Claims for Patent: 12,303,493

Summary for Patent: 12,303,493

Title:	Anticancer compositions
Abstract:	The present invention concerns pharmaceutical formulations of ARN-509, which can be administered to a mammal, in particular a human, suffering from an androgen receptor (AR)-related disease or condition, in particular cancer, more in particular prostate cancer, including but not limited to castration-resistant prostate cancer, metastatic castration resistant prostate cancer, chemotherapy-naive metastatic castration resistant prostate cancer, biochemically relapsed hormone sensitive prostate cancer, or high-risk, non-metastatic castration-resistant prostate cancer. In one aspect, these formulations comprise a solid dispersion of ARN-509 and HPMCAS. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by melt-extruding a mixture comprising ARN-509 and HPMCAS and optionally subsequently milling said melt-extruded mixture. In one aspect, the solid dispersion of ARN-509 and HPMCAS is obtainable, in particular is obtained, by spray drying a mixture comprising ARN-509 and HPMCAS in a suitable solvent.
Inventor(s):	Dennis Martin Hester, Jason Michael Vaughn
Assignee:	Aragon Pharmaceuticals Inc
Application Number:	US18/660,698
Patent Claims:	1. A solid dispersion comprising (ARN-509) and hydroxypropyl methylcellulose acetate succinate (HPMCAS). 2. The solid dispersion according to claim 1 wherein the dispersion consists of ARN-509 and HPMCAS. 3. The solid dispersion according to claim 1 wherein ARN-509 and HPMCAS are present in the solid dispersion in a weight-by-weight ratio of ARN-509: HPMCAS in a range of from 1:1 to 1:5. 4. The solid dispersion according to claim 3 wherein the weight-by-weight ratio of ARN-509: HPMCAS in the solid dispersion is 1:3. 5. The solid dispersion according to claim 3 wherein the weight-by-weight ratio of ARN-509: HPMCAS in the solid dispersion is 1:2. 6. The solid dispersion according to claim 3 wherein the weight-by-weight ratio of ARN-509: HPMCAS in the solid dispersion is 1:1. 7. The solid dispersion according to claim 1 wherein ARN-509 is present in an amorphous form. 8. The solid dispersion according to claim 1 wherein the dispersion is a solid solution. 9. The solid dispersion according to claim 1 wherein the HPMCAS is HPMCAS LG. 10. The solid dispersion according to claim 1 obtainable by spray drying. 11. The solid dispersion according to claim 1 obtainable by hot melt extrusion. 12. The solid dispersion according to claim 1 wherein the HPMCAS is HPMCAS LG or HPMCAS LF and the weight-by-weight ratio of ARN-509: HPMCAS LG or HPMCAS LF in the solid dispersion is 1:2 or 1:3. 13. A particle consisting of the solid dispersion as defined in claim 1. 14. The particle according to claim 13 wherein the HPMCAS is HPMCAS LG or HPMCAS LF and the weight-by-weight ratio of ARN-509: HPMCAS LG or HPMCAS LF in the solid dispersion is 1:2 or 1:3. 15. A particle comprising the solid dispersion as defined in claim 2. 16. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and the solid dispersion according to claim 1. 17. The pharmaceutical formulation according to claim 16 wherein the HPMCAS is HPMCAS LG or HPMCAS LF and the weight-by-weight ratio of ARN-509: HPMCAS LG or HPMCAS LF in the solid dispersion is 1:2 or 1:3. 18. The pharmaceutical formulation according to claim 16 wherein the formulation comprises 60 mg of ARN-509. 19. The pharmaceutical formulation according to claim 16 wherein the formulation comprises 120 mg of ARN-509. 20. The pharmaceutical formulation according to claim 16 wherein the formulation comprises 240 mg of ARN-509. 21. The pharmaceutical formulation according to claim 16 wherein the solid dispersion is present in a weight range of from 20 to 40% of the total weight of the formulation. 22. The pharmaceutical formulation according to claim 16 wherein the formulation is a tablet. 23. The pharmaceutical formulation according to claim 22 wherein the tablet is suitable for oral administration. 24. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a plurality of particles according to claim 13. 25. The pharmaceutical formulation according to claim 24 wherein the HPMCAS is HPMCAS LG or HPMCAS LF and the weight-by-weight ratio of ARN-509: HPMCAS LG or HPMCAS LF in the solid dispersion is 1:2 or 1:3. 26. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and the solid dispersion according to claim 4. 27. The pharmaceutical formulation according to claim 26 wherein the formulation comprises 60 mg of ARN-509. 28. A process for preparing the solid dispersion according to claim 10 comprising mixing ARN-509 and HPMCAS in a suitable solvent and spray drying said mixture. 29. The process according to claim 28 wherein the suitable solvent is a mixture of dichloromethane and methanol. 30. The process according to claim 29 wherein dichloromethane and methanol are present in the mixture in a weight-by-weight ratio of 4:6.