Chemoembolization agents

Patent metadata

Field	Value
Publication number	US-12357570-B2
Application number	US-202318211428-A
Country	US
Kind code	B2
Filing date	Jun 19, 2023
Priority date	May 26, 2017
Publication date	Jul 15, 2025
Grant date	Jul 15, 2025

Abstract

Described herein is a chemoembolization therapy, which combines therapeutic effects of peripheral arterial occlusion with the local administration of an anti-cancer agent. A particle or microsphere occludes the arteries providing blood flow to the tumor, resulting in tumor oxygen deprivation. The anti-angiogenic agent is an anti-cancer drug, as described herein.

First claim

What is claimed is:

1. A method of treating a cancer in a subject, the method comprising administering to a subject in need thereof a pharmaceutical composition of a pharmaceutically effective amount of a chemoembolization agent, comprising:
an embolizing particle or microsphere;
an encapsulating agent, the encapsulating agent being affixed to the embolizing particle or microsphere through ionic or other non-covalent interactions,
one or more therapeutic agents contained within the encapsulating agent,
wherein each therapeutic agent is independently uncharged or weakly charged or has low solubility in aqueous media at physiological pH; and
wherein the encapsulating agent is configured to release the one or more therapeutic agents.

2. The method of claim 1 , wherein the pharmaceutically effective amount of the chemoembolization agent is administered by catheter into an arterial blood vessel that vascularizes a solid tumor of the cancer of the subject.

3. The method of claim 2 , wherein the arterial blood vessel is a hepatic artery.

4. The method of claim 1 , wherein the cancer is liver cancer.

5. The method of claim 4 , wherein the liver cancer is hepatocellular carcinoma.

6. The method of claim 1 , wherein an amount of the one or more therapeutic agents to be administered to the subject from the encapsulated agent is at a dose of about 0.01 mg/kg of body weight to about 10 mg/kg body weight.

7. The method of claim 1 , wherein the chemoembolization agent is comprised of one therapeutic agent contained within the encapsulating agent, wherein the one therapeutic agent is weakly negatively charged.

8. The method of claim 1 , wherein the chemoembolization agent is comprised of one therapeutic agent contained within the encapsulating agent, wherein the one therapeutic agent is weakly positively charged.

9. The method of claim 1 , wherein the chemoembolization agent is comprised of one therapeutic agent contained within the encapsulating agent, wherein the one therapeutic agent is an anti-cancer agent.

10. The method of claim 9 , wherein the anti-cancer agent is selected from the group consisting of Sorafenib, Regorafenib, Lenvatinib, Tirapazamine, Cabozantinib, and Sunitinib.

11. The method of claim 9 , wherein the anti-cancer agent is Sorafenib, Regorafenib, or Lenvatinib.

12. The method of claim 1 wherein the chemoembolization agent further comprises a non-encapsulated therapeutic agent affixed via a releasable mechanism to the embolizing particle or microsphere.

13. The method of claim 1 , wherein the embolizing particle or microsphere is a polyvinyl alcohol material.

14. The method of claim 1 , wherein the embolizing particle or microsphere is selected from the group consisting of beads of sulfonate functionalized polyvinyl alcohol hydrogels, acetalized polyvinyl alcohol hydrogels, hydrogel cores made of sodium poly (methacrylate) coated with poly bis[trifluoroethoxy]phosphazene, and polyvinyl alcohol-co-sodium acrylate cross-linked hydrogels, and hydrogel networks of polyethylene glycol and 3-sulfopropyl acrylate.

15. The method of claim 1 , wherein the encapsulating agent is a liposome.

16. The method of claim 15 , wherein the liposome is a cationic liposome.

17. The method of claim 16 , wherein the cationic liposome comprises a mixture of DOTAP and DOPC.

18. The method of claim 17 , wherein the mixture of DOTAP and DOPC ranges from a 1:9 to 9:1 molar ratio of DOTAP to DOPC.

Assignees

• Bruin Biosciences Inc
• Univ California

Inventors

• Na James
• Imagawa David
• Tucci Fabio
• Beaton Graham
• Ravula Satheesh

Classifications

• A61K47/24

  containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids · CPC title

• A61K31/53

  having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine (melarsoprol A61K31/555 {; with four nitrogen atoms A61K31/495}) · CPC title

• A61K31/47

  Quinolines; Isoquinolines · CPC title

• A61K31/44 Primary

  Non condensed pyridines; Hydrogenated derivatives thereof · CPC title

• A61K31/404

  Indoles, e.g. pindolol · CPC title