IP Library Granted Patent US 12,186,428
Granted Patent B2
US 12,186,428 · App. 17/986,430 · Granted Jan 7, 2025

Combination taxoid nanoemulsion with immunotherapy in cancer

Inventors: James E. Egan (Stony Brook, NY); Mansoor M. Amiji (Attleboro, MA); Iwao Ojima (Port Jefferson, NY)
Assignees: TargaGenix, Inc.; The Research Foundation for the State University of New York; Northeastern University
A61K9/1075A61K31/337A61K39/39558A61K47/44A61K47/542A61P35/00C07K16/2827A61K2039/505
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Quick Facts
Patent No.
US 12,186,428
App. No.
17/986,430
Granted
Jan 7, 2025
Kind
B2
Abstract

A composition of an omega-3 polyunsaturated fatty acid (PUFA)-taxoid conjugate formulated in an oil-in-water nanoemulsion (NE) drug delivery system in combination with an immune-oncology (IO) agent to enhance therapeutic efficacy in refractory cancers, such as PDAC. A method of treating cancer, by administering an effective amount of a pharmaceutical composition including an omega03 PUFA-taxoid conjugate in combination with an IO agent encapsulated in an NE drug delivery system to a subject in need of treatment, and treating cancer.

Claims (18)

1. A pharmaceutical composition comprising an omega-3 polyunsaturated fatty acid (PUFA)-taxoid conjugate formulated in an oil-in-water nanoemulsion (NE) drug delivery system in combination with an immune-oncology ( 10 ) agent of anti-PD-L1 antibody, wherein said PUFA-taxoid conjugate is NE-DHA-SBT-1214.

2. The pharmaceutical composition of claim 1 , wherein said PUFA is chosen from the group consisting of docosahexaenoic acid (DHA), eicosapentaenoic acid (EPA), and alpha-linolenic acid (LNA).

3. The pharmaceutical composition of claim 1 , wherein said oil-in-water NE includes omega-3 fatty acid-rich edible oil.

4. The pharmaceutical composition of claim 3 , wherein said omega-3 fatty acid-rich edible oil is chosen from the group consisting of fish oil, flax-seed oil, pine nut oil, safflower oil, primrose oil, black currant oil, borage oil, wheat germ oil, chia oil, hemp oil, perilla oil, grape oil, squalene oil, and fungal oil.

5. The pharmaceutical composition of claim 3 , wherein said omega-3 fatty acid-rich edible oil is modified with a compound chosen from the group consisting of surfactants and targeting agents.

6. A method of treating cancer, including the steps of:

administering an effective amount of a pharmaceutical composition including a PUFA-taxoid conjugate encapsulated in an NE drug delivery system, wherein said PUFA-taxoid conjugate is NE-DHA-SBT-1214, in combination with an IO agent of to a subject in need of treatment; and

treating pancreatic cancer.

7. The method of claim 6 , further including the steps of increasing expression of PD-L1 in the tumor microenvironment, increasing CD4 + and CD8 + tumor-infiltrating lymphocytes, and making the subject more responsive to the IO agent.

8. The method of claim 6 , wherein the cancer is highly drug resistant.

9. The method of claim 6 , further including the step of down-regulating survival genes in tumors and activating p53 and p21.

10. The method of claim 6 , wherein the PUFA is chosen from the group consisting of docosahexaenoic acid (DHA), eicosapentaenoic acid (EPA), and alpha-linolenic acid (LNA).

11. The method of claim 6 , further including the step of upregulating PD-L1.

12. The method of claim 6 , wherein the oil-in-water NE includes omega-3 fatty acid-rich edible oil.

13. The method of claim 12 , wherein the omega-3 fatty acid-rich edible oil is chosen from the group consisting of fish oil, flax-seed oil, pine nut oil, safflower oil, primrose oil, blackcurrant oil, borage oil, wheat germ oil, chia oil, hemp oil, perilla oil, grape oil, squalene oil, and fungal oil.

14. The method of claim 12 , wherein the omega-3 fatty acid-rich edible oil is modified with a compound chosen from the group consisting of surfactants and targeting agents.

15. The method of claim 6 , wherein a tumor treated has less dense stroma after treatment.

16. The method of claim 6 , further including the steps of increasing intra-tumoral IFN-gamma producing T cells and inducing infiltration of inflammatory macrophages.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2022
From: EGAN, JAMES E.; AMIJI, MANSOOR; OJIMA, IWAO
To: TARGAGENIX, INC.; THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK; NORTHEASTERN UNIVERSITY
Reel/Frame 061807/0710 →
Continuity (3)
Division 16225629 · Dec 19, 2018
Provisional Application 62608015 · Dec 20, 2017
Related Publication 20230082272A1 · Mar 16, 2023
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