IP Library Granted Patent US 9,956,238
Granted Patent B2
US 9,956,238 · App. 15/787,612 · Granted May 1, 2018

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

Inventor: Herriot Tabuteau (New York, NY)
Assignee: ANTECIP BIOVENTURES II LLC
A61K31/675A61K9/0053A61K9/20A61K9/2004A61K9/28A61K31/663A61K45/06A61K47/12
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Quick Facts
Patent No.
US 9,956,238
App. No.
15/787,612
Granted
May 1, 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 low back pain.

Claims (30)

1. A method of treating 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 150 mg to about 250 mg.

2. The method of claim 1 , wherein the zoledronic acid is in an acid form.

3. The method of claim 1 , wherein the zoledronic acid is in a salt form.

4. The method of claim 1 , wherein the zoledronic acid is in a disodium salt form.

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

6. The method of claim 1 , 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.

7. The method of claim 1 , 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.

8. The method of claim 1 , 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.

9. The method of claim 1 , 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.

10. The method of claim 1 , wherein the human being has suffered from low back pain for at least 2 months.

11. 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.

12. The method of claim 1 , 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.

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

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 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 1.1% to about 1.5%, as determined when orally administered to a human being who has fasted for eight hours.

17. The method of claim 16 , wherein a single oral administration of the dosage form results in an AUC for zoledronic acid of about 130 ng·hr/mL to about 160 ng·hr/mL.

18. The method of claim 16 , wherein a single oral administration of the dosage form results in an AUC for zoledronic acid of about 300 ng·hr/mL to about 350 ng·hr/mL.

19. The method of claim 16 , wherein a single oral administration of the dosage form results in an AUC for zoledronic acid of about 405 ng·hr/mL to about 450 ng·hr/mL.

20. The method of claim 16 , wherein the dosage form contains about 100 mg to about 200 mg of the zoledronic acid based on the weight of the diacid form.

21. The method of claim 16 , wherein the dosage form is orally administered three times within a period of six months.

22. The method of claim 16 , wherein the dosage form is orally administered at an interval of about 2 weeks.

23. The method of claim 16 , wherein an amount of a non-steroidal anti-inflammatory drug that is orally administered to the human being is reduced after the dosage form comprising zoledronic acid in the acid form or the salt form is orally administered.

24. The method of claim 16 , wherein the zoledronic acid is in a salt form, wherein the imidazole ring of zoledronic acid is in an imidazolium form.

25. 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.

26. The method of claim 16 , wherein, at the beginning of treatment, the human being has an average weekly pain intensity of at least 6 on the 0-10 numeric rating scale.

27. The method of claim 16 , wherein the human being has suffered from low back pain for at least 3 months.

28. The method of claim 16 , wherein the human being has a type 1 Modic change.

29. The method of claim 16 , wherein the human being has a type 2 Modic change.

30. The method of claim 16 , wherein the human being is at least 40 years of age.

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 Nov 9, 2017
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 044081/0434 →
Continuity (14)
Continuation In Part 15378939 · Dec 14, 2016
Continuation In Part 15348808 · Nov 10, 2016
Continuation In Part PCTUS2015032739 · May 27, 2015
Continuation PCTUS2014050427 · Aug 8, 2014
Continuation 14279241 · May 15, 2014
Continuation In Part 15211827 · Jul 15, 2016
Continuation 14968514 · Dec 14, 2015
Continuation 14540333 · Nov 13, 2014
Continuation 14481097 · Sep 9, 2014
Continuation 14288720 · May 28, 2014
Continuation 14288241 · May 27, 2014
Continuation In Part 15136092 · Apr 22, 2016
Provisional Application 62150871 · Apr 22, 2015
Related Publication 20180055862A1 · Mar 1, 2018