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Last Updated: November 30, 2020

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Claims for Patent: 10,039,779

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Summary for Patent: 10,039,779
Title:Combination formulation of two antiviral compounds
Abstract: Disclosed are pharmaceutical compositions having an effective amount of substantially amorphous ledipasvir and an effective amount of substantially crystalline sofosbuvir.
Inventor(s): Chal; Ben (Millbrae, CA), Mogalian; Erik (San Francisco, CA), Oliyai; Reza (Burlingame, CA), Pakdaman; Rowchanak (San Carlos, CA), Stefanidis; Dimitrios (Mountain View, CA), Zia; Vahid (San Carlos, CA)
Assignee: Gilead Pharmasset LLC (Foster City, CA)
Application Number:15/393,847
Patent Claims: 1. A fixed dose combination tablet comprising: a) from about 10% to about 25% w/w of a solid dispersion comprising ledipasvir dispersed within a polymer matrix formed by copovidone, wherein the weight ratio of ledipasvir to copovidone in the solid dispersion is about 1:1 and greater than 70% of the ledipasvir is amorphous; b) from about 35% to about 45% w/w of sofosbuvir wherein greater than 70% of the sofosbuvir is crystalline and the crystalline sofosbuvir has XRPD 2.theta.-reflections (.degree. .+-.0.2.theta.) at about: 6.1, 12.7, 20.1 and 20.8; c) from about 5.0% to about 25% w/w of lactose monohydrate; d) from about 5.0% to about 25% w/w of microcrystalline cellulose; e) from about 1.0% to about 10% w/w of croscarmellose sodium; f) from about 0.5% to about 3% w/w of colloidal silicon dioxide; and g) from about 0.1% to about 3% w/w of magnesium stearate.

2. The fixed dose combination tablet of claim 1, which comprises a) about 40% w/w of sofosbuvir and b) about 18% w/w of the solid dispersion comprising ledipasvir.

3. The fixed dose combination tablet of claim 1, which comprises about 90 mg of ledipasvir and about 400 mg of sofosbuvir.

4. The fixed dose combination tablet of claim 3, which comprises: (c) about 165 mg of lactose monohydrate; (d) about 180 mg of microcrystalline cellulose; (e) about 50 mg of croscarmellose sodium; (f) about 10 mg of colloidal silicon dioxide; and (g) about 15 mg of magnesium stearate.

5. The fixed dose combination tablet of claim 3 comprising a film coating.

6. A method of treating a patient infected with hepatitis C virus comprising administering to the patient a therapeutically effective amount of a fixed dose combination tablet of claim 1.

7. The method of claim 6, wherein the fixed dose combination tablet is administered for about 24 weeks or less.

8. The method of claim 6, wherein the fixed dose combination tablet is administered for about 12 weeks or less.

9. The method of claim 6, wherein the fixed dose combination tablet is administered for about 8 weeks or less.

10. The method of claim 6, wherein the fixed dose combination tablet is administered for about 6 weeks or less.

11. The method of claim 6, wherein the fixed dose combination tablet is administered once daily for about 12 weeks or less and wherein the hepatitis C virus is genotype 1, 2, 3, 4, 5, or 6.

12. The method of claim 11, wherein the hepatitis C virus is genotype 1a or 1b.

13. The method of claim 6, wherein the fixed dose combination tablet is administered once daily for about 8 weeks or less and wherein the hepatitis C virus is genotype 1, 2, 3, 4, 5, or 6.

14. The method of claim 6, wherein the fixed dose combination tablet is administered once daily for about 6 weeks or less and wherein the hepatitis C virus is genotype 1, 2, 3, 4, 5, or 6.

15. A fixed dose combination tablet comprising: a) about 18% w/w of a solid dispersion comprising ledipasvir dispersed within a polymer matrix formed by copovidone, wherein the weight ratio of ledipasvir to copovidone in the solid dispersion is about 1:1 and wherein greater than 70% of the ledipasvir is amorphous; b) about 40% w/w of sofosbuvir, wherein greater than 70% of the sofosbuvir is crystalline, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections (.degree. .+-.0.2.theta.) at about: 6.1, 12.7, 20.1 and 20.8; c) about 16.5% w/w of lactose monohydrate; d) about 18.0% w/w of microcrystalline cellulose; e) about 5.0% w/w of croscarmellose sodium; f) about 1.0% w/w of colloidal silicon dioxide; and g) about 1.5% w/w of magnesium stearate.

16. A fixed dose combination tablet comprising: a) about 180 mg of a solid dispersion comprising ledipasvir dispersed within a polymer matrix formed by copovidone, wherein the weight ratio of ledipasvir to copovidone in the solid dispersion is about 1:1 and wherein greater than 70% of the ledipasvir is amorphous; b) about 400 mg of sofosbuvir, greater than 70% of the wherein sofosbuvir is crystalline, wherein the crystalline sofosbuvir has XRPD 2.theta.-reflections (.degree. .+-.0.2.theta.) at about: 6.1, 12.7, 20.1 and 20.8; c) about 165 mg of lactose monohydrate; d) about 180 mg of microcrystalline cellulose; e) about 50 mg of croscarmellose sodium; f) about 10 mg of colloidal silicon dioxide; and g) about 15 mg of magnesium stearate.

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Serving leading biopharmaceutical companies globally:

Express Scripts
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McKinsey

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