Delving into the Latest Updates on Implitapide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [1]

Target

MTTP

Mechanism

MTTP inhibitors(Microsomal triglyceride transfer protein inhibitors)

Therapeutic Areas

Congenital DisordersEndocrinology and Metabolic DiseaseOther Diseases

Active Indication-

Inactive Indication

Heterozygous familial hypercholesterolemiaHomozygous familial hypercholesterolemiaHypercholesterolemia+ [2]

Originator Organization

Aegerion Pharmaceuticals, Inc.

Active Organization-

Inactive Organization

Medical Research Laboratories International, Inc.

Aegerion Pharmaceuticals, Inc.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC35H37N3O2

InChIKeyKIMRCJZMVARVSU-DITALETJSA-N

CAS Registry177469-96-4

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.

01 May 2006·Cellular and Molecular Life SciencesQ2 · BIOLOGY

Lipid-lowering drugs

Q2 · BIOLOGY

Review

Author: 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.

01 Jan 2005·Biological and Pharmaceutical BulletinQ4 · MEDICINE

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

Q4 · MEDICINE

Article

Author: 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 Deals associated with Implitapide

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB04852

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Homozygous familial hypercholesterolemia	Phase 2	NO	Medical Research Laboratories International, Inc.	01 Sep 2003
Homozygous familial hypercholesterolemia	Phase 2	NL	Medical Research Laboratories International, Inc.	01 Sep 2003
Homozygous familial hypercholesterolemia	Phase 2	CA	Medical Research Laboratories International, Inc.	01 Sep 2003
Homozygous familial hypercholesterolemia	Phase 2	US	Medical Research Laboratories International, Inc.	01 Sep 2003
Homozygous familial hypercholesterolemia	Phase 2	IL	Medical Research Laboratories International, Inc.	01 Sep 2003
Hyperlipoproteinemia Type II	Phase 2	CA	Medical Research Laboratories International, Inc.	01 Sep 2003
Hyperlipoproteinemia Type II	Phase 2	NO	Medical Research Laboratories International, Inc.	01 Sep 2003
Hyperlipoproteinemia Type II	Phase 2	NL	Medical Research Laboratories International, Inc.	01 Sep 2003
Hyperlipoproteinemia Type II	Phase 2	US	Medical Research Laboratories International, Inc.	01 Sep 2003
Hypercholesterolemia	Phase 2	-	Aegerion Pharmaceuticals, Inc.	-