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US 2022/0054645 A1Published application
Targeted Delivery of Therapeutic Molecules
AssigneePeter ZHANG
InventorsXiaoyong LU, David M. EVANS, Patrick Y. LU, Alan LU, Jon XU, Peter Zhang
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Abstract
The invention relates to the targeted delivery of therapeutic molecules to organs, tissues, and cells of humans and other mammals. The invention is directed to a chemical construct for delivering such therapeutic molecules and to methods of making and using the constructs.
Claims32
A chemical construct comprising the formula:
- A-B—[—C-D]n
- wherein A comprises a first linker (linker 1), B comprises a bridge, C comprises a second linker (linker 2), D comprises a targeting ligand, and n is an integer from 1-4, wherein linker 1 and linker 2 can be the same or different, and wherein linker 1 comprises a linear polyethylene glycol as shown in the first structure below, wherein n1 is an integer between 1-50, or linker 1 comprises a poly(L-lactide) as shown in the second structure below, wherein n2 is an integer from 1-70, and wherein Z (shown in structures below) is a functional group, such as thiol or carboxylic acid, which will react with a maleimide or an amine to conjugate covalently with the bridge.
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A construct for delivering an oligonucleotide to a human hepatocyte, comprising the structure:
- O-A-B—[—C-D]n
- wherein O comprises an oligonucleotide, A comprises a first linker (linker 1), B comprises a bridge, C comprises a second linker (linker 2), D comprises a targeting ligand, and n is an integer from 1-4 wherein the oligonucleotide comprises an siRNA that is between 10-27 nucleotides long and wherein the siRNA optionally is fully or partially chemically modified at a 2′ position or a phosphorothioate bond linkage.
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Dependencies are inferred from the claim text.