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Issue 57, 2020
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In vivo and in vitro studies of antisense oligonucleotides – a review

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Abstract

The potential of antisense oligonucleotides in gene silencing was discovered over 40 years ago, which resulted in the growing interest in their chemistry, mechanism of action, and metabolic pathways. This review summarizes the selected mechanisms of antisense drug action, as well as therapeutics which are to date approved by the Food and Drug Administration and European Medicines Agency. Moreover, bioanalytical methods used for ASO pharmacokinetics and metabolism studies are briefly summarized. Special attention is paid to the primary pharmacokinetic properties of the different chemistry classes of antisense oligonucleotides. Moreover, in vivo and in vitro metabolic pathways of these compounds are widely described with the emphasis on the different animal models as well as in vitro models, including tissues homogenates, enzyme solutions, and human liver microsomes.

Graphical abstract: In vivo and in vitro studies of antisense oligonucleotides – a review

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Article information


Submitted
05 Jun 2020
Accepted
06 Sep 2020
First published
17 Sep 2020

This article is Open Access

RSC Adv., 2020,10, 34501-34516
Article type
Review Article

In vivo and in vitro studies of antisense oligonucleotides – a review

A. Kilanowska and S. Studzińska, RSC Adv., 2020, 10, 34501
DOI: 10.1039/D0RA04978F

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    [Original citation] - Published by The Royal Society of Chemistry.

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