IP Library Granted Patent US 10,576,101
Granted Patent B2
US 10,576,101 · App. 15/556,183 · Granted Mar 3, 2020

Roneparstat combined therapy of multiple myeloma

Inventors: Ralph D. Sanderson (Birmingham, AL); Vishnu Prakash C. Ramani (Birmingham, AL); Alessandro Noseda (Mendrisio, CH); Paola Barbieri (Mendrisio, CH)
Assignees: Leadiant Biosciences SA; The UAB Research Foundation
A61K31/727A61K31/198A61K38/05A61K38/07A61K2300/00
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Quick Facts
Patent No.
US 10,576,101
App. No.
15/556,183
Granted
Mar 3, 2020
Kind
B2
Abstract

The present invention relates to roneparstat for use in a combined therapy for the treatment of multiple myeloma. In particular it has unexpectedly been found that the combined use of roneparstat with a proteasome inhibitor, in particular selected between bortezomib and carfilzomib or with melphalan improve efficacy in decreasing the overall tumor burden, especially showing synergism, with respect to the administration of each active ingredient alone.

Claims (37)

1. A method for treating or preventing a multiple myeloma in an individual in need thereof, comprising administering to the individual in need thereof a combined therapy comprising:

(a) a roneparstat, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and;

(b) (i) a melphalan or a pharmaceutically acceptable salt, hydrate or solvate thereof, (ii) a proteasome inhibitor, or (iii) a combination thereof,

wherein said component (a) and said component (b) are separately or sequentially administered at an effective amount that is determined by synergistic reduction of immunoglobulin light chain kappa level.

2. The method of claim 1 , wherein said proteasome inhibitor comprises: a bortezomib or a pharmaceutically acceptable salt, hydrate or solvate thereof; a carfilzomib or a pharmaceutically acceptable salt, hydrate or solvate thereof; or, a combination thereof.

3. The method of claim 1 , wherein the multiple myeloma is at any stage, or is a recurrent, refractory or relapsed myeloma.

4. The method of claim 1 , wherein the roneparstat is administered in a subcutaneous dose of from about 100 to about 600 mg daily.

5. The method of claim 1 , wherein said proteasome inhibitor for the combined therapy comprises a bortezomib administered in a dose of about 1.3 mg/m 2 by intravenous bolus, optionally on days 1, 4, 8 and 11, or optionally at a 21-day cycle for a maximum of eight cycles.

6. The method of claim 1 , wherein said proteasome inhibitor for the combined therapy is carfilzomib and it is administered intravenously in a dose of 20 mg/m 2 /day, optionally on two consecutive days each week for three weeks.

7. The method of claim 1 , wherein for the combined therapy the melphalan is administered intravenously in a dose of about 16 mg/m 2 , optionally as a single infusion over 15 to 20 minutes.

8. The method of claim 1 , wherein for the combined therapy the melphalan is administered in an oral dose of about 6 mg once a day for 2 to 3 weeks.

9. A method of treating a human suffering from multiple myeloma, plasma cell myeloma, or recurrent, refractory or relapsed myeloma comprising administering to the human in need thereof a therapeutically effective amount of a pharmaceutical composition or a therapeutic combination comprising:

(a) a roneparstat, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and;

(b) (i) a melphalan or a pharmaceutically acceptable salt, hydrate or solvate thereof, (ii) a proteasome inhibitor, or (iii) a combination thereof,

wherein said component (a) and said component (b) are separately or sequentially administered at the effective amount that is determined by synergistic reduction of immunoglobulin light chain kappa level.

10. A method for inhibiting, treating, or preventing multiple myeloma, plasma cell myeloma, or recurrent, refractory or relapsed myeloma in a subject, said method comprising administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition or a therapeutic combination comprising:

(a) a roneparstat, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and;

(b) (i) a melphalan or a pharmaceutically acceptable salt, hydrate or solvate thereof, (ii) a proteasome inhibitor, or (iii) a combination thereof,

wherein said component (a) and said component (b) are separately or sequentially administered at the effective amount that is determined by synergistic reduction of immunoglobulin light chain kappa level.

11. The method of claim 1 , wherein said component (a) and said component (b) are formulated independently.

12. The method of claim 1 , wherein said component (a) and said component (b) are separately packaged.

13. The method of claim 1 , wherein said component (a) and said component (b) are packaged or formulated together.

14. The method of claim 9 , wherein the proteasome inhibitor comprises: a bortezomib or a pharmaceutically acceptable salt, hydrate or solvate thereof; a carfilzomib or a pharmaceutically acceptable salt, hydrate or solvate thereof; or, a combination thereof.

15. The method of claim 10 , wherein the proteasome inhibitor comprises: a bortezomib or a pharmaceutically acceptable salt, hydrate or solvate thereof; a carfilzomib or a pharmaceutically acceptable salt, hydrate or solvate thereof; or, a combination thereof.

16. The method of claim 9 , wherein the roneparstat is administered in a subcutaneous dose of from between about 100 to about 600 mg daily.

17. The method of claim 10 , wherein the roneparstat is administered in a subcutaneous dose of from about 100 to about 600 mg daily.

18. The method of claim 1 , wherein the combined therapy comprises:

(a) a roneparstat, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and;

(b) a melphalan or a pharmaceutically acceptable salt, hydrate or solvate thereof.

19. The method of claim 1 , wherein the combined therapy comprises:

(a) a roneparstat, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and;

(b) a proteasome inhibitor.

20. The method of claim 19 , wherein the proteasome inhibitor comprises bortezomib.

21. The method of claim 19 , wherein the proteasome inhibitor comprises carfilzomib.

22. The method of claim 1 , wherein the combined therapy comprises:

(a) a roneparstat, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and;

(b) (i) a melphalan or a pharmaceutically acceptable salt, hydrate or solvate thereof, and (ii) a proteasome inhibitor.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 4, 2020
From: LEADIANT BIOSCIENCES S.A. IN LIQUIDAZIONE
To: LEADIANT BIOSCIENCES S.P.A.
Reel/Frame 051715/0840 →
CHANGE OF NAME Recorded Dec 16, 2019
From: LEADIANT BIOSCIENCES SA
To: LEADIANT BIOSCIENCES SA IN LIQUIDAZONE
Reel/Frame 051316/0268 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 21, 2019
From: LEADIANT BIOSCIENCES S.A.
To: LEADIANT BIOSCIENCES S.P.A.
Reel/Frame 050782/0176 →
CHANGE OF NAME Recorded May 16, 2019
From: SIGMA TAU RESEARCH SWITZERLAND SA
To: LEADIANT BIOSCIENCES SA
Reel/Frame 049217/0322 →
Continuity (3)
Provisional Application 62129221 · Mar 6, 2015
Provisional Application 62153899 · Apr 28, 2015
Related Publication 20180050061A1 · Feb 22, 2018