Method and conjugate for treating h. pylori infection

Details Method and conjugate for treating h. pylori infection Method and conjugate for treating h. pylori infection

C - Chemistry, Metallurgy

12

N

C12N 15/11 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C07H 21/04 (2006.01)

Patent

CA 2278924

A method and conjugate for treating H. pylori infection in a subject are disclosed. The conjugate is composed of (a) a nuclease-resistant antisense oligomer effective to inhibit H. pylori infection in the subject by base- specific Watson-Crick binding to an H. pylori mRNA transcript, and (b) a transport moiety conjugated to the oligomer. The transport moiety is effective to facilitate uptake of the conjugate from the environment of the stomach into the cytoplasm of H. pylori cells by active transport or by pH-gradient transport across of the cell membrane of H. pylori. The conjugate is administered by oral route, preferably in a swellable polymer bolus designed to release the conjugate in sustained release.

L'invention concerne une méthode et un conjugué pour traiter chez un sujet une infection à H. pylori. Le conjugué se compose: (a) d'un oligomère antisens résistant aux nucléases, efficace pour inhiber chez le sujet l'infection à H. pylori par une liaison Watson-Crick, spécifique de bases, à un transcrit d'ARNm de H. pylori et (b) d'une fraction de transport conjuguée à l'oligomère. La fraction de transport facilite efficacement l'absorption du conjugué se trouvant dans l'estomac, dans le cytoplasme des cellules H. pylori, le passage à travers la membrane cellulaire de H. pylori se faisant soit par transport actif, soit par transport à gradient de pH. On administre le conjugué par voie orale, de préférence dans un bol polymère dilatable conçu pour une libération prolongée du conjugué.

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