US 12,291,708 B2
Oral delivery of antisense conjugates targeting PCSK9
Henrik Oerum, Copenhagen (DK); Stewart Alwyn Noble, San Diego, CA (US); and Charles Lester Shear, Collegeville, PA (US)
Assigned to CiVi Biopharma, Inc., Chevy Chase, MD (US)
Filed by CiVi Biopharma, Inc., Chevy Chase, MD (US)
Filed on Dec. 10, 2021, as Appl. No. 17/547,879.
Claims priority of provisional application 63/261,505, filed on Sep. 22, 2021.
Claims priority of provisional application 63/178,340, filed on Apr. 22, 2021.
Claims priority of provisional application 63/134,884, filed on Jan. 7, 2021.
Claims priority of provisional application 63/124,581, filed on Dec. 11, 2020.
Prior Publication US 2022/0213476 A1, Jul. 7, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. C12N 15/113 (2010.01); A61K 31/7088 (2006.01); A61P 3/06 (2006.01); A61P 43/00 (2006.01); C12N 15/11 (2006.01)
CPC C12N 15/113 (2013.01) [A61K 31/7088 (2013.01); A61P 3/06 (2018.01); A61P 43/00 (2018.01); C12N 15/111 (2013.01); C12N 2310/11 (2013.01); C12N 2310/313 (2013.01); C12N 2310/315 (2013.01); C12N 2310/321 (2013.01); C12N 2310/3231 (2013.01); C12N 2310/341 (2013.01); C12N 2310/351 (2013.01); C12N 2320/33 (2013.01)] 14 Claims
 
1. A pharmaceutical composition for oral delivery to a subject comprising
(i) an antisense oligonucleotide of formula I (SEQ ID NO: 19)

OG Complex Work Unit Chemistry

OG Complex Work Unit Chemistry

OG Complex Work Unit Chemistry
and,
(ii) N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC) or a salt thereof,
in a tablet or capsule comprising a pH-sensitive enteric coating, wherein the pharmaceutical composition is formulated to release the antisense oligonucleotide of formula I in the subject's small intestine following oral administration.