IP Library Granted Patent US 9,949,993
Granted Patent B2
US 9,949,993 · App. 15/623,274 · Granted Apr 24, 2018

Compositions for administration of zoledronic acid or related compounds for treating low back pain

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Quick Facts
Patent No.
US 9,949,993
App. No.
15/623,274
Granted
Apr 24, 2018
Kind
B2
Abstract

Oral dosage forms of osteoclast inhibitors, such as zoledronic acid, in an acid or a salt form can be used to treat or alleviate pain or related conditions, such as chronic low back pain.

Claims (30)

1. A method of treating chronic low back pain comprising orally administering a dosage form comprising zoledronic acid in an acid form or a salt form to a human being in need thereof, wherein the bioavailability of zoledronic acid in the dosage form is about 1.8% to about 2.5%, as determined when orally administered to a human being who has fasted for eight hours.

2. The method of claim 1 , wherein the bioavailability of zoledronic acid in the dosage form is about 1.8% to 2.3%, as determined when orally administered to a human being who has fasted for eight hours.

3. The method of claim 1 , wherein a single oral administration of the dosage form to the human being results in an AUC for zoledronic acid of about 130 ng·hr/mL to about 160 ng·hr/mL.

4. The method of claim 1 , wherein the dosage form is orally administered three times within a period of six months.

5. The method of claim 1 , wherein the dosage form is orally administered six times within a period of six months.

6. The method of claim 1 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 4 on the 0-10 numeric rating scale.

7. The method of claim 1 , wherein the human being has suffered from low back pain for at least 3 months.

8. The method of claim 1 , wherein a single oral administration of the dosage form to the human being results in an AUC for zoledronic acid of about 300 ng·hr/mL to about 350 ng·hr/mL.

9. The method of claim 1 , wherein a single oral administration of the dosage form to the human being results in an AUC for zoledronic acid of about 405 ng·hr/mL to about 450 ng·hr/mL.

10. The method of claim 1 , wherein orally administering the dosage form to the human being results in a C max of zoledronic acid of about 30 ng/mL to about 50 ng/mL.

11. The method of claim 1 , wherein orally administering the dosage form to the human being results in a C max of zoledronic acid of about 50 ng/mL to about 80 ng/mL.

12. The method of claim 1 , wherein orally administering the dosage form to the human being results in a C max of zoledronic acid of about 80 ng/mL to about 120 ng/mL.

13. The method of claim 1 , wherein an amount of a non-steroidal anti-inflammatory drug that is administered to the human being is reduced after the dosage form is orally administered.

14. The method of claim 1 , wherein the low back pain is associated with a type 1 Modic change.

15. The method of claim 1 , wherein the low back pain is associated with a type 2 Modic change.

16. A method of treating chronic low back pain comprising orally administering zoledronic acid to a human being in need thereof, wherein the amount of zoledronic acid orally administered to the human being within a period of about one month is about 200 mg to about 300 mg.

17. The method of claim 16 , wherein the zoledronic acid is in an acid form.

18. The method of claim 16 , wherein the zoledronic acid is in a salt form.

19. The method of claim 16 , wherein the zoledronic acid is in a disodium salt form.

20. The method of claim 16 , wherein the zoledronic acid is orally administered in at least two consecutive doses that are at least about 1 week apart.

21. The method of claim 16 , wherein the AUC of zoledronic acid in the human being, measured over a period of one month, is about 100 ng·hr/mL to about 500 ng·hr/mL.

22. The method of claim 16 , wherein the AUC of zoledronic acid in the human being, measured over a period of one month, is about 500 ng·hr/mL to about 1000 ng·hr/mL.

23. The method of claim 16 , wherein the AUC of zoledronic acid in the human being, measured over a period of one month, is about 500 ng·hr/mL to about 700 ng·hr/mL.

24. The method of claim 16 , wherein the AUC of zoledronic acid in the human being, measured over a period of one month, is about 700 ng·hr/mL to about 1000 ng·hr/mL.

25. The method of claim 16 , wherein the human being has suffered from low back pain for at least 2 months.

26. The method of claim 16 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 4 on the 0-10 numeric rating scale.

27. The method of claim 16 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 5 on the 0-10 numeric rating scale.

28. The method of claim 16 , wherein the low back pain is associated with a Modic change.

29. The method of claim 16 , wherein the low back pain is associated with a type 1 Modic change.

30. The method of claim 16 , wherein the low back pain is associated with a type 2 Modic change.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 10, 2018
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 045034/0542 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 8, 2017
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 044777/0488 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 8, 2017
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 043234/0837 →