辛伐他汀/烟酸(Simvastatin/Nicotinic Acid) - 药物靶点：HCAR3 x HMG-CoA reductase x NIACR1_在研适应症：高甘油三酯血症，原发性高胆固醇血症，原发性高脂血症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Niacin/simvastatin、Niaspan/simvastatin、Nicotinic acid/simvastatin

+ [4]

靶点

HCAR3 x HMG-CoA reductase x NIACR1

作用机制

HCAR3激动剂(烟酸G蛋白偶联受体HM74激动剂)、HMG-CoA reductase抑制剂(羟甲基戊二酰辅酶A合酶抑制剂)、NIACR1激动剂(羟基酸受体-2激动剂)

治疗领域

内分泌与代谢疾病

在研适应症

高甘油三酯血症原发性高胆固醇血症原发性高脂血症

非在研适应症-

原研机构

AbbVie, Inc.

在研机构-

非在研机构

Abbott Laboratories

最高研发阶段临床3期

首次获批日期

美国 (2008-02-15),

血脂障碍

最高研发阶段(中国)临床3期

特殊审评-

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结构

分子式C31H43NO7

InChIKeyWNWXXAPGHTVCDL-OKDJMAGBSA-N

CAS号1054452-10-6

关联

5

项与辛伐他汀/烟酸相关的临床试验

CTR20131900 / Recruiting临床3期

辛伐他汀烟酸缓释片治疗原发性高脂血症的随机、双盲、阳性药平行对照、多中心临床试验

以辛伐他汀片为对照，评价辛伐他汀烟酸缓释片治疗原发性高脂血症的有效性和安全性

开始日期2013-01-08

申办/合作机构

山东百诺医药股份有限公司

CTR20132025 / Recruiting

辛伐他汀烟酸缓释片人体药代动力学试验

对辛伐他汀烟酸缓释片进行人体药代动力学评价；测定主要成分辛伐他汀、烟酸和代谢物辛伐他汀酸、烟酰胺和烟脲酸的经时血药浓度和尿药浓度，估算其主要药代动力学参数，了解辛伐他汀烟酸缓释片在健康人体内的吸收、分布、消除、代谢规律。

开始日期2012-12-21

申办/合作机构

山东百诺医药股份有限公司

NCT01178320 / CompletedN/AIIT

Carotid Plaque Characteristics by MRI in AIM-HIGH

Heart attacks and strokes caused by the unstable atherosclerotic plaques remain the leading cause of death in the United States. Unstable plaques often have more fat than stable plaques. This study will investigate if a treatment with LDL-lowering plus HDL-raising compared with LDL-lowering alone would more effectively reduce the plaque fat content assessed by magnetic resonance imaging (MRI), therefore, further reducing heart attacks and strokes.

开始日期2008-03-01

申办/合作机构

University of Washington

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100 项与辛伐他汀/烟酸相关的临床结果

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100 项与辛伐他汀/烟酸相关的转化医学

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100 项与辛伐他汀/烟酸相关的专利（医药）

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8

项与辛伐他汀/烟酸相关的文献（医药）

2019-12-01·Trials4区 · 医学

The Evaluation of Vitiligous lesions Repigmentation after the Administration of Atorvastatin calcium salt and Simvastatin-acid sodium salt in patients with active vitiligo (EVRAAS), a pilot study: study protocol for a randomized controlled trial

4区 · 医学

ArticleOA

作者: Kowaliszyn, Bogna ; Winnicki, Andrzej ; Kosmalski, Tomasz ; Niezgoda, Anna ; Czajkowski, Rafał ; Krysiński, Jerzy

BACKGROUNDVitiligo is a chronic skin disorder presenting with depigmentation, the pathogenesis of which is complex but the autoimmune theory is now preferred. Multiple immunologic processes, including stimulation of the T-helper (Th)1 response, formation of autoreactive melanocyte-specific CD8⁺ T lymphocytes, a decrease in the blood concentration of T regulatory (Treg) cells, and an increase in interleukin (IL)-17 and interferon (IFN) concentration, have been shown to contribute to vitiligo progression and maintenance. The aim of this study is to evaluate the influence of simvastatin and atorvastatin on vitiligous lesions in patients with nonsegmental vitiligo (NSV). According to available data, statins act through several immunological pathways, potentially reversing undesirable phenomena underlying autoimmune vitiligo pathogenesis.METHODS/DESIGNA study has been designed as a single-center, randomized, double-blind, placebo-controlled pilot study with the enrollment of at least 24 active NSV patients presenting with vitiligous lesions on both upper and lower limbs. The clinical effects of ointments containing 1% simvastatin-acid sodium salt or 1% atorvastatin calcium salt applied on a preselected limb will be assessed in comparison with vehicle ointment applied on the opposite limb. All study participants will undergo clinical evaluation using body surface area (BSA) and Vitiligo Area Scoring Index (VASI) scales at baseline and at weeks 4, 8, and 12 time points. A precise assessment of skin lesions will be performed using photographic documentation obtained during each study visit and processed with NIS-Elements software.DISCUSSIONCurrently available vitiligo topical therapeutic approaches including calcineurin inhibitors and corticosteroids remain poorly effective and are associated with either relatively high cost or potentially dangerous adverse effects. The clinical application of orally administrated statins, widely used as systemic cholesterol-lowering agents, in vitiligous patients has only been tested in two clinical trials; however, data on their potential usefulness is scarce. Moreover, due to a high risk of clinically significant toxicity, topical administration was recommended by researchers. This study is the first to evaluate safety and efficacy of the topical use of statins in patients presenting with NSV.TRIAL REGISTRATIONClinicaltrials.gov, NCT03247400 . Registered on 05 August 2017.

2011-09-01·Geriatric Nursing3区 · 医学

Focus on Statin Safety Concerns

3区 · 医学

Article

作者: Lefkovitz, Allen ; Zarowitz, Barbara

Muscle complaints, including rhabdomyolysis (severe muscle damage), related to the cholesterol-lowering medications known as statins, are a class effect. Following preliminary data from the Study of the Effectiveness of Additional Reductions in Cholesterol and Homocysteine (SEARCH) trial showing increased muscle injuries, the Food and Drug Administration (FDA) began reviewing the safety of simvastatin, particularly the high-dose 80-mg simvastatin, in March 2010. On June 8, 2011, the Food and Drug Administration (FDA) released the updated product information with revised safety warnings regarding myopathy and rhabdomyolysis associated with products for high cholesterol that contain simvastatin. Simvastatin is the generic form of Zocor and is the statin contained in both Vytorin (simvastatin and ezetimibe) and Simcor (simvastatin and niacin extended-release). From the SEARCH trial and analysis of the FDA’s Adverse Event Reporting System (AERS) database, the FDA found that fatal rhabdomyolysis was significantly more common with 80 mg compared with 20 mg of simvastatin, and that overall rates of myopathy and rhabdomyolysis were higher in simvastatin 80 mg versus lower doses of simvastatin or other statins (e.g., atorvastatin, pravastatin, etc.). The risks for both myopathy and rhabdomyolysis were highest for 80 mg simvastatin during the first 12 months of treatment and are shown in Table 1. Both older age and female sex were seen as risk factors for

2010-11-01·Drugs in R&D4区 · 医学

Niacin Extended Release (ER)/Simvastatin (Simcor®)

4区 · 医学

ReviewOA

作者: Lyseng-Williamson, Katherine A

Oral fixed-dose niacin extended release/simvastatin is associated with clinically relevant improvements in plasma lipid profiles, including lowering of non-high-density lipoprotein cholesterol levels, relative to simvastatin monotherapy in patients with mixed dyslipidemias who had not responded fully to simvastatin monotherapy, and is generally well tolerated.

100 项与辛伐他汀/烟酸相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	辛伐他汀/烟酸	C10AD52	-

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
高甘油三酯血症	临床3期	中国	-	2013-01-08
原发性高胆固醇血症	临床3期	中国	-	2013-01-08
原发性高脂血症	临床3期	中国	-	2013-01-08