S-乙基异硫脲二乙基磷酸盐(S-ethylisothiouronium diethylphosphate) - 药物靶点：NOS_在研适应症：丛集性头痛，低血压，偏头痛_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [6]

靶点

NOS

作用机制

NOS抑制剂(一氧化氮合酶抑制剂)

治疗领域

神经系统疾病心血管疾病其他疾病

在研适应症

丛集性头痛低血压偏头痛

非在研适应症

透析性低血压终末期肾脏病

原研机构

Meditor Pharmaceuticals Ltd.

在研机构-

非在研机构

Meditor Pharmaceuticals Ltd.

最高研发阶段批准上市

首次获批日期

(1997-01-01),

丛集性头痛低血压偏头痛

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构

分子式C7H19N2O4PS

InChIKeyCSYSULGPHGCBQD-UHFFFAOYSA-N

CAS号21704-46-1

关联

2

项与 S-乙基异硫脲二乙基磷酸盐相关的临床试验

NCT00482287 / Withdrawn临床2期

A Phase II, Randomized, Double Blind, Placebo-controlled, Dose-escalating Study to Assess the Pharmacokinetics and Pharmacodynamics of MTR105 in Cardiac Surgery Induced Hypotension Patients During Weaning Off Cardiopulmonary Bypass

The purpose of this study is to evaluate the safety, pharmacokinetic and the pharmacodynamic effects of escalating doses of MTR105 while weaning from bypass in a hypotensive population of cardiac surgery patients.

开始日期2008-01-01

申办/合作机构

Meditor Pharmaceuticals Ltd.

NCT00448071 / Unknown status临床2期IIT

A Phase II, Randomized Double Blind Placebo-Controlled, Dose Escalating Study to Determine Pharmacokinetic and Pharmacodynamic Effects of MTR107 in End-Stage Renal Disease (ESRD) Patients

MTR107 effect on blood pressure throught the dialysis procedure and its ability to prevent Intra dialytic Hypotension

开始日期2006-05-01

申办/合作机构

Wolfson Medical Center

[+1]

100 项与 S-乙基异硫脲二乙基磷酸盐相关的临床结果

登录后查看更多信息

100 项与 S-乙基异硫脲二乙基磷酸盐相关的转化医学

登录后查看更多信息

100 项与 S-乙基异硫脲二乙基磷酸盐相关的专利（医药）

登录后查看更多信息

4

项与 S-乙基异硫脲二乙基磷酸盐相关的文献（医药）

2021-10-01·Investigational New Drugs3区 · 医学

Discovery of MTR-106 as a highly potent G-quadruplex stabilizer for treating BRCA-deficient cancers

3区 · 医学

Article

作者: Zhang, Yong-Liang ; Li, Meng-Zhu ; Xiong, Bing ; Miao, Ze-Hong ; Shen, Jing-Kang ; Song, Shan-Shan ; Ma, Lan-Ping ; Zhang, Ning ; Bao, Xu-Bin ; Meng, Tao ; He, Jin-Xue ; Yu, Ting

G-quadruplexes (G4s) are DNA or RNA structures formed by guanine-rich repeating sequences. Recently, G4s have become a highly attractive therapeutic target for BRCA-deficient cancers. Here, we show that a substituted quinolone amide compound, MTR-106, stabilizes DNA G-quadruplexes in vitro. MTR-106 displayed significant antiproliferative activity in homologous recombination repair (HR)-deficient and PARP inhibitor (PARPi)-resistant cancer cells. Moreover, MTR-106 increased DNA damage and promoted cell cycle arrest and apoptosis to inhibit cell growth. Importantly, its oral and i.v. administration significantly impaired tumor growth in BRCA-deficient xenograft mouse models. However, MTR-106 showed modest activity against talazoparib-resistant xenograft models. In rats, the drug rapidly distributes to tissues within 5 min, and its average concentrations were 12-fold higher in the tissues than in the plasma. Overall, we identified MTR-106 as a novel G-quadruplex stabilizer with high tissue distribution, and it may serve as a potential anticancer agent.

2008-01-01·Cardiology4区 · 医学

Nitric Oxide Synthase Inhibitor (MTR-105) during Open-Heart Surgery

4区 · 医学

Article

作者: Borer, Jeffrey S. ; Manolache, Gheorghe ; Ciubotaru, Anatol ; Schachner, Arie ; Ureche, Andrei ; Sasson, Lior

Objectives: Hypotension is common immediately following cardiopulmonary bypass. Experimentally, MTR-105 (S-ethylisothiuronium diethylphosphate), a fast-acting synthetic nitric oxide synthase inhibitor, rapidly increases blood pressure. The purpose of the current study was to assess the influence of MTR-105 on hemodynamics early after cardiopulmonary bypass in patients undergoing open-heart surgery. Methods:Thirty-six patients with an ejection fraction >50% undergoing open-heart surgery were randomly assigned to either 50 µg kg–1 min–1 MTR-105 (M50, n = 12), 10 µg kg–1 min–1 MTR-105 (M10, n = 12) or buffered phosphate solution (placebo control, n = 12). Half suffered from atrial fibrillation and 75% had severe tricuspid regurgitation. Patients received the drug for 6 h after cross-clamp removal. Hemodynamic variables were measured before drug administration until 24 h after operation. Adverse events were recorded from study drug initiation through 30 days after the operation. Results:Compared with control, both MTR-105 doses were associated with an immediate increase in systemic blood pressure (16%) and systemic vascular resistance and a decrease in cardiac index. Half-life time of MTR-105 was calculated to be 4.1 ± 0.8 h (M10) and 4.45 ± 0.92 h (M50). Three patients died during hospitalization, unrelated to the study medication. Conclusions:At the doses employed, MTR-105 appears hemodynamically active in increasing both blood pressures.

Radiatsionnaia biologiia, radioecologiia

[The estimation of the nitric oxide role in the aggravation of combined radiation-thermal injuries].

Article

作者: Budagov, R S ; Skvotsov, V G ; Ul'ianova, L P ; Proskuriakov, S Ia

The influence of specific inhibitor of inducible NO synthase S-ethil-isothiourea (as "Difetur" preparation) on liver NO production level, and 30-days survival, mean survival time and probability of mortality within animals under combined radiation/thermal injury (CRTI) were evaluated. Experiments were carrying out on mice (whole body gamma-irradiation at the dose of 7 Gy + 10% body surface full-thickness thermal burn). It was shown, that CRTI induce 2-fold statistical significant increase of NO production in liver of experimental animals. Mice pretreatment with Difetur preparation lead to practically full inhibition of NO production. In the group of animals, with Difetur administration during first two days after CRTI 60% mice survived as compared 15% survive in control group. In pair with data on probability of mortality it was suggested that growth of NO production in the early period of CRTI increase sensitivity of animals to pathological processes leading to death on 10-12 days.

100 项与 S-乙基异硫脲二乙基磷酸盐相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	S-乙基异硫脲二乙基磷酸盐	C	-

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
丛集性头痛	-	-	1997-01-01
低血压	-	-	1997-01-01
偏头痛	-	-	1997-01-01

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
低血压	临床2期	美国	Meditor Pharmaceuticals Ltd.	2008-01-01
透析性低血压	临床前	以色列	Meditor Pharmaceuticals Ltd.	2006-05-01
终末期肾脏病	临床前	以色列	Meditor Pharmaceuticals Ltd.	2006-05-01