| Apolipoprotein B synthesis inhibition: results from clinical trials. | |
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MedLine Citation:
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PMID: 20508521 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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PURPOSE OF REVIEW: Mipomersen is a second-generation antisense oligonucleotide developed to inhibit the synthesis of apolipoprotein B-100 in the liver. In this review we will summarize the results of recent preclinical and clinical studies addressing safety and low-density lipoprotein-cholesterol (LDL-c) lowering efficacy of this new compound. RECENT FINDINGS: In phase 3 clinical trials, mipomersen has been shown to significantly reduce LDL-c in patients with homozygous and heterozygous familial hypercholesterolemia on maximally tolerated lipid-lowering therapy. Injection site reactions, flu-like symptoms and increases in liver transaminases were the main adverse events. A recent safety study, designed to investigate the effects of mipomersen on intrahepatic triglyceride content, failed to show evidence of clinically relevant hepatic steatosis after 13 weeks of treatment. SUMMARY: Mipomersen is a new agent to lower LDL-c in patients at increased risk of cardiovascular disease and/or intolerant to statins. Whereas safety concerns have focused on hepatic fat accumulation, to date no evidence of clinically relevant increases of intrahepatic triglyceride content are reported. Ongoing and future studies are eagerly awaited to assess the impact of mipomersen on hepatic triglyceride content after prolonged exposure. |
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Authors:
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Maartje E Visser; John J P Kastelein; Erik S G Stroes |
Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Current opinion in lipidology Volume: 21 ISSN: 1473-6535 ISO Abbreviation: Curr. Opin. Lipidol. Publication Date: 2010 Aug |
Date Detail:
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Created Date: 2010-07-13 Completed Date: 2010-10-08 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9010000 Medline TA: Curr Opin Lipidol Country: England |
Other Details:
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Languages: eng Pagination: 319-23 Citation Subset: IM |
Affiliation:
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Department of Vascular Medicine, Academic Medical Center Amsterdam, The Netherlands. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Apolipoproteins B / biosynthesis*, metabolism Clinical Trials as Topic Drug Toxicity Humans Oligonucleotides / adverse effects, pharmacology Protein Biosynthesis / drug effects* |
| Chemical | |
Reg. No./Substance:
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0/Apolipoproteins B; 0/ISIS 301012; 0/Oligonucleotides |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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