IP Library Granted Patent US 9,987,245
Granted Patent B2
US 9,987,245 · App. 14/875,342 · Granted Jun 5, 2018

Therapeutic regimen and methods for treating or ameliorating visual disorders associated with an endogenous retinoid deficiency

Inventors: H. Andrew Strong (North Vancouver, CA); Suzanne Cadden (North Vancouver, CA)
Assignee: Novelion Therapeutics Inc.
A61K31/22A61K9/0048A61K9/0053A61K31/215Y10S514/912
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Quick Facts
Patent No.
US 9,987,245
App. No.
14/875,342
Granted
Jun 5, 2018
Kind
B2
Abstract

Disclosed herein are therapeutic regimens for treating or ameliorating a visual disorder associate with an endogenous retinoid deficiency in a subject by administering a therapeutically effective amount of a synthetic retinal derivative or a pharmaceutically acceptable composition comprising a synthetic retinal derivative according to the therapeutic regimen which leads to local recovery of visual functions such as visual fields, visual acuity and retinal sensitivity, among others.

Claims (60)

1. A method for treating a human patient suffering from the loss or impairment of vision caused by Retinitis Pigmentosa (RP), wherein said patient is deficient in endogenous 11-cis-retinal, comprising the steps of:

a) administering to the human patient an initial therapeutically effective dose of a synthetic retinal derivative selected from the group consisting of 9-cis-retinyl acetate, 9-cis-retinyl formate, 9-cis-retinyl succinate, 9-cis-retinyl citrate, 9-cis-retinyl ketoglutarate, 9-cis-retinyl fumarate, 9-cis-retinyl malate, 9-cis-retinyl oxaloacetate, 9-cis-retinyl propionate, 9-cis-retinyl butyrate, 9-cis-retinyl valerate, 9-cis-retinyl hexanoate, 9-cis-retinyl heptanoate, 9-cis-retinyl octanoate, 9-cis-retinyl nonanoate, 9-cis-retinyl decanoate, 9-cis-retinyl undecanoate, 9-cis-retinyl dodecanoate 9-cis-retinyl oxalate, 9-cis-retinyl malonate, 9-cis-retinyl glutarate, 9-cis-retinyl adipate, 9-cis-retinyl pimelate, 9-cis-retinyl suberate, 9-cis-retinyl azelate, and 9-cis-retinyl sebacate,

b) refraining from administering to the human patient an additional therapeutically effective dose of the synthetic retinal derivative for a resting interval, wherein the resting interval is a time period between 1 month and 9 months, and

c) administering to the human patient the additional therapeutically effective dose of the synthetic retinal derivative.

2. The method of claim 1 , wherein the initial dose is administered in a single dose.

3. The method of claim 1 , wherein the initial dose is administered in a divided dose over a period of up to two weeks.

4. The method of claim 1 , wherein the initial dose is administered in a divided dose over a period of from 5 to 14 days.

5. The method of claim 1 , wherein the initial dose is administered in a divided dose over a period of 7 to 10 days.

6. The method of claim 1 , wherein the initial dose is administered in a divided dose over a period of one week.

7. The method of claim 1 , wherein the initial dose is administered in a divided dose over a period of two weeks.

8. The method of claim 3 , wherein the initial dose is administered as equal daily amounts over the dosing period.

9. The method of claim 1 , wherein the synthetic retinal derivative is 9-cis-retinyl acetate.

10. The method of claim 1 , wherein the initial dose is in the range of from 70 mg/m 2 to 525 mg/m 2 .

11. The method of claim 1 , wherein the initial dose is in the range of from 49 mg/m 2 to 840 mg/m 2 .

12. The method of claim 11 , wherein the initial dose is in the range of from 49 mg/m 2 to 280 mg/m 2 .

13. The method of claim 1 , wherein the initial dose is in the range of from 70 mg/m 2 to 490 mg/m 2 .

14. The method of claim 1 , wherein the initial dose is in the range of from 280 mg/m 2 to 490 mg/m 2 .

15. The method of claim 1 , wherein the initial dose is in the range of from 70 mg/m 2 to 280 mg/m 2 .

16. The method of claim 15 , wherein the initial dose is 280 mg/m 2 .

17. The method of claim 1 , wherein the initial dose of a synthetic retinal derivative is administered orally.

18. The method of claim 1 , wherein the initial dose of a synthetic retinal derivative is administered by intraocular injection.

19. The method of claim 1 , wherein the resting interval is a time period between 1 month and 2 months.

20. The method of claim 1 , wherein the resting interval is a time period between 1 month and 3 months.

21. The method of claim 1 , wherein the resting interval is a time period between 1 month and 6 months.

22. The method of claim 1 , wherein the resting interval is a time period between 3 and 6 months.

23. The method of claim 1 , wherein the resting interval is a time period between 6 and 9 months.

24. The method of claim 1 , wherein the resting interval is a time period between 3 and 9 months.

25. The method of claim 1 , wherein the RP is caused by a mutation in the LRAT gene.

26. The method of claim 1 , wherein the RP is caused by a mutation in the RPE65 gene.

27. The method of claim 1 , wherein the dose in step c) is lower than the amount of the first therapeutic dose.

28. The method of claim 1 , wherein the dose in step c) is the same as the amount of the first therapeutic dose.

29. The method of claim 1 , wherein the dose in step c) is higher than the amount of the first therapeutic dose.

30. A method for treating a human patient suffering from loss or impairment of vision due to inherited mutations in RPE65 or LRAT genes associated with Retinitis Pigmentosa, comprising the steps of:

a) administering to the human patient an initial therapeutically effective dose of a 9-cis-retinyl acetate,

b) refraining from administering to the human patient an additional therapeutically effective dose of the 9-cis-retinyl acetate for a resting interval, wherein the resting interval is a time period between 1 month and 9 months, and

c) administering to the human patient the additional therapeutically effective dose of the 9-cis-retinyl acetate.

31. The method of claim 30 , wherein the initial dose is administered in a divided dose over a period of up to two weeks.

32. The method of claim 30 , wherein the initial dose is administered in a divided dose over a period of from 5 to 14 days.

33. The method of claim 30 , wherein the initial dose is administered in a divided dose over a period of from 7 to 10 days.

34. The method of claim 30 , wherein the initial dose is administered in a divided dose over a period of one week.

35. The method of claim 30 , wherein the initial dose is administered as equal daily amounts over the dosing period.

36. The method of claim 30 , wherein the initial dose is in the range of from 49 mg/m 2 to 840 mg/m 2 .

37. The method of claim 30 , wherein the initial dose is in the range of from 70 mg/m 2 to 525 mg/m 2 .

38. The method of claim 30 , wherein the initial dose is in the range of from 70 mg/m 2 to 280 mg/m 2 .

39. The method of claim 30 , wherein the initial dose is in the range of from 49 mg/m 2 to 840 mg/m 2 .

40. The method of claim 39 , wherein the initial dose is in the range of from 49 mg/m 2 to 280 mg/m 2 .

41. The method of claim 40 , wherein the initial dose is 280 mg/m 2 .

42. The method of claim 30 , wherein the initial dose of a synthetic retinal derivative is administered orally.

43. The method of claim 30 , wherein the initial dose of a synthetic retinal derivative is administered by intraocular injection.

44. The method of claim 30 , wherein the resting interval is a time period between 1 month and 2 months.

45. The method of claim 30 , wherein the resting interval is a time period between 1 month and 3 months.

46. The method of claim 30 , wherein the resting interval is a time period between 1 month and 6 months.

47. The method of claim 30 , wherein the resting interval is a time period between 3 months and 6 months.

48. The method of claim 30 , wherein the resting interval is a time period between 6 months and 9 months.

49. The method of claim 30 , wherein the resting interval is a time period between 3 months and 9 months.

50. The method of claim 30 , wherein the RP is caused by a mutation in the LRAT gene.

51. The method of claim 30 , wherein the RP is caused by a mutation in the RPE65 gene.

52. The method of claim 30 , wherein the dose in step c) is lower than the amount of the first therapeutic dose.

53. The method of claim 30 , wherein the dose in step c) is the same as the amount of the first therapeutic dose.

54. The method of claim 30 , wherein the dose in step c) is higher than the amount of the first therapeutic dose.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 9, 2022
From: RETINAGENIX HOLDINGS LLC
To: ELUMINEX BIOSCIENCES (SUZHOU) LIMITED
Reel/Frame 060763/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 7, 2021
From: RETINAGENIX THERAPEUTICS, INC.
To: RETINAGENIX HOLDINGS LLC
Reel/Frame 055857/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 20, 2020
From: RETINAGENIX, LLC
To: RETINAGENIX THERAPEUTICS, INC.
Reel/Frame 052175/0176 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 21, 2019
From: NOVELION THERAPEUTICS INC.
To: RETINAGENIX, LLC
Reel/Frame 048403/0004 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2017
From: STRONG, H. ANDREW; CADDEN, SUZANNE
To: QLT INC.
Reel/Frame 042245/0425 →
CHANGE OF NAME Recorded May 4, 2017
From: QLT INC.
To: NOVELION THERAPEUTICS INC.
Reel/Frame 042245/0563 →
Continuity (5)
Continuation 13090215 · Apr 19, 2011
Provisional Application 61447611 · Feb 28, 2011
Provisional Application 61407436 · Oct 27, 2010
Provisional Application 61325763 · Apr 19, 2010
Related Publication 20170087114A1 · Mar 30, 2017