IP Library Granted Patent US 10,821,189
Granted Patent B2
US 10,821,189 · App. 15/565,666 · Granted Nov 3, 2020

CD38 ligand-drug conjugates for targeted cancer therapy

Inventor: Youli Zu (Bellaire, TX)
A61K47/549A61K31/704A61K48/00C07H21/04C12N15/115C12N15/117C12N2310/16C12N2310/351C12N2310/3511
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Quick Facts
Patent No.
US 10,821,189
App. No.
15/565,666
Granted
Nov 3, 2020
Kind
B2
Abstract

Disclosed are compositions and methods relating to nucleic acid aptamers that specifically target CD38 protein and also selective binding to CD38-expressing cells. The ligand-drug conjugates specifically target CD38-expressing cancer cells and subsequently internalize into the cell.

Claims (10)

1. A method of targeting CD38 cells with an agent, the method comprising conjugating a nucleic acid aptamer comprising a region that interacts with a CD38 cell to the agent, and exposing CD38 cells to the aptamer-agent conjugate, wherein the nucleic acid comprises SEQ ID NO: 1 or SEQ ID NO: 2.

2. The method of claim 1 , wherein the nucleic acid aptamer comprises a G-C (guanine-cysteine) repeat region.

3. The method of claim 2 , wherein the G-C repeat region is 5′ or 3′ of the region that interacts with CD38.

4. The method of claim 2 , wherein the G-C repeat region comprises at least 80% guanine (G) and cysteine (C) nucleic acids.

5. The method of claim 2 , wherein the aptamer comprises at least eight (8) consecutive guanine or cysteine nucleotides.

6. The method of claim 1 , wherein the agent is a small molecule, organometallic compound, nucleic acid, protein, peptide, lipid, carbohydrate, hormone, metal, radioactive element, gelonin, phototoxic agent, drug, vaccine, or immunological agent.

7. The method of claim 1 , wherein the agent is non-covalently associated with the nucleic acid and rapidly released from aptamer in a pH<5.5 environment.

8. The method of claim 2 , wherein the agent intercalates in the G-C repeat region.

9. The method of claim 1 , wherein the agent is a therapeutic agent.

10. The method of claim 9 , wherein the therapeutic agent causes apoptosis of CD38-expressing cells.

Continuity (2)
Provisional Application 62145781 · Apr 10, 2015
Related Publication 20180078649A1 · Mar 22, 2018