵廠製(餘顧餘鹽壓夢蓋淵範遞) = 淵製鬱鏇獵糧襯鬱餘製 顧遞衊鬱廠範膚鏇觸鹹 (繭窪繭製獵廠鹽鬱憲願, 構獵構遞襯鹹網壓糧觸 ~ 齋繭廠觸網網醖鹽鑰艱) 更多 | - | 2021-12-28 | ||
(Low-risk Group (Regimen T)) | 鏇糧窪蓋遞蓋選淵廠製(餘顧餘鹽壓夢蓋淵範遞) = 蓋簾醖觸鑰醖選網廠鹹 顧遞衊鬱廠範膚鏇觸鹹 (繭窪繭製獵廠鹽鬱憲願, 遞繭夢糧範膚繭鹽醖製 ~ 網衊壓願淵窪壓衊糧膚) 更多 | ||||||
N/A | 2,375 | 夢鏇觸餘餘廠鏇衊餘窪(憲願醖糧積窪憲鏇壓膚): OR = 1.15 (95% CI, 0.57 ~ 2.31), P-Value = 0.7 更多 | - | 2021-06-29 | |||
No drug or placebo | |||||||
N/A | 173 | 憲繭醖膚廠餘築選壓窪(簾簾遞繭繭獵餘蓋膚網) = 鏇網簾構廠願壓築遞膚 遞憲淵觸餘鑰衊簾壓齋 (廠蓋鏇壓構築築餘製範, 6.0 ~ 18.0) 更多 | 积极 | 2020-05-25 | |||
憲繭醖膚廠餘築選壓窪(簾簾遞繭繭獵餘蓋膚網) = 鑰餘夢鑰築餘襯糧膚餘 遞憲淵觸餘鑰衊簾壓齋 (廠蓋鏇壓構築築餘製範, 6.0 ~ 28.2) 更多 | |||||||
临床2期 | 46 | (Arm A: VACdxr With ImmTher) | 憲淵網壓夢衊蓋網齋鏇(鹹夢顧糧糧構鬱衊衊築) = 簾鑰鏇壓範鬱衊艱淵廠 淵顧醖襯衊鏇鬱鏇顧製 (廠網壓觸願鏇範選築窪, 淵鬱鏇蓋壓醖壓積餘選 ~ 積鹹壓齋顧餘觸淵獵範) 更多 | - | 2020-01-29 | ||
(Arm B: VACdxr) | 憲淵網壓夢衊蓋網齋鏇(鹹夢顧糧糧構鬱衊衊築) = 淵夢壓鑰遞鹽窪鹹淵願 淵顧醖襯衊鏇鬱鏇顧製 (廠網壓觸願鏇範選築窪, 積構積蓋夢膚壓廠製築 ~ 觸繭壓觸餘構廠願膚簾) 更多 | ||||||
临床1期 | 1 | 鹽鑰餘衊艱構醖衊夢壓(憲窪衊衊齋壓膚鏇壓構) = 製艱遞繭艱膚獵蓋鬱鑰 願餘齋淵網膚鹹選選積 (憲鏇襯選範鹽餘範醖築, 醖鏇製願選簾選繭選憲 ~ 獵蓋蓋糧鹹築廠艱糧鹽) 更多 | - | 2019-02-19 | |||
N/A | 乳腺癌 辅助 | 1,545 | 衊鹹觸鹽鬱壓窪願齋蓋(齋觸淵網鏇廠遞繭艱鑰): RR = 0.262 (95% CI, 0.169 ~ 0.407) 更多 | 积极 | 2018-06-01 | ||
Anthracycline-based chemotherapy |
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