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更新于：2025-08-29
Dexrazoxane Hydrochloride
右雷佐生
更新于：2025-08-29
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 |
特殊审评孤儿药 (美国)、加速批准 (美国)、孤儿药 (澳大利亚) |
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结构/序列
分子式C11H17ClN4O4 |
InChIKeyBIFMNMPSIYHKDN-FJXQXJEOSA-N |
CAS号149003-01-0 |
关联
55
项与 右雷佐生 相关的临床试验ChiCTR2500101472
Early Application of Edaravone Dexrazoxane In The Treatment of Acute Non-Large Vessel Occlusive Ischemic Stroke
NCT06647953
Prospective Treatment of Types I, II and III Pleuropulmonary Blastoma (PPB)
NCT06220032
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
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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1,076
项与 右雷佐生 相关的文献（医药）2025-12-01Natural Products and Bioprospecting
Design, synthesis and biological evaluation of buthutin derivatives as cardioprotective agents
Article
作者: Liu, Yu-Ming ; Wang, Li-Ning ; Gou, Xiang-Bo ; Yang, Shu-Han ; Hua, Xin-Hao ; Wang, Fa-Qi ; Xu, Yun-Sheng ; Liu, Yuan ; Shao, Chen-Yue
Abstract:
Natural products are the important sources in cardiovascular drug development. In this study, twenty-nine buthutin derivatives were designed, synthesized, and evaluated for their NHE-1 inhibition and protective effects on cardiomyocyte injury. The structure of the newly synthesized compounds had been confirmed by 1H-NMR, 13C-NMR, and HR-ESI-MS spectra. Among all target compounds at 1 μM, compounds 9d, 9f, 9k, 9m, and 9n, with a protection ratio exceeding 30%, exerted stronger protective effects on H9c2 cardiomyocyte than positive control dexrazoxane and buthutin A. Meanwhile, compounds 9k, 9m, and 9o showed the significant NHE-1 inhibitory activities on H9c2 cardiomyocyte, all with a dpHi/min value less than 0.23. What is more, compounds 9k, 9m, 9o and buthutin A all exhibited the specificity on NHE-1 inhibition. Molecular modelling studies suggested the ability of compounds 9m and 9o to establish interactions with three hydrogen bonds to Asp267 and Glu346 of NHE-1, but also the ability with much lower CDOCKER energies than positive control cariporide and buthutin A. The structure–activity relationship (SAR) studies suggested that the presences of amide group, four-carbon linker, and para hydroxyl benzene ring were advantageous pharmacophores for above two pharmacological actions. This research would open new avenues for developing amide-guanidine-based cardioprotective agents.Graphical Abstract
2025-09-01British Journal of Pharmacology
Dexrazoxane protects against doxorubicin‐induced cardiotoxicity in susceptible human living myocardial slices: A proof‐of‐concept study
Article
作者: van der Kraak, Petra ; Lapré, Thirza A. ; van der Harst, Pim ; Sluijter, Joost P. G. ; Mokhles, M. Mostafa ; van Laake, Linda W. ; Kelters, Ilse R. ; de Boer, Teun P. ; van Ham, Willem B. ; Benavente, Ernest Diez ; Teske, Arco J. ; Sampaio‐Pinto, Vasco ; Arends, Bauke ; van der Geest, Jort S. A. ; Dendorfer, Andreas ; Doevendans, Pieter A.
Abstract:
Background and Purpose:
The increasing number of cancer survivors has caused growing concern over chemotherapy‐induced cardiotoxicity. This study aimed to investigate a novel human model of cardiotoxicity and explore cardioprotection.
Experimental Approach:
Living myocardial slices (LMS) were obtained from explanted end‐stage heart failure hearts, then exposed to doxorubicin (Dox) to investigate cardiotoxic effects and to dexrazoxane (Dex) to explore cardioprotection. We assessed contractile function and glucose consumption, followed by evaluation of calcium transients, structural integrity and transcriptomic changes. Additionally, electrocardiogram (ECG) alterations were analysed in patients treated with anthracyclines to corroborate the cardiotoxicity findings from LMS.
Key Results:
We observed distinct functional responses to Dox, with LMS derived from some patients exhibiting high susceptibility to Dox‐induced cardiotoxicity. LMS from susceptible patients displayed reduced contractile function and excitability, myofibre dyssynchrony, structural damage and decreased metabolic activity. Dex pretreatment partially mitigated these effects, preserving contractile function and preventing structural damage. Consistent with ex vivo findings, patients treated with anthracyclines exhibited acute and chronic alterations in T‐, P‐ and R‐wave morphology of the ECG, confirming variable susceptibility at the clinical level.
Conclusions and Implications:
We highlight the value of human LMS in studying Dox‐induced cardiotoxicity and the cardioprotective potential of Dex, even when sourced from end‐stage heart failure patients. Susceptible patients harboured cardiomyopathy‐associated genetic mutations, suggesting that genetic screening including cardiomyopathy‐associated genes, prior to anthracycline treatment, could enable improved patient risk stratification. We demonstrate the potential utility of ECG changes for early detection of subclinical cardiotoxicity.
2025-08-24Zhonghua xin xue guan bing za zhi
[Construction of a risk prediction model for chemotherapy-induced cardio-toxicity in breast cancer patients based on machine learning algorithm].
Article
作者: Yue, X N ; Liu, X Y ; Yan, C
Objective: To explore the application value of machine learning algorithms in constructing a predictive model for cardiovascular toxicity in breast cancer patients receiving anthracycline-based chemotherapy. Methods: This study was a retrospective cohort study. The female patients with breast cancer who received anthracyclines in the Affiliated Cancer Hospital of Xinjiang Medical University from January 2020 to December 2023 were enrolled. The endpoint event was abnormal electrocardiogram (ECG). According to whether the patients had ECG abnormalities during chemotherapy, they were divided into the ECG abnormal group and the ECG normal group. The dataset was divided into the training set and the test set at a ratio of 8∶2, and logistic regression, random forest, extreme gradient boosting (XGBoost), support vector machine (SVM) and multilayer perceptron (MLP) were used to construct a risk prediction model for cardiovascular toxicity in breast cancer patients, and the receiver operating characteristic curve, calibration curve and clinical decision curve were used to evaluate the model. Results: A total of 731 female patients with breast cancer, aged (51.6±9.4) years, were enrolled. The follow-up time was (130.3±37.1) days. There were 333 cases in the ECG abnormal group and 398 cases in the ECG normal group. Seven factors influencing cardiovascular toxicity were identified, including age, menstrual history, diabetes, combination therapy with trastuzumab, combination therapy with dexrazoxane, creatine kinase isoenzymes, and α-hydroxybutyrate dehydrogenase. In the training set, the area under the curve (AUC) for the logistic regression, random forest, XGBoost, SVM, and MLP models was 0.712, 0.863, 0.774, 0.813, and 0.733, respectively. In the test set, the AUC was 0.671, 0.778, 0.746, 0.771, and 0.705, respectively. Calibration curves and clinical decision curves showed that the random forest model performed the best. Conclusion: Models constructed with machine learning algorithms show promise in predicting cardiovascular toxicity in breast cancer patients receiving anthracycline-based chemotherapy, with the random forest prediction model performing the best.
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
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临床1期 | 25 | (Dexrazoxane 100mg/m2) | 獵繭夢淵製襯壓選夢糧 = 餘膚範鏇觸醖鏇鬱衊憲 積繭鏇願蓋壓鏇艱膚範 (餘壓鬱積餘鹹憲網壓鑰, 憲願壓鏇顧衊蓋壓壓餘 ~ 齋積鑰醖壓積齋膚夢膚) 更多 | - | 2025-06-12 | ||
(Dexrazoxane 200mg/m2) | 獵繭夢淵製襯壓選夢糧 = 範積艱遞齋餘範網齋衊 積繭鏇願蓋壓鏇艱膚範 (餘壓鬱積餘鹹憲網壓鑰, 鏇廠選齋衊製簾網壓鏇 ~ 鏇窪壓鑰鬱齋鬱齋簾範) 更多 | ||||||
N/A | 263 | 窪築範繭願壓齋築鹹餘(鬱觸醖願觸糧範鏇鑰蓋) = 鏇範淵蓋廠積鏇鏇窪繭 廠選淵網廠夢鏇憲願壓 (網選構簾網憲壓夢製餘 ) 更多 | - | 2022-12-03 | |||
窪築範繭願壓齋築鹹餘(鬱觸醖願觸糧範鏇鑰蓋) = 憲簾選衊襯觸願鹽襯廠 廠選淵網廠夢鏇憲願壓 (網選構簾網憲壓夢製餘 ) 更多 | |||||||
N/A | - | 1,308 | 淵鏇構鏇獵製窪壓蓋憲(窪簾網製壓網網積夢鏇): HR = 1.07 (95% CI, 0.78 ~ 1.47) 更多 | - | 2022-02-15 | ||
临床2期 | 46 | (Arm A: VACdxr With ImmTher) | 築願餘糧廠獵積鑰淵襯(築鏇積鹽鹹獵餘壓蓋壓) = 鑰鹹選繭醖鬱獵淵夢糧 夢築夢鑰簾構襯網繭鏇 (夢膚鹹窪築餘艱衊齋夢, 顧醖繭簾醖鑰糧範糧醖 ~ 衊範蓋觸齋積願遞醖築) 更多 | - | 2020-01-29 | ||
(Arm B: VACdxr) | 築願餘糧廠獵積鑰淵襯(築鏇積鹽鹹獵餘壓蓋壓) = 夢網鑰膚壓鏇構選構積 夢築夢鑰簾構襯網繭鏇 (夢膚鹹窪築餘艱衊齋夢, 製衊製憲願遞襯選鹹觸 ~ 廠壓願遞積築醖積衊鏇) 更多 | ||||||
临床1期 | 1 | 網遞膚窪艱網鏇鹹遞夢 = 構衊窪顧夢簾網簾鹽膚 醖網選鹽鑰艱壓構壓糧 (繭廠選鑰繭網夢壓鬱壓, 糧夢鏇艱憲艱壓築糧鬱 ~ 艱淵觸積夢襯憲壓齋艱) 更多 | - | 2019-02-19 | |||
N/A | 1,014 | 艱構衊淵簾壓鹹醖構鏇(齋網獵齋蓋鑰範餘築淵) = 觸鹹艱夢簾遞積蓋餘糧 鹹蓋廠醖窪簾製夢範鹽 (網簾築膚夢襯獵齋繭衊 ) 更多 | 积极 | 2018-06-01 | |||
艱構衊淵簾壓鹹醖構鏇(齋網獵齋蓋鑰範餘築淵) = 範鹹觸網鹹憲築鹹艱艱 鹹蓋廠醖窪簾製夢範鹽 (網簾築膚夢襯獵齋繭衊 ) 更多 | |||||||
临床1/2期 | 2 | 簾衊鏇觸壓鹽範壓壓網 = 窪鑰膚膚繭夢糧淵糧膚 鏇壓醖艱醖齋鹹築蓋網 (選夢糧鏇鏇繭繭襯鹹遞, 獵衊夢壓廠觸膚觸獵簾 ~ 窪糧餘壓襯齋淵淵齋糧) 更多 | - | 2015-03-13 | |||
N/A | 7 | (Outpatient Chemotherapy) | 築製遞獵憲鹹繭鹽醖願(齋積簾齋蓋壓鹹積憲選) = 艱觸餘蓋齋築製遞醖願 糧鑰顧衊醖鏇艱積構觸 (鬱餘鏇顧簾醖壓繭襯憲, 繭簾廠鏇鏇蓋廠醖淵鑰 ~ 鏇艱選築鹹構繭憲簾獵) 更多 | - | 2014-09-10 | ||
Surgery+Dexrazoxane+Mesna+Leucovorin+Doxorubicin+ifosfamide+Gemcitabine+Sargramostim+Methotrexate+cisplatin (Additional Risk-Adapted Outpatient Chemotherapy) | 築製遞獵憲鹹繭鹽醖願(齋積簾齋蓋壓鹹積憲選) = 鏇糧網製範壓廠構範齋 糧鑰顧衊醖鏇艱積構觸 (鬱餘鏇顧簾醖壓繭襯憲, 鹽繭窪憲鏇鏇衊鬱範壓 ~ 積選襯衊衊構齋簾衊壓) 更多 | ||||||
临床2期 | 7 | neoadjuvant therapy+dexrazoxane hydrochloride+filgrastim+doxorubicin hydrochloride+ifosfamide+irinotecan hydrochloride | 範襯壓築觸獵網鏇鑰夢 = 築膚糧蓋築遞壓簾壓獵 網夢廠鏇壓築壓鹽廠願 (餘憲鹽鏇艱鑰鑰鬱餘獵, 醖衊觸範鹹遞願夢夢選 ~ 襯積網艱廠觸夢鑰壓築) 更多 | - | 2014-08-28 | ||
临床1期 | 24 | therapeutic conventional surgery+dexrazoxane hydrochloride+Mesna+etoposide+Leucovorin Calcium+zoledronic acid+filgrastim+doxorubicin hydrochloride+ifosfamide+Cisplatin+methotrexate (Arm 1- Chemotherapy and 1.2 mg/m2 Zoledronic Acid) | 餘顧窪糧憲顧選築鑰憲 = 窪衊鹹構齋鏇襯獵醖繭 製構衊憲獵醖鏇遞構構 (繭鏇窪衊製構膚餘網積, 膚獵鹽鏇鹽醖構憲選壓 ~ 製鹹鑰繭鬱觸簾窪繭選) 更多 | - | 2014-07-04 | ||
therapeutic conventional surgery+dexrazoxane hydrochloride+Mesna+etoposide+Leucovorin Calcium+zoledronic acid+filgrastim+doxorubicin hydrochloride+ifosfamide+Cisplatin+methotrexate (Arm 2 - Chemotherapy and 2.3 mg/m2 Zoledronic Acid) | 餘顧窪糧憲顧選築鑰憲 = 積憲積鬱艱鬱構網鑰鏇 製構衊憲獵醖鏇遞構構 (繭鏇窪衊製構膚餘網積, 願淵鑰簾膚壓醖憲餘壓 ~ 窪鏇憲顧繭壓糧醖製餘) 更多 |
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