英普他派(Implitapide) - 药物靶点：MTTP_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [1]

靶点

MTTP

作用机制

MTTP抑制剂(微粒体甘油三酯转运蛋白复合体抑制剂)

治疗领域

遗传病与畸形内分泌与代谢疾病其他疾病

在研适应症-

非在研适应症

杂合子家族性高胆固醇血症纯合子家族性高胆固醇血症高胆固醇血症+ [2]

原研机构

Aegerion Pharmaceuticals, Inc.

在研机构-

非在研机构

Medical Research Laboratories International, Inc.

Aegerion Pharmaceuticals, Inc.

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构

分子式C35H37N3O2

InChIKeyKIMRCJZMVARVSU-DITALETJSA-N

CAS号177469-96-4

关联

3

项与英普他派相关的临床试验

NCT00080132 / Terminated临床2期

An Open-Label, Dose-Escalating Efficacy and Safety Study of Implitapide in Patients With Hypertriglyceridemia (HTG) on Maximal, Concurrent Triglyceride-Lowering Therapy

The purpose of this study is to determine if implitapide is effective in lowering triglyceride (TG) levels in patients with Fredrickson Type I or V hypertriglyceridemia where the maximum tolerable medication and diet were not sufficient.

开始日期2004-10-01

申办/合作机构

Medical Research Laboratories International, Inc.

NCT00079859 / Terminated临床2期

Safety and Efficacy Study of Implitapide Compared With Placebo in Patients With Heterozygous Familial Hypercholesterolemia (HeFH) on Maximal Concurrent Lipid-Lowering Therapy

The purpose of this study is to determine if implitapide, used in conjunction with other lipid-lowering therapies, is safe and effective when compared to placebo in lowering low-density lipoprotein cholesterol (LDL-C) in patients with heterozygous familial hypercholesterolemia (HeFH).

开始日期2003-10-01

申办/合作机构

Medical Research Laboratories International, Inc.

NCT00079846 / Terminated临床2期

Safety and Efficacy Study of Implitapide Compared With Placebo in Patients With Homozygous Familial Hypercholesterolemia (HoFH) on Maximal Concurrent Lipid-Lowering Therapy

The purpose of this study is to determine if implitapide, used in conjunction with other lipid-lowering therapies, is safe and effective when compared to placebo in lowering low-density lipoprotein cholesterol (LDL-C) in patients with homozygous familial hypercholesterolemia (HoFH).

开始日期2003-09-01

申办/合作机构

Medical Research Laboratories International, Inc.

100 项与英普他派相关的临床结果

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100 项与英普他派相关的转化医学

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100 项与英普他派相关的专利（医药）

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5

项与英普他派相关的文献（医药）

2018-06-11·Angewandte Chemie International Edition1区 · 化学

Stereospecific Nucleophilic Substitution with Arylboronic Acids as Nucleophiles in the Presence of a CONH Group

1区 · 化学

Article

作者: Li, Chengxi ; Tian, Duanshuai ; Gu, Guoxian ; Peng, Henian ; Tang, Wenjun ; Zhang, Xumu

AbstractStereospecific nucleophilic substitution was achieved for the first time with arylboronic acids as nucleophiles. This transition‐metal‐free coupling between chiral α‐aryl‐α‐mesylated acetamides and arylboronic acids provided access to a series of chiral α,α‐diaryl acetamides with excellent enantioselectivity and moderate to good yields. The CONH functionality proved to be crucial for bridging the reactants and promoting the reaction. Efficient syntheses of a cannabinoid CB1 receptor ligand, the antidepressant (S)‐diclofensine, and a key chiral building block of the inhibitor implitapide were successfully accomplished by using this method.

2006-05-01·Cellular and Molecular Life Sciences2区 · 生物学

Lipid-lowering drugs

2区 · 生物学

Review

作者: Pahan, K

Although a change in life-style is often the method of first choice for lipid lowering, lipid-lowering drugs, in general, help to control elevated levels of different forms of lipids in patients with hyperlipidemia. While one group of drugs, statins, lowers cholesterol, the other group, fibrates, is known to take care of fatty acids and triglycerides. In addition, other drugs, such as ezetimibe, colesevelam, torcetrapib, avasimibe, implitapide, and niacin are also being considered to manage hyperlipidemia. As lipids are very critical for cardiovascular diseases, these drugs reduce fatal and nonfatal cardiovascular abnormalities in the general population. However, a number of recent studies indicate that apart from their lipid-lowering activities, statins and fibrates exhibit multiple functions to modulate intracellular signaling pathways, inhibit inflammation, suppress the production of reactive oxygen species, and modulate T cell activity. Therefore, nowadays, these drugs are being considered as possible therapeutics for several forms of human disorders including cancer, autoimmunity, inflammation, and neurodegeneration. Here I discuss these applications in the light of newly discovered modes of action of these drugs.

2005-01-01·Biological and Pharmaceutical Bulletin4区 · 医学

Implitapide, a Microsomal Triglyceride Transfer Protein Inhibitor, Reduces Progression of Atherosclerosis in Apolipoprotein E Knockout Mice Fed a Western-Type Diet: Involvement of the Inhibition of Postprandial Triglyceride Elevation

4区 · 医学

Article

作者: Ueshima, Koji ; Mutoh, Seitaro ; Nagayoshi, Akira ; Akihisa-Umeno, Hitomi ; Takakura, Shoji ; Matsuo, Masahiko

Microsomal triglyceride transfer protein (MTP) is essential for the synthesis of both chylomicron in the intestine and very low-density lipoprotein in the liver. An MTP inhibitor, (2S)-2-cyclopentyl-2-[4-[(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-yl)methyl]phenyl]-N-[(1S)-2-hydroxy-1-phenylethyl]ethanamide (implitapide), has been shown to suppress atherosclerosis in apolipoprotein E knockout (apoE KO) mice. To elucidate the antiatherosclerotic mechanisms of implitapide in the mice, we examined the effects on plasma lipid levels, triglyceride (TG) elevation after oral fat loading, and development of atherosclerosis in apoE KO mice fed a Western-type diet. Implitapide at a dosage of approximately 3.2 mg/kg/day significantly reduced both total cholesterol and TG levels during the 8-week treatment period. In addition, implitapide significantly inhibited the increase in plasma TG levels after oral olive oil loading tests conducted after 4 weeks of treatment. After the treatment, implitapide significantly suppressed the atherosclerotic lesion area by 83% compared with a control group. These results provide direct evidence that the antiatherosclerotic effects of implitapide in apoE KO mice are associated with the inhibition of postprandial TG elevation, in addition to the reduction of both plasma total cholesterol and TG levels.

100 项与英普他派相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB04852

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
纯合子家族性高胆固醇血症	临床2期	挪威	Medical Research Laboratories International, Inc.	2003-09-01
纯合子家族性高胆固醇血症	临床2期	荷兰	Medical Research Laboratories International, Inc.	2003-09-01
纯合子家族性高胆固醇血症	临床2期	加拿大	Medical Research Laboratories International, Inc.	2003-09-01
纯合子家族性高胆固醇血症	临床2期	美国	Medical Research Laboratories International, Inc.	2003-09-01
纯合子家族性高胆固醇血症	临床2期	以色列	Medical Research Laboratories International, Inc.	2003-09-01
II型高脂蛋白血症	临床2期	加拿大	Medical Research Laboratories International, Inc.	2003-09-01
II型高脂蛋白血症	临床2期	挪威	Medical Research Laboratories International, Inc.	2003-09-01
II型高脂蛋白血症	临床2期	荷兰	Medical Research Laboratories International, Inc.	2003-09-01
II型高脂蛋白血症	临床2期	美国	Medical Research Laboratories International, Inc.	2003-09-01
高胆固醇血症	临床2期	-	Aegerion Pharmaceuticals, Inc.	-