IP Library › Granted Patent US 12,357,607
Granted Patent B2
US 12,357,607 · App. 18/083,922 · Granted Jul 15, 2025

Compositions and methods for intravenous administration of 2-bromo-1-(3,3-dinitroazetidin-1-yl)ethanone

Inventors: Bryan T. Oronsky (Los Altos Hills, CA); Jan Scicinski (Saratoga, CA); Scott Caroen (San Francisco, CA)
Assignee: EPICENTRX, INC.
A61K31/397A61K9/0019A61K31/194A61K31/727A61K35/14A61K47/10A61K47/18A61P35/00A61P35/02A61K9/08A61K47/46
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Quick Facts
Patent No.
US 12,357,607
App. No.
18/083,922
Granted
Jul 15, 2025
Kind
B2
Abstract

The invention provides compositions and methods for intravenous administration of 2-bromo-1-(3,3-dinitroazetidin-1-yl)ethanone (ABDNAZ), including formulations containing, autologous whole blood and ABDNAZ that can be rapidly administered to a patient by intravenous infusion without any significant pain at the site of infusion.

Claims (41)

1. A formulation for intravenous administration to a patient, comprising:

at least 60% v/v of whole blood;

at least 10 μg/mL of 2-bromo-1-(3,3-dinitroazetidin-1-yl) ethanone (ABDNAZ);

and

an anticoagulant.

2. The formulation of claim 1 , wherein the formulation further comprises a polyethylene glycol, and wherein the polyethylene glycol has a number average molecular weight in the range of about 200 g/mol to about 600 g/mol.

3. The formulation of claim 2 , wherein the polyethylene glycol has a number average molecular weight of about 400 g/mol.

4. The formulation of claim 1 , wherein the anticoagulant is selected from the group consisting of heparin and a citrate salt, or a combination thereof.

5. The formulation of claim 1 , wherein the anticoagulant is a solution comprising an alkali metal citrate salt, dextrose, and water.

6. The formulation of claim 1 , wherein the formulation comprises at least 20 μg/mL of ABDNAZ.

7. The formulation of claim 1 , wherein the formulation comprises at least 50 μg/mL of ABDNAZ.

8. The formulation of claim 1 , wherein the formulation comprises at least 100 μg/mL of ABDNAZ.

9. The formulation of claim 1 , wherein the formulation comprises at least 150 μg/mL of ABDNAZ.

10. The formulation of claim 1 , wherein the formulation comprises about 10 μg/mL to about 1 mg/mL of ABDNAZ.

11. The formulation of claim 1 , wherein the formulation comprises about 10 μg/mL to about 0.5 mg/mL of ABDNAZ.

12. The formulation of claim 1 , wherein the formulation comprises about 10 μg/mL to about 250 μg/mL of ABDNAZ.

13. The formulation of claim 1 , wherein the formulation comprises about 20 μg/mL to about 200 μg/mL of ABDNAZ.

14. The formulation of claim 1 , wherein the whole blood constitutes at least 60% wt./wt. of the formulation.

15. The formulation of claim 1 , wherein the whole blood constitutes at least 75% wt./wt. of the formulation.

16. The formulation of claim 1 , wherein the whole blood constitutes at least 90% wt./wt. of the formulation.

17. The formulation of claim 1 , wherein the whole blood constitutes from about 60% wt./wt. to about 99% wt./wt. of the formulation.

18. The formulation of claim 1 , wherein the whole blood constitutes from about 70% wt./wt. to about 95% wt./wt. of the formulation.

19. The formulation of claim 1 , wherein the whole blood constitutes from about 75% wt./wt. to about 90% wt./wt. of the formulation.

20. The formulation of claim 1 , wherein there is from about 90 mL to about 110 mL of whole blood in the formulation.

21. The formulation of claim 1 , wherein there is from about 95 mL to about 105 mL of whole blood in the formulation.

22. The formulation of claim 1 , wherein there is about 100 mL of whole blood in the formulation.

23. The formulation of claim 1 , wherein there is about 10 mL to about 20 mL of whole blood in the formulation.

24. The formulation of claim 1 , wherein the formulation is in the form of a unit dose having a volume in the range of about 50 mL to about 200 mL.

25. The formulation of claim 1 , wherein the formulation is in the form of a unit dose having a volume in the range of about 75 mL to about 150 mL.

26. The formulation of claim 1 , wherein the formulation is in the form of a unit dose having a volume in the range of about 90 mL to about 140 mL.

27. The formulation of claim 1 , wherein the formulation is in the form of a unit dose having a volume in the range of about 100 mL to about 140 mL.

28. The formulation of claim 1 , wherein the formulation is in the form of a unit dose having a volume in the range of about 100 mL to about 120 mL.

29. The formulation of claim 1 , wherein the formulation is in the form of a unit dose having a volume in the range of about 10 mL to about 30 mL.

30. The formulation of claim 1 , wherein the formulation further comprises a polyethylene glycol, wherein the polyethylene glycol is present at a concentration of from about 0.4 μL/mL to about 4 μL/mL in the formulation.

31. The formulation of claim 1 , wherein the formulation further comprises N,N-dimethylacetamide, wherein the N,N-dimethylacetamide is present at a concentration of from about 0.2 μL/mL to about 2 μL/mL in the formulation.

32. The formulation of claim 1 , wherein intravenous administration of the formulation to the patient causes any pain experienced by the patient at the site of administration that is no greater than Grade 2.

33. The formulation of claim 1 , wherein intravenous administration of the formulation to the patient causes any pain experienced by the patient at the site of administration that is no greater than Grade 1.

34. The formulation of claim 1 , wherein the whole blood is autologous whole blood.

35. The formulation of claim 1 , wherein the patient has cancer, and the formulation is suitable for administration to the patient in order to treat the cancer.

36. The formulation of claim 1 , wherein the formulation comprises at least 1 mg/ml of ABDNAZ.

37. The formulation of claim 1 , wherein the formulation comprises 2 mg/mL of ABDNAZ.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 19, 2023
From: ORONSKY, BRYAN T.; SCICINSKI, JAN; CAROEN, SCOTT
To: EPICENTRX, INC.
Reel/Frame 064320/0084 →
Continuity (3)
Division 16069012
Provisional Application 62277236 · Jan 11, 2016
Related Publication 20230233524A1 · Jul 27, 2023
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