Merck Sharp + Dohme Corp.

Jeffrey G Aaronson

Steven L Colletti

Thomas Joseph Tucker

Weimin Wang

David M Tellers

Matthew G Stanton

Rob Burke

Rubina G Parmar

Kathleen B Calati

Boyoung Kim

Anthony W Shaw

Yu Yuan

Stanley F Barnett

Vasant R Jadhav

René Bartz

Aaron A Momose

Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L)-(G); wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; each of a and b is independently 0, 1, 2, 3 or 4; and (2) a composition comprising (P)-(L)-(G); wherein P is a peptide and each occurrence of P is independently selected from Table 2; L is a linker and each occurrence of L is independently selected from Table 3; G is a targeting ligand and each occurrence of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.

Dual molecular delivery of oligonucleotides and peptide containing conjugates

In an embodiment the instant invention discloses a modular composition comprising 1) an oligonucleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at any 3' and/or 5&#x2032; end; 3) one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.

Single chemical entities and methods for delivery of oligonucleotides

Growing community of inventors

Philadelphia, PA, United States of America

Jeffrey G Aaronson