1492984-65-2
Chemical Structure
Inotersen
Synonym(s): GSK-2998728; ISIS-420915
- CAS No.: 1492984-65-2
- Formula:N/A
- Molecular Weight:7183.08
SMILES: [Inotersen]
Biological Activity: Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy[1][2][3][4].
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Inotersen | 96.44% | Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy. | ||||||||||||||||||||
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- [1]. Mathew V, et al. Inotersen: new promise for the treatment of hereditary transthyretin amyloidosis. Drug Des Devel Ther. 2019;13:1515-1525. Published 2019 May 6. [Content Brief]
- [2]. Yu RZ, et al. Immunogenicity Assessment of Inotersen, a 2'-O-(2-Methoxyethyl) Antisense Oligonucleotide in Animals and Humans: Effect on Pharmacokinetics, Pharmacodynamics, and Safety. Nucleic Acid Ther. 2020;30(5):265-275. [Content Brief]
- [3]. Durwin A. The Effect of Cellular Glucose Levels on Inotersen-Mediated Target Reduction in in vitro Cell Models[J]. 2025.
- [4]. Kim TW, et al. Carcinogenicity assessment of inotersen in Tg.rasH2 mice and Sprague-Dawley rats: Implications for 2'-MOE antisense oligonucleotides. Regul Toxicol Pharmacol. 2025;155:105743. [Content Brief]
Keywords
