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Last Updated: November 19, 2019

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Claims for Patent: 10,010,507

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Summary for Patent: 10,010,507
Title:Pharmaceutical formulations of a bruton's tyrosine kinase inhibitor
Abstract: Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pi- peridin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Inventor(s): Chong; Ching W. (Fremont, CA), Kuehl; Robert (San Francisco, CA), Tan; Heow (Cupertino, CA), Atluri; Harisha (Palo Alto, CA)
Assignee: Pharmacyclics LLC (Sunnyvale, CA)
Application Number:15/909,779
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 10,010,507
Patent Claims: 1. A solid tablet formulation comprising ibrutinib and one or more pharmaceutically acceptable excipients, wherein ibrutinib is a compound with the structure of Compound 1, ##STR00007## wherein the ibrutinib is in micronized form; and wherein ibrutinib is in an amount of about 140 mg, about 280 mg, about 420 mg, or about 560 mg in the tablet.

2. The solid tablet formulation of claim 1, wherein the particle size of micronized ibrutinib is about or less than 30 microns.

3. The solid tablet formulation of claim 1, wherein the particle size of micronized ibrutinib is about or less than 10 microns.

4. The solid tablet formulation of claim 1, wherein the particle size of micronized ibrutinib is less than about 1 micron.

5. The solid tablet formulation of claim 1 further comprising one or more diluents.

6. The solid tablet formulation of claim 5, wherein the one or more diluents are selected from the group consisting of lactose, sucrose, dextrose, dextrates, maltodextrin, mannitol, xylitol, sorbitol, cyclodextrins, calcium phosphate, calcium sulfate, starches, modified starches, cellulose, microcrystalline cellulose, microcellulose, and talc.

7. The solid tablet formulation of claim 5, wherein the one or more diluents are lactose, cellulose, microcrystalline cellulose, or a combination thereof.

8. The solid tablet formulation of claim 5 further comprising one or more lubricants.

9. The solid tablet formulation of claim 8, wherein the one or more lubricants are a stearate, a polyethylene glycol (PEG), or a wax.

10. The solid tablet formulation of claim 8 further comprising one or more disintegrating agents.

11. The solid tablet formulation of claim 10, wherein the one or more disintegrating agents are selected from the group consisting of natural starch, a pregelatinized starch, a sodium starch, methylcrystalline cellulose, methylcellulose, croscarmellose, croscarmellose sodium, cross-linked sodium carboxymethylcellulose, cross-linked carboxymethylcellulose, cross-linked croscarmellose, cross-linked starch, cross-linked polymer, cross-linked polyvinylpyrrolidone, sodium alginate, a clay, and a gum.

12. The solid tablet formulation of claim 10, wherein the one or more disintegrating agents are selected from the group consisting of natural starch, a pregelatinized starch, a sodium starch, methylcrystalline cellulose, methylcellulose, croscarmellose, croscarmellose sodium, cross-linked sodium carboxymethylcellulose, cross-linked carboxymethylcellulose, cross-linked croscarmellose, sodium starch glycolate, crospovidone, cross-linked polyvinylpyrrolidone, sodium alginate, a clay, and a gum.

13. The solid tablet formulation of claim 8 further comprising one or more binders.

14. The solid tablet formulation of claim 13, wherein the one or more binders are polyvinylpyrrolidone or hydroxypropyl cellulose.

15. The solid tablet formulation of claim 1 comprising: a. at least 50% w/w of ibrutinib; b. one or more diluents; and c. one or more lubricants.

16. The solid tablet formulation of claim 1 comprising: a. about 50% w/w to about 90% w/w of ibrutinib; b. about 5% w/w to about 20% w/w of one or more diluents; and c. about 0.1% w/w to about 1.5% w/w of one or more lubricants.

17. The solid tablet formulation of claim 1, wherein the excipients comprise intragranular and extragranular excipients; and the intragranular excipients comprise one or more diluents; and the extragranular excipients comprise one or more lubricants.

18. The solid tablet formulation of claim 1, wherein the excipients comprise intragranular and extragranular excipients; and the intragranular excipients comprise lactose and microcrystalline cellulose; and the extragranular excipients comprise magnesium stearate.

19. The solid tablet formulation of claim 1, wherein the excipients comprise lactose in an amount from about 5% w/w to about 20% w/w, about 10% w/w to about 20% w/w, about 8% w/w to about 15% w/w, about 8.5% w/w to about 14% w/w, or about 12% w/w to about 15% w/w.

20. The solid tablet formulation of claim 1, wherein the excipients comprise microcrystalline cellulose in an amount from about 5% w/w to about 20% w/w, about 8% w/w to about 20% w/w, about 8% w/w to about 15% w/w, about 1% w/w to about 10% w/w, or about 2% w/w to about 5% w/w.

21. The solid tablet formulation of claim 1, wherein the excipients comprise magnesium stearate in an amount from about 0.1% w/w to about 1.5% w/w, about 0.4% w/w to about 0.8% w/w, or about 0.5% w/w to about 0.6% w/w.

22. The solid tablet formulation of claim 1, wherein the excipients comprise intragranular and extragranular excipients; and the intragranular excipients comprise lactose, microcrystalline cellulose, croscarmellose sodium, and hydroxypropyl cellulose; and the extragranular excipients comprise croscarmellose sodium and magnesium stearate.

23. The solid tablet formulation of claim 1, wherein the excipients comprise croscarmellose sodium in an amount from about 0 to about 10% w/w, about 0 to about 5% w/w, about 1% w/w to about 10% w/w, about 2% w/w to about 5% w/w, about 2% w/w to about 4% w/w, about 3% w/w to about 7% w/w, or about 1% w/w to about 3% w/w.

24. The solid tablet formulation of claim 1, wherein the excipients comprise hydroxypropyl cellulose in an amount from about 0 to about 2% w/w, about 0.1% w/w to about 1.1% w/w, or about 0.1% w/w to about 1% w/w.

25. The solid tablet formulation of claim 1, wherein the excipients comprise intragranular and extragranular excipients; and the intragranular excipients comprise lactose, polyvinylpyrrolidone, and croscarmellose sodium; and the extragranular excipients comprise croscarmellose sodium, microcrystalline cellulose, and magnesium stearate.

26. The solid tablet formulation of claim 1, wherein the excipients comprise polyvinylpyrrolidone in an amount from about 0% w/w to about 5% w/w, or about 1% w/w to about 3% w/w.

27. The solid tablet formulation of claim 1, wherein the high-load solid tablet formulation is used for one tablet once a day dosing.

28. The solid tablet formulation of claim 1, wherein the formulation comprises about 60% w/w to about 80% w/w of ibrutinib.

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