US 2013/0172402 A1 · OLIGONUCLEOTIDE, AND THERAPEUTIC AGENT FOR DYSLIPIDEMIA CONTAINING OLIGONUCLEOTIDE AS ACTIVE INGREDIENT

Oligonucleotide, and therapeutic agent for dyslipidemia containing oligonucleotide as active ingredient

AssigneesOsaka University, Tokyo University of Science Educational Foundation Administrative Organization, National Cerebral and Cardiovascular Center

InventorsSatoshi Obika, Takeshi Imanishi, Tsuyoshi Yamamoto, Keisuke Narukawa, Mariko Shiba, Tetsuji Yamaoka, Hidetaka Torigoe, Atsushi Yamashita, Yoichi Tachibana, Sachiro Kakinoki, Kiyomi Sasaki

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Abstract

An object of the present invention is to provide an oligonucleotide useful as a therapeutic agent for dyslipidemia that has excellent binding affinity to the PCSK9 gene as well as stability and safety. The oligonucleotide of the present invention contains a sugar-modified nucleoside, the sugar-modified nucleoside has a bridging structure between 4′-position and 2′-position, and the oligonucleotide can bind to the human PCSK9 gene. Also, the present invention provides a therapeutic agent for dyslipidemia containing the oligonucleotide as an active ingredient, and the therapeutic agent preferably contains a bioabsorbable material as a carrier. The bioabsorbable material is preferably atelocollagen or peptide gel.

Claims14

Dependent claims

An oligonucleotide comprising a sugar-modified nucleoside,

the sugar-modified nucleoside having a bridging structure between 4′-position and 2′-position, and
the oligonucleotide being capable of binding to human PCSK9 gene.

Dependencies are inferred from the claim text.

Facts

Application

13/819,722Filed 31 Aug 2011

Priority

JP 2010-19518731 Aug 2010

Published

4 Jul 2013

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Classification16 codes

C12N 15/1137
Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming…: against enzymes
A61K 9/0019
Galenical forms characterised by the site of application: injectable compositions; Intramuscular, intravenous, arterial, subcutaneous…
A61K 9/0021
Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in…
A61K 9/06
Medicinal preparations characterised by special physical form: ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels