右甲状腺素钠(Dextrothyroxine Sodium) - 药物靶点：THR-α_专利_临床

概要

基本信息

药物类型

小分子化药

别名

dextrothyroxine sodium、右旋甲状腺素、Choloxin

靶点

THR-α

作用机制

THR-α激动剂(甲状腺激素受体α激动剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

冠状动脉疾病心肌梗塞

原研机构

AbbVie, Inc.

在研机构-

非在研机构

AbbVie, Inc.

National Institute for Materials Science IAI

最高研发阶段撤市

首次获批日期

美国 (1967-04-14)

最高研发阶段(中国)-

特殊审评-

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结构

分子式C15H12I4NNaO5

InChIKeyANMYAHDLKVNJJO-CURYUGHLSA-M

CAS号7054-08-2

关联

2

项与右甲状腺素钠相关的临床试验

NCT00000483 / CompletedN/AIIT

Coronary Drug Project Mortality Surveillance

To determine whether there were any long term sequelae of the drugs used in the Coronary Drug Project (estrogens, dextrothyroxine, nicotinic acid, clofibrate).

开始日期1981-06-01

申办/合作机构

National Heart, Lung & Blood Institute

NCT00000482 / Completed临床3期IIT

Coronary Drug Project

To determine whether regular administration of lipid modifying drugs (clofibrate, nicotinic acid, estrogen, dextrothyroxine) to men with a documented myocardial infarction would result in significant reduction in total mortality over a five year period. Secondarily, to determine whether the degree to which these drugs changed serum lipids was correlated with any effect on mortality and morbidity rates; to gain further information on the long-term prognosis of myocardial infarction (by studying the control group as intensively as the treatment group); to acquire further experience and knowledge concerning the techniques and methodology of long-term clinical trials; to determine, in a substudy, the effectiveness of aspirin, a platelet inhibitor, in reducing recurrences of myocardial infarction.

开始日期1965-04-01

申办/合作机构

National Heart, Lung & Blood Institute

100 项与右甲状腺素钠相关的临床结果

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100 项与右甲状腺素钠相关的转化医学

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100 项与右甲状腺素钠相关的专利（医药）

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107

项与右甲状腺素钠相关的文献（医药）

2005-09-01·The American Journal of Cardiology3区 · 医学

Diet, Lifestyle, and Nonstatin Trials: Review of Time to Benefit

3区 · 医学

Review

作者: Denke, Margo A

How rapidly benefits accrue from nonstatin, lipid-lowering therapies is a 21st-century question posed to data collected in the 20th century. The 3 early dietary trials conducted in institutional settings where diet was strictly controlled demonstrate that, compared with a control diet, cholesterol-lowering diets reduce coronary event rates over several years. These data do not reveal whether a more homogeneous high-risk population would demonstrate an earlier time to benefit. Dietary counseling trials of men with coronary disease conducted in the 1950s and 1960s failed to demonstrate a consistent benefit from dietary therapy, in part because of confounding factors from methodologic flaws in trial design. By the 1980s and 1990s, improvements in trial design, such as larger numbers of subjects, control of confounding risk factors, and limiting trial end points to those directly attributable to atherosclerotic events, were in place. Subsequently, 5 randomized clinical trials showed a consistent benefit of dietary therapy, with significant reductions by 1 to 2 years in fatal events, nonfatal events, and total mortality; 2 of these studies, each including omega-3 fatty acids as part of the dietary intervention, reported a rapid and significant time to benefit (within 3 to 6 months). Additional lifestyle benefits of cardiac rehabilitation (a surrogate for physical activity) and smoking cessation clearly show long-term benefit at 1 and 5 years, respectively. Nonstatin drug and surgical therapies either have shown no significant benefit (estrogen, dextrothyroxine) or benefit after 1 to 5 years of therapy (intestinal bypass surgery, cholestyramine, clofibrate, niacin, and a combination of niacin and clofibrate). In conclusion, rapid time to benefit has been observed in older lifestyle and nonstatin trials that have included omega-3 fatty acids as a component of dietary therapy. Lifestyle changes in diet, physical activity, weight loss, and smoking cessation remain important and effective therapies with which significant long-term benefits can be expected.

1999-02-01·Thyroid1区 · 医学

A Novel Resistance to Thyroid Hormone Associated with a New Mutation (T329N) in the Thyroid Hormone Receptor β Gene

1区 · 医学

Article

作者: Malezet-Desmoulins, C ; Mesmacque, A ; Bony-Trifunovic, H ; Margotat, A ; Dace, A ; Sarkissian, G ; Torresani, J

Resistance to thyroid hormone (RTH) is a syndrome of elevated serum thyroxine, inappropriately "normal" serum thyrotropin (TSH) and reduced thyroid hormone responsiveness associated with point mutations in the thyroid hormone receptor-beta (TRbeta) gene. We describe a novel point mutation resulting in a cytosine for adenine substitution at nucleotide 1271 (exon 9) that results in the substitution of threonine for asparagine (T329N). This mutation was identified in a 30-year-old woman who was investigated for recurrent spontaneous abortions and was found to have RTH. Dextrothyroxine (D-T4) therapy was instituted. At 8 mg per day 2 pregnancies followed with the delivery of a healthy boy and an RTH-affected girl another miscarriage occurred on D-T4 treatment at 6 mg per day. The T329N mutation, which was also identified in the daughter, markedly reduces the affinity of TRbeta for triiodothyronine (T3). Formation of T329N mutant TR homodimers and heterodimers with RXRalpha on thyroid hormone response element F2 (TRE F2) was not affected, but the ability of T3 to interrupt T329N mutant TRbeta homodimerization was markedly reduced. The T329N mutant TRbeta was transcriptionally inactive in transient expression assays. In cotransfection assays with wild-type TRbeta1, the mutant TRbeta1 functioned in a dominant negative manner. The results suggest that the T329N mutation in the T3-binding domain of TRbeta is responsible for RTH in the proposita's family.

1992-01-01·Thyroid1区 · 医学

Dextrothyroxine in the Treatment of Generalized Thyroid Hormone Resistance in a Boy Homozygous for a Defect in the T₃Receptor

1区 · 医学

Article

作者: Bercu, B B ; Schwartz, I D

The dextroisomer of thyroxine (D-T4) has been shown to have suppressive effects on pituitary TSH secretion in euthyroid individuals and patients with mild thyroid hormone resistance. We treated a 3-year-old boy with D-T4 who was homozygous for a T3 receptor defect, resulting in a complex clinical picture of tissue-specific hyperthyroidism and hypothyroidism. There was no evidence of significant alteration in thyroid physiology, including serum concentrations of basal and TRH stimulated TSH or echocardiographic parameters measuring systolic time interval. We conclude that D-T4 at a daily dose of 6 mg (0.65 mg/kg) was ineffective in this boy with homozygous dominant negative thyroid hormone resistance.

100 项与右甲状腺素钠相关的药物交易

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外链

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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
冠状动脉疾病	药物发现	-	National Institute for Materials Science IAI	1965-04-30
心肌梗塞	药物发现	-	National Institute for Materials Science IAI	1965-04-30