盐酸莎巴比星(Sabarubicin Hydrochloride) - 药物靶点：Top II_在研适应症：难治性小细胞肺癌，复发性小细胞肺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Sabarubicin

+ [1]

靶点

Top II

作用方式

抑制剂

作用机制

Top II抑制剂(拓扑异构酶II抑制剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

非在研机构

权益机构-

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)临床1期

特殊审评特殊审批 (中国)

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结构/序列

分子式C32H37NO13

InChIKeyVQHRZZISQVWPLK-UIRGBLDSSA-N

CAS号211100-13-9

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关联

5

项与盐酸莎巴比星相关的临床试验

CTR20150203

/ Recruiting临床1期

注射用盐酸莎巴比星联合顺铂治疗小细胞肺癌（广泛期）安全性、耐受性及药代动力学Ⅰ期临床研究

主要目的：确定注射用盐酸莎巴比星联合顺铂治疗小细胞肺癌（广泛期）患者的最大耐受剂量及剂量限制性毒性，评价注射用盐酸莎巴比星治疗小细胞肺癌患者体内药代动力学特征。次要目的：初步评价注射用盐酸莎巴比星联合顺铂治疗小细胞肺癌（广泛期）的有效性与安全性，为Ⅱ期临床研究推荐合理给药方法。

开始日期2014-08-28

申办/合作机构

北京新沿线医药科技发展有限公司

[+1]

NCT00027781

/ Completed临床2期IIT

Open Label Phase II Study of MEN-10755 Administered Every 3 Weeks in Patients With Progressive Hormone Refractory Prostate Cancer

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase II trial to study the effectiveness of MEN-10755 in treating patients who have progressive prostate cancer that has not responded to hormone therapy.

开始日期2001-08-01

申办/合作机构

Eortc

NCT00003982

/ Completed临床1期IIT

Phase I Study to Determine the Safety of MEN-10755 (BMS-195615) in Patients With a Solid Tumor on a Short I.V. Infusion Given Once Every Week for 3 Consecutive Weeks, Followed by One Week's Rest

RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die.
PURPOSE: Phase I trial to study the effectiveness of MEN-10755 in treating patients who have solid tumors.

开始日期1997-06-01

申办/合作机构

Eortc

100 项与盐酸莎巴比星相关的临床结果

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100 项与盐酸莎巴比星相关的转化医学

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100 项与盐酸莎巴比星相关的专利（医药）

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60

项与盐酸莎巴比星相关的文献（医药）

2016-07-01·Journal of Chromatography B3区 · 医学

Development and validation of a UHPLC–MS/MS method for simultaneous quantitation the plasma concentration of Sabarubicin and its alcohol metabolite M3 in Chinese small cell lung cancer patients

3区 · 医学

Article

作者: Han, Xiaohong ; Zhang, Yan ; Shi, Yuankai ; Wu, Di ; Song, Yuanyuan ; Li, Ning ; Feng, Yun ; Liu, Peng

To support a novel anthracycline agent - Sabarubicin's pharmacokinetics study in Chinese small cell lung cancer patients, a rapid, sensitive, and high throughput ultra-performance liquid chromatography tandem mass spectrometry method using Doxorubicin hydrochloride as internal standard (IS) was developed and validated for simultaneously quantifying Sabarubicin and its alcohol metabolite M3 in human plasma. Plasma samples were pre-extracted with n-hexane to remove hydrophobic interferences and the target compounds were extracted into a 1ml mixture of chloroform and isopropanol (1:1, v/v) and separated on an ACQUITY UPLC BEH Shield RP18 (100mm×2.1mm, 1.7μm) column with gradient mobile phase composed of acetonitrile and water containing 0.1% formic acid. Detection was performed by electrospray ionization in the positive ionization mode under multiple reaction monitoring of the transitions at m/z 644→130 for Sabarubicin, m/z 646→333.2 for M3, and m/z 544→360 for IS. For Sabarubicin and M3, calibration curves over 2-400ng/ml and 0.5-100ng/ml could achieve excellent linearity respectively(r>0.99). Intra- and inter-day precisions were 1.5%-9.1% and 2.2%-12.8%, and accuracy were -9.6% to 0.7% and -4.8% to 5.9% for Sabarubicin and M3 respectively at four concentration levels. The mean recovery for Sabarubicin was 62.4%, 71.9% for M3, and 58.8% for IS. This method was completely validated and successfully applied in the pharmacokinetics study of Sabarubicin and M3 in Chinese small cell lung cancer patients.

2014-03-01·Medicinal Chemistry Research

Quantitative structure–property relationship study on the intercalation of anticancer drugs with ct-DNA

作者: Shahin Ahmadi ; Azize Abdolmaleki ; Mohammad Reza Khazaei

Studies on the intercalation of anticancer compounds with DNA can provide useful suggestions and guidance for the design of new and more efficient anticancer drugs.A quant. structure-property relationship (QSPR) study of a series of anticancer and candidate anticancer drugs with calf thymus DNA (ct-DNA) was performed.Constitutional, Topol., and WHIM descriptors, as well as GETAWAY, 3D-MoRSE, and Aromaticity Indexes descriptors generated from Dragon, were selected to describe the mols.The resampling by half-means method was used to detect the outlier mols.Self-organizing map was used to split the original dataset into training and test set.Genetic algorithm-multiple linear regression technique was used to establish QSPR model for training set.Finally, the best four-mol. descriptor model was developed on a training set of mols. and the external validation was performed on test set of mols.The stability and predictability of QSPR model were determined with the leave-one-out cross-validated variance and the external-validated variance.This QSPR approach can contribute to a better understanding of structural factors of the compounds responsible for drug-DNA intercalations, and be useful in predicting the binding affinity of other compounds with DNA.

2011-08-01·Photochemical & Photobiological Sciences3区 · 化学

Complexes of the antitumoral drugs Doxorubicin and Sabarubicin with telomeric G-quadruplex in basket conformation: ground and excited state properties

3区 · 化学

Article

作者: Stefano Ottani ; Ilse Manet ; Barbara Zambelli ; Giuseppina Andreano ; Luciano Cellai ; Giancarlo Marconi ; Sandra Monti ; Annalisa Masi ; Francesco Manoli

We studied the binding of two anthracycline drugs, Doxorubicin and Sabarubicin, to a model telomeric sequence 5'-d[GGG(TTAGGG)(3)]-3' (21-mer), assuming the basket G-quadruplex (G4) conformation in Na(+)-rich aqueous solution. We used an approach that combines spectroscopic and microcalorimetric techniques to obtain information about ground and excited state properties of the most stable complexes. Both drugs bind to the 21-mer in basket conformation and complexes of 1:1 and 2:1 drug : 21-mer stoichiometry coexist in solution. Binding constants were determined from fluorescence and isothermal titration calorimetry experiments. For both drugs association is driven by enthalpy and disfavoured by entropy in the case of two sequential binding events to different sites. The drug fluorescence is completely quenched in the 1:1 complex, most likely by electron transfer from the guanine system to the anthraquinone moiety, while part of the emission survives in the 2:1 complex. Circular dichroism (CD) of the individual complexes is dominated by the G-quadruplex signal in the UV and by the anthracycline signal in the near-UV and Vis region. The experimental CD spectra combined with conformational calculations at MM level and quantum mechanical calculation of the rotational strength of the electronic transitions afforded information on the binding geometries.

100 项与盐酸莎巴比星相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	盐酸莎巴比星	-	DB12410

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
去势抵抗性前列腺癌	临床前	比利时	Eortc	2001-08-01
去势抵抗性前列腺癌	临床前	以色列	Eortc	2001-08-01
去势抵抗性前列腺癌	临床前	西班牙	Eortc	2001-08-01
去势抵抗性前列腺癌	临床前	瑞士	Eortc	2001-08-01
去势抵抗性前列腺癌	临床前	德国	Eortc	2001-08-01
去势抵抗性前列腺癌	临床前	法国	Eortc	2001-08-01
睾丸生殖细胞肿瘤	临床前	挪威	Eortc	1997-06-01
实体瘤	临床前	葡萄牙	Eortc	1997-04-01
实体瘤	临床前	意大利	Eortc	1997-04-01
实体瘤	临床前	希腊	Eortc	1997-04-01

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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


ASCO2010	临床1/2期	广泛期小细胞肺癌一线	-	Sabarubicin (SABA) + cisplatin (DDP)	齋選製獵簾顧築鹽遞繭(鑰齋蓋齋鏇鏇糧顧蓋齋) = 淵醖憲齋鑰構遞積夢鏇鹽鹹鏇遞醖淵觸鬱範襯 (齋憲鬱憲蓋簾糧醖遞憲 ) 更多	-	2010-05-20
ASCO2008	临床2期	广泛期小细胞肺癌	26	Sabarubicin	(範獵憲襯艱範壓鹽構繭) = 憲襯鹽顧製餘鹽鹽繭繭構淵憲鏇艱糧鹹衊觸願 (醖襯艱願醖範製鬱糧繭, 22.43 ~ 57.46) 更多	-	2008-05-20