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Claims for Patent: 8,889,159

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Claims for Patent: 8,889,159

Title:Compositions and methods for treating hepatitis C virus
Abstract: Disclosed herein are a composition and unit dosage form for the treatment of hepatitis C virus (HCV) infection comprising GS-7977 and at least one pharmaceutically acceptable excipient, as well as methods for making said composition and unit dosage form. Also disclosed herein is a method of treating a subject, preferably a human, infected with hepatitis C virus, said method comprising administering to the subject for a time period an effective amount of GS-7977 and an effective amount of ribavirin. In one aspect, the method comprises administering to the subject an interferon-free treatment regimen comprising an effective amount of GS-7977 and an effective amount of ribavirin. In a particular aspect, the method is sufficient to produce an undetectable amount of HCV RNA in the subject for at least 12 weeks after the end of the time period.
Inventor(s): Cleary; Darryl G. (Chapel Hill, NC), Reynolds; Charles J. (Greenville, NC), Berrey; Miriam Michelle (Durham, NC), Hindes; Robert G. (Skillman, NJ), Symonds; William T. (San Francisco, CA), Ray; Adrian S. (Redwood City, CA), Mo; Hongmei (Palo Alto, CA), Hebner; Christy M. (Belmont, CA), Oliyai; Reza (Burlingame, CA), Zia; Vahid (San Carlos, CA), Stefanidis; Dimitrios (Mountain View, CA), Pakdaman; Rowchanak (San Carlos, CA), Casteel; Melissa Jean (Burlingame, CA)
Assignee: Gilead Pharmasset LLC (Foster City, CA)
Application Number:13/686,664
Patent Claims: 1. A pharmaceutical composition comprising: a) about 25% to about 35% w/w of crystalline GS-7977 having the structure ##STR00002## and b) at least one pharmaceutically acceptable excipient, wherein the crystalline GS-7977 has XRPD 2.theta.-reflections (.degree.) at about: 6.1 and 12.7.

2. The composition according to claim 1, wherein the crystalline GS-7977 has XRPD 2.theta.-reflections (.degree.) at about: 6.1, 8.2, 10.4, 12.7, 17.2, 17.7, 18.0, 18.8, 19.4, 19.8, 20.1, 20.8, 21.8, and 23.3.

3. The composition according to claim 1, wherein the at least one pharmaceutically acceptable excipient comprises at least one of a diluent, a disintegrant, a glidant, and a lubricant.

4. The composition according to claim 3, wherein the at least one pharmaceutically acceptable excipient comprises a diluent selected from the group consisting of dicalcium phosphate, cellulose, compressible sugars, dibasic calcium phosphate dehydrate, lactose, mannitol, microcrystalline cellulose, starch, tribasic calcium phosphate, and combinations thereof.

5. The composition according to claim 4, wherein the diluent is selected from the group consisting of mannitol, microcrystalline cellulose, and combinations thereof.

6. The composition according to claim 3, wherein the at least one pharmaceutically acceptable excipient comprises a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, microcrystalline cellulose, modified corn starch, povidone, pregelatinized starch, sodium starch glycolate, and combinations thereof.

7. The composition according to claim 6, wherein the disintegrant is croscarmellose sodium.

8. The composition according to claim 3, wherein the at least one pharmaceutically acceptable excipient comprises a glidant selected from the group consisting of colloidal silicon dioxide, talc, starch, starch derivatives, and combinations thereof.

9. The composition according to claim 8, wherein the glidant is colloidal silicon dioxide.

10. The composition according to claim 3, wherein the at least one pharmaceutically acceptable excipient comprises a lubricant selected from the group consisting of calcium stearate, magnesium stearate, polyethylene glycol, sodium stearyl fumarate, stearic acid, talc, and combinations thereof.

11. The composition according to claim 10, wherein the lubricant is magnesium stearate.

12. The composition according to claim 1 further comprising a coating agent.

13. The composition according to claim 1, wherein the at least one pharmaceutically acceptable excipient comprises: a) about 55% w/w to about 65% w/w of a diluent; b) about 2.5% w/w to about 7.5% w/w of a disintegrant; c) about 0.25% w/w to about 0.75% w/w of a glidant; and d) about 1.25% w/w to about 1.75% w/w of a lubricant.

14. The composition according to claim 1, wherein the at least one pharmaceutically acceptable excipient comprises: a) about 30% w/w of mannitol and about 30% w/w of microcrystalline cellulose; b) about 5% w/w of croscarmellose sodium; c) about 0.5% w/w of colloidal silicon dioxide; and d) about 1.5% w/w of magnesium stearate.

15. The composition according to claim 1, wherein the composition comprises: a) about 33% w/w of crystalline GS-7977; b) about 30% w/w of mannitol and about 30% w/w of microcrystalline cellulose; c) about 5% w/w of croscarmellose sodium; d) about 0.5% w/w of colloidal silicon dioxide; and e) about 1.5% w/w of magnesium stearate.

16. A unit dosage form comprising: a) about 400 mg of crystalline GS-7977 having the structure ##STR00003## and b) at least one pharmaceutically acceptable excipient, wherein the crystalline GS-7977 has XRPD 2.theta.-reflections (.degree.) at about 6.1 and 12.7.

17. The unit dosage form according to claim 16, wherein the crystalline GS-7977 has XRPD 2.theta.-reflections (.degree.) at about: 6.1, 8.2, 10.4, 12.7, 17.2, 17.7, 18.0, 18.8, 19.4, 19.8, 20.1, 20.8, 21.8, and 23.3.

18. The unit dosage form according to claim 17, wherein the at least one pharmaceutically acceptable excipient comprises at least one of a diluent, a disintegrant, a glidant, and a lubricant.

19. The unit dosage form according to claim 18, wherein the at least one pharmaceutically acceptable excipient comprises a diluent selected from the group consisting of dicalcium phosphate, cellulose, compressible sugars, dibasic calcium phosphate dehydrate, lactose, mannitol, microcrystalline cellulose, starch, tribasic calcium phosphate, and combinations thereof.

20. The unit dosage form according to claim 19, wherein the diluent is selected from the group consisting of mannitol, microcrystalline cellulose, and combinations thereof.

21. The unit dosage form according to claim 18, wherein the at least one pharmaceutically acceptable excipient comprises a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, microcrystalline cellulose, modified corn starch, povidone, pregelatinized starch, sodium starch glycolate, and combinations thereof.

22. The unit dosage form according to claim 21, wherein the disintegrant is croscarmellose sodium.

23. The unit dosage form according to claim 18, wherein the at least one pharmaceutically acceptable excipient comprises a glidant selected from the group consisting of colloidal silicon dioxide, talc, starch, starch derivatives, and combinations thereof.

24. The unit dosage form according to claim 23, wherein the glidant is colloidal silicon dioxide.

25. The unit dosage form according to claim 18, wherein the at least one pharmaceutically acceptable excipient comprises a lubricant selected from the group consisting of calcium stearate, magnesium stearate, polyethylene glycol, sodium stearyl fumarate, stearic acid, talc, and combinations thereof.

26. The unit dosage form according to claim 25, wherein the lubricant is magnesium stearate.

27. The unit dosage form according to claim 17 further comprising a coating agent.

28. The unit dosage form according to claim 17, wherein the at least one pharmaceutically acceptable excipient comprises: a) about 660 mg to about 780 mg of a diluent; b) about 30 mg to about 90 mg of a disintegrant; c) about 3 mg to about 9 mg of a glidant; and d) about 15 mg to about 21 mg of a lubricant.

29. The unit dosage form according to claim 17, wherein the unit dosage form comprises: a) about 400 mg of crystalline GS-7977; b) about 360 mg of mannitol and about 356 mg of microcrystalline cellulose; c) about 60 mg of croscarmellose sodium; d) about 6 mg of colloidal silicon dioxide; and e) about 18 mg of magnesium stearate.

30. The unit dosage form according to claim 17, wherein the unit dosage form comprises a capsule or a tablet.

31. A process for preparing a tablet composition comprising the unit dosage form of claim 28 comprising: blending an intragranular composition and an extragranular composition to obtain a blended composition; compressing the blended composition to obtain the tablet composition; and optionally coating the tablet composition; wherein the intragranular composition comprises GS-7977, a first intragranular diluent, optionally a second intragranular diluent, an intragranular disintegrant, an intragranular glidant, and an intragranular lubricant; and the extragranular composition comprises a first extragranular diluent, optionally a second extragranular diluent, an extragranular glidant, an extragranular disintegrant, and an extragranular lubricant.

32. A tablet composition comprising about 400 mg of GS-7977 made according to the process of claim 31.

33. A method of treating a human infected with hepatitis C virus comprising administering to the human the composition according to claim 1.

34. The method according to claim 33, wherein the composition is administered to the human in combination with ribavirin.

35. A method of treating a human infected with hepatitis C virus comprising administering to the human the unit dosage form according to claim 17.

36. The method according to claim 35, wherein the unit dosage form is administered to the human in combination with ribavirin.

37. The method according to claim 36, wherein the unit dosage form is administered to the human in combination with ribavirin as part of an interferon-free treatment regimen.
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