IP Library Granted Patent US 10,039,757
Granted Patent B2
US 10,039,757 · App. 15/426,804 · Granted Aug 7, 2018

C-Met modulator pharmaceutical compositions

Inventors: Jo Ann Wilson (San Francisco, CA); Khalid Shah (Half Moon Bay, CA)
Assignee: Exelixis, Inc.
A61K31/47A61K9/2009A61K9/2013A61K9/2018A61K9/2054A61K9/2095A61K9/28A61K9/2833A61K9/2893
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 10,039,757
App. No.
15/426,804
Granted
Aug 7, 2018
Kind
B2
Abstract

Pharmaceutical compositions and unit dosage forms comprising Compound I are disclosed.

Claims (77)

1. A method of treating kidney cancer, comprising administering to a patient in need of such treatment a tablet pharmaceutical composition comprising:

30-32 percent by weight of Compound I, L-malate salt wherein Compound I is:

38-40 percent by weight of microcrystalline cellulose;

18-22 percent by weight of lactose;

2-4 percent by weight of hydroxypropyl cellulose;

4-8 percent by weight of croscarmellose sodium;

0.2-0.6 percent by weight of colloidal silicon dioxide; and

0.5-1 percent by weight of magnesium stearate;

alone or in combination with another therapeutic agent.

2. The method of claim 1 , wherein the lactose in the tablet pharmaceutical composition is lactose anhydrous.

3. The method of claim 1 , wherein the tablet pharmaceutical composition further comprises a film coating containing hypromellose, titanium dioxide, triacetin, and iron oxide yellow.

4. The method of claim 1 , wherein the tablet pharmaceutical composition contains 20 to 100 mg of Compound I.

5. The method of claim 1 , wherein the tablet pharmaceutical composition contains 20, 25, 50, 60, 75, 80, or 100 mg of Compound I.

6. The method of claim 1 , wherein the kidney cancer is renal cell carcinoma.

7. A method of treating kidney cancer, comprising administering to a patient in need of such treatment a tablet pharmaceutical composition comprising, based on 100 weight/weight percent:

30-32 percent by weight of Compound I, L-malate salt wherein Compound I is:

38-40 percent by weight of microcrystalline cellulose;

18-22 percent by weight of lactose;

2-4 percent by weight of hydroxypropyl cellulose;

4-8 percent by weight of croscarmellose sodium;

0.2-0.6 percent by weight of colloidal silicon dioxide; and

0.5-1 percent by weight of magnesium stearate;

and further comprising a film coating containing hypromellose, titanium dioxide, triacetin, and iron oxide yellow.

8. The method of claim 7 , wherein the lactose in the tablet pharmaceutical composition is lactose anhydrous.

9. The method of claim 7 , wherein the tablet pharmaceutical composition contains 20 to 100 mg of Compound I.

10. The method of claim 7 , wherein the tablet pharmaceutical composition contains 20, 25, 50, 60, 75, 80, or 100 mg of Compound I.

11. The method of claim 7 , wherein the kidney cancer is renal cell carcinoma.

12. A method of treating kidney cancer, comprising administering to a patient in need of such treatment a tablet pharmaceutical composition comprising about:

Ingredient

(% w/w)

Compound I, L-malate salt

31.68

Microcrystalline Cellulose

38.85

Lactose anhydrous

19.42

Hydroxypropyl Cellulose

3.00

Croscarmellose Sodium

6.00

Silicon dioxide, Colloidal

0.30

Magnesium Stearate

0.75

Total

100.00

wherein Compound I is:

13. The method of claim 12 , wherein the tablet pharmaceutical composition contains 20 to 100 mg of Compound I.

14. The method of claim 12 , wherein the tablet pharmaceutical composition contains 20, 25, 50, 60, 75, 80, or 100 mg of Compound I.

15. The method of claim 12 , wherein the kidney cancer is renal cell carcinoma.

16. A method of treating kidney cancer, comprising administering to a patient in need of such treatment a tablet pharmaceutical composition comprising about:

Ingredient

(% w/w)

Compound I, L-malate salt

31.68

Microcrystalline Cellulose

38.85

Lactose anhydrous

19.42

Hydroxypropyl Cellulose

3.00

Croscarmellose Sodium

3.00

Total Intra-granular

95.95

Silicon dioxide, Colloidal

0.30

Croscarmellose Sodium

3.00

Magnesium Stearate

0.75

Total

100.00

wherein Compound I is:

17. The method of claim 16 , wherein the tablet pharmaceutical composition contains 20 to 100 mg of Compound I.

18. The method of claim 16 , wherein the tablet pharmaceutical composition contains 20, 25, 50, 60, 75, 80, or 100 mg of Compound I.

19. The method of claim 16 , wherein the kidney cancer is renal cell carcinoma.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 5, 2017
From: WILSON, JO ANN
To: EXELIXIS, INC.
Reel/Frame 043489/0881 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 5, 2017
From: WILSON, JO ANN
To: EXELIXIS, INC.
Reel/Frame 043490/0006 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 5, 2017
From: SHAH, KHALID
To: EXELIXIS, INC.
Reel/Frame 043490/0126 →
Continuity (4)
Division 13810537
Provisional Application 61370843 · Aug 5, 2010
Provisional Application 61365253 · Jul 16, 2010
Related Publication 20170143689A1 · May 25, 2017
Cited By (8)
US 12,275,706 US 12,415,784 US 12,486,233 US 12,516,025 US 12,516,026 US 12,522,567 US 12,552,749 US 12,661,350