Claims for Patent: 10,213,386

Summary for Patent: 10,213,386

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:	15/970,721
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,213,386
Patent Claims:	1. A solid tablet formulation comprising a. ibrutinib, and b. one or more pharmaceutically acceptable excipients, wherein the ibrutinib is present in an amount of at least about 50% w/w, and wherein oral administration of one or more tablet(s) of the solid tablet formulation in an amount sufficient to deliver 560 mg of ibrutinib to a population of healthy human adults in a fasted state results in a mean AUC.sub.0-.infin. of about 465 ng*h/ml+/-248 ng*h/ml. 2. The solid tablet formulation of claim 1, wherein the ibrutinib is present in an amount of at least about 60% w/w. 3. The solid tablet formulation of claim 1, comprising 420 mg of ibrutinib. 4. The solid tablet formulation of claim 1, further comprising a surfactant. 5. The solid tablet formulation of claim 1, wherein the ibrutinib is present in micronized form. 6. The solid tablet formulation of claim 5, further comprising a surfactant. 7. The solid tablet formulation of claim 5, wherein the particle size of micronized ibrutinib is about or less than 30 micron. 8. The solid tablet of claim 7, further comprising a surfactant. 9. A solid tablet formulation comprising a. 560 mg of ibrutinib, and b. one or more pharmaceutically acceptable excipients, wherein the ibrutinib is present in an amount of at least about 50% w/w, and wherein oral administration of the solid tablet formulation to a population of healthy human adults in a fasted state results in a mean AUC.sub.0-.infin. of about 465 ng*h/ml+/-248 ng*h/ml. 10. The solid tablet formulation of claim 9, wherein the ibrutinib is present in an amount of at least about 60% w/w. 11. The solid tablet formulation of claim 9, further comprising a surfactant. 12. The solid tablet formulation of claim 9, wherein the ibrutinib is present in micronized form. 13. The solid tablet formulation of claim 12, further comprising a surfactant. 14. The solid tablet formulation of claim 12, wherein the particle size of micronized ibrutinib is about or less than 30 micron. 15. The solid tablet formulation of claim 14, further comprising a surfactant. 16. The solid tablet formulation of claim 12, wherein the particle size of micronized ibrutinib is about or less than 10 micron. 17. A solid tablet formulation comprising a. 560 mg of micronized ibrutinib having a particle size of about or less than 10 micron, b. a surfactant, and c. one or more additional pharmaceutically acceptable excipients, wherein the ibrutinib is present in an amount of at least about 50% w/w, and wherein oral administration of the solid tablet formulation to a population of healthy human adults in a fasted state results in a mean AUC.sub.0-.infin. of about 465 ng*h/ml+/-248 ng*h/ml. 18. The solid tablet formulation of claim 1, comprising 140 mg of ibrutinib. 19. The solid tablet formulation of claim 1, comprising 280 mg of ibrutinib. 20. The solid tablet formulation of claim 1, comprising 560 mg of ibrutinib. 21. The solid tablet formulation of claim 1, wherein the solid tablet formulation has pharmaceutically acceptable stability. 22. The solid tablet formulation of claim 9, wherein the solid tablet formulation has pharmaceutically acceptable stability. 23. The solid tablet formulation of claim 17, wherein the solid tablet formulation has pharmaceutically acceptable stability.