Antisense oligonucleotide composite

JP2024015491A5Pending Publication Date: 2025-10-03LIID PHARM INC
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Patent Information

Application Number
JP2023200811
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2021-12-07
Filing Date
2023-11-28
Publication Date
2025-10-03

AI Technical Summary

Technical Problem

Existing antisense oligonucleotides face challenges with off-target toxicity due to hybridization-dependent and hybridization-independent mechanisms, hindering their clinical use and expansion of indications.

Method used

A novel antisense oligonucleotide complex, BROTHERS, is developed with a toehold region and a complementary strand that forms a well-controlled higher-order structure, reducing toxicity by minimizing hybridization-dependent effects and enhancing nuclease resistance.

Benefits of technology

BROTHERS effectively suppresses hepatotoxicity and nephrotoxicity while maintaining antisense activity, demonstrating reduced toxicity and efficient gene expression regulation in target cells.

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Abstract

To provide a novel antisense oligonucleotide composite with reduced toxicity while having activity of antisense oligonucleotide, a pharmaceutical composition containing the antisense oligonucleotide composite, and a composition for regulating expression of a target gene which contains the antisense composite.SOLUTION: An antisense oligonucleotide composite having an antisense effect and reduced toxicity contains antisense oligonucleotide, and a complementary strand including a sequence complementary with the antisense oligonucleotide, where the antisense oligonucleotide has a toehold of a single-stranded structure, and the complementary strand has nuclease tolerance over the entire length.SELECTED DRAWING: None
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