二溴卫矛醇(Mitolactol) - 药物靶点：DNA_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Bromoalcohol、DBD、Dibromdicil

+ [8]

靶点

DNA

作用机制

DNA抑制剂(DNA抑制剂)、DNA烷化剂

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症

脑癌宫颈癌

原研机构-

在研机构-

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

登录后查看时间轴

结构

分子式C6H12Br2O4

InChIKeyVFKZTMPDYBFSTM-GUCUJZIJSA-N

CAS号10318-26-0

关联

2

项与二溴卫矛醇相关的临床试验

NCT02005783 / Completed临床2期IIT

Adjuvant Treatment of EC/TC Versus EC/TC Plus Danggui Buxue Decoction in Breast Cancer：A Prospective, Randomized Trial

To evaluate EC/TC (epirubicin and cyclophosphomide or docetaxel and cyclophosphomide) with EC/TC plus DBD (Danggui Buxue Decoction) in adjuvant treatment of breast cancer patients. The aim is to evaluate whether DBD can decrease the incidence of grade 3/4 neutropenia induced by EC/TC regimen during chemotherapy.

开始日期2013-10-01

申办/合作机构

上海交通大学

NCT00002620 / Completed临床3期IIT

EFFECT OF DIBROMODULCITOL PLUS BCNU ON FREE INTERVAL AND SURVIVAL OF PATIENTS WITH SUPRATENTORIAL MALIGNANT BRAIN GLIOMAS, A PHASE III TYPE STUDY

RATIONALE: Radiation therapy uses high-energy x-rays to damage tumor cells and may be an effective treatment for patients with anaplastic astrocytomas.
PURPOSE: Randomized phase III trial to study the effectiveness of radiation therapy in treating patients with anaplastic astrocytomas.

开始日期1994-11-01

申办/合作机构

Eortc

100 项与二溴卫矛醇相关的临床结果

登录后查看更多信息

100 项与二溴卫矛醇相关的转化医学

登录后查看更多信息

100 项与二溴卫矛醇相关的专利（医药）

登录后查看更多信息

266

项与二溴卫矛醇相关的文献（医药）

2025-02-01·Journal of Ethnopharmacology

Danggui Buxue Decoction and its components dilate coronary artery through activating the inward rectification K+ channels pathway

Article

作者: Guo, Pengmei ; Yang, Peng ; Chen, Mingzhu ; Zhang, Ting ; An, Wenqiao ; Zhang, Sanyin ; Tian, Qianqian

ETHNOPHARMACOLOGICAL RELEVANCEDanggui Buxue Decoction (DBD), a classic representative prescription of invigorating Qi and producing blood, is used to treat coronary heart disease angina pectoris and vascular injury diseases. Abnormal coronary artery is an important cause of cardiovascular disease. However, the mechanism of DBD dilates coronary arteries is still unclear.AIM OF THE STUDYThis study aimed to elucidate the impacts and distinctions among DBD, Astragalus, Angelica sinensis, and identified active components on pre-constricted coronary arteries, as well as to delve deeper into their respective mechanisms.MATERIALS AND METHODSAfter the preconstriction of a rat isolated coronary artery ring with either 30 mM KCl or 200 nM U46619, the vascular tension was observed following the addition of DBD, and other components. Subsequently, the impact of these active components on coronary blood flow (CBF) was confirmed through in vivo testing. Further investigation into the underlying mechanism was carried out using a combination of blockers, molecular docking, surface plasmon resonance (SPR), cell heat transfer analysis (CETSA), and patch-clamp techniques.RESULTSIn vitro experiments showed that DBD and its components butylidenephthalide, ligustilide, calycosin, and quercetin could dilate coronary artery preconstricted with either 30 mM KCl or 200 nM U46619. In addition, the active ingredient was found to significantly increase CBF. Mechanistically, BaCl₂ was found to reduce the relaxation effect of the drug by adding a blocker. Molecular docking, SPR and CETSA results showed that the active ingredients had a strong binding potential with inward rectification K⁺ channels (K_IR) channel protein. Patch clamp studies demonstrate that quercetin can increase K_IR current, and BaCl₂ can significantly reduce its current.CONCLUSIONSThe active components of DBD, butylidenephthalide, ligustilide, calycosin, and quercetin, activate K_IR channels to relax coronary artery and increase CBF.

2024-12-01·Phytomedicine

Dang-Gui-Bu-Xue decoction against diabetic nephropathy via modulating the carbonyl compounds metabolic profile and AGEs/RAGE pathway

Article

作者: Zhang, Zhi-Tong ; Liu, Jie ; Chen, Pan ; Fan, Zhiliang ; Jiang, Yue ; Chen, Li ; Zhao, Di ; Yan, Guojun ; Qi, Yali ; Bai, Lei ; Guan, Huanhuan

BACKGROUNDDang-Gui-Bu-Xue decoction (DBD) is a traditional Chinese medicine prescription clinically employed for diabetic nephropathy (DN). However, the components and pharmacological mechanisms of DBD against DN remain incompletely understood.PURPOSETo clarify the beneficial effect of DBD on DN and to explore its nephroprotective effect's probable mechanism and the main components.METHODSA diabetic mice model was established by feeding a high-fat diet (HFD) and intraperitoneal injections of streptozotocin (STZ, 40 mg‧kg^-1). Subsequently, the mice were maintained on a HFD and administered with DBD. The benefits of DBD against DN were comprehensively assessed by monitoring energy and water intake, blood glucose and lipids, renal functions and pathological status. The UPLC-MS/MS was measured to detect chemical constituents in DBD and absorbed components in DBD-treated plasma under physiological and pathological states. Network pharmacology was employed to forecast the probable pathways of DBD intervention in DN, with subsequent validation of these predictions through testing biochemical parameters, anti-glycation and ELISA assays, immunofluorescence, immunohistochemistry, and western blotting. Then, a chemical derivatization method paired with UPLC-MS/MS analysis was performed to detect the carbonyl compounds in renal tissue. Finally, the main components of DBD against DN were screened by anti-glycation and MTT assays.RESULTSDBD regulated energy and water intakes, glucose and lipid metabolism disorders, renal dysfunction, glomerular filtration rate, renal interstitial glycogen accumulation and fibrosis in HFD/STZ-induced DN mice. A total of 129 distinct chemical constituents in DBD were characterized, of which 28 were detected in the DBD-treated plasma under a pathological state. The network pharmacological results suggested AGEs/RAGE and its downstream pathway may be a potential pathway for DBD intervention in DN. Further experiments confirmed that DBD reduced renal oxidative stress by modulating the AGEs/RAGE pathway. Moreover, 21 differential carbonyl compounds were detected between normal and DN mice, and DBD significantly modulated 16. Ultimately, seven components were screened out in DBD, which may be the main components of DBD regulating carbonyl compounds metabolic profile and AGEs/RAGE pathway.CONCLUSIONOur findings suggested for the first time that DBD could regulate the carbonyl compounds metabolic profile and AGEs/RAGE signaling pathway to ameliorate DN.

2024-10-01·American Journal of Transplantation

Association of procurement technique with organ yield and cost following donation after circulatory death

Article

作者: Cain, Michael T ; Nydam, Trevor L ; Bakhtiyar, Syed Shahyan ; Rove, Jessica Y ; Gutowski, John ; Reece, T Brett ; Bababekov, Yanik J ; Schold, Jesse D ; Cleveland, Joseph C ; Hoffman, Jordan R H ; Park, Sarah Y ; Maksimuk, Tiffany E ; Pomposelli, James J ; Pomfret, Elizabeth A

Donation after circulatory death (DCD) could account for the largest expansion of the donor allograft pool in the contemporary era. However, the organ yield and associated costs of normothermic regional perfusion (NRP) compared to super-rapid recovery (SRR) with ex-situ normothermic machine perfusion, remain unreported. The Organ Procurement and Transplantation Network (December 2019 to June 2023) was analyzed to determine the number of organs recovered per donor. A cost analysis was performed based on our institution's experience since 2022. Of 43 502 donors, 30 646 (70%) were donors after brain death (DBD), 12 536 (29%) DCD-SRR and 320 (0.7%) DCD-NRP. The mean number of organs recovered was 3.70 for DBD, 3.71 for DCD-NRP (P < .001), and 2.45 for DCD-SRR (P < .001). Following risk adjustment, DCD-NRP (adjusted odds ratio 1.34, confidence interval 1.04-1.75) and DCD-SRR (adjusted odds ratio 2.11, confidence interval 2.01-2.21; reference: DBD) remained associated with greater odds of allograft nonuse. Including incomplete and completed procurement runs, the total average cost of DCD-NRP was $9463.22 per donor. By conservative estimates, we found that approximately 31 donor allografts could be procured using DCD-NRP for the cost equivalent of 1 allograft procured via DCD-SRR with ex-situ normothermic machine perfusion. In conclusion, DCD-SRR procurements were associated with the lowest organ yield compared to other procurement methods. To facilitate broader adoption of DCD procurement, a comprehensive understanding of the trade-offs inherent in each technique is imperative.

100 项与二溴卫矛醇相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	-	L01XX	DB12916

研发状态

批准上市

10 条最早获批的记录,

登录

后查看更多信息

适应症	国家/地区	公司	日期
肿瘤	-	-	-

未上市

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
脑癌	临床3期	美国	-	-
肿瘤	临床3期	英国	-	-
肿瘤	临床3期	爱尔兰	-	-
宫颈癌	临床3期	美国	-	-

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00002620 (Pubmed \| Ann Neurol)	临床3期	胶质瘤辅助	269	Radiation therapy + DBD + BCNU	(夢蓋範獵齋廠淵糧鑰構) = 蓋顧願鹹鑰鬱繭獵簾窪遞鬱顧願壓齋鹽鏇構簾 (積築製襯遞鬱廠廠顧積 ) 更多	积极	1994-08-01
				Radiation therapy alone	(夢蓋範獵齋廠淵糧鑰構) = 築齋膚選壓選製簾範鑰遞鬱顧願壓齋鹽鏇構簾 (積築製襯遞鬱廠廠顧積 ) 更多