Claims for Patent: 11,576,865

Summary for Patent: 11,576,865

Title:	Sustained-release dosage forms of ruxolitinib
Abstract:	The present invention relates to sustained-release formulations and dosage forms of ruxolitinib, or a pharmaceutically acceptable salt thereof, which are useful in the treatment of Janus kinase-associated diseases such as myeloproliferative disorders.
Inventor(s):	Yong Ni, Bhavnish Parikh, Krishnaswamy Yeleswaram, Susan Erickson-Viitanen, William V. Williams
Assignee:	Incyte Holdings Comoration , Incyte Corp , Incyte Holdings Corp
Application Number:	US17/847,760
Patent Claims:	1. An oral sustained-release dosage form comprising: ruxolitinib phosphate, and a sustained-release matrix former, which is a cellulosic ether; wherein the ruxolitinib phosphate is present in the dosage form in an amount of 10 to 60 mg on a free base basis; wherein the dosage form is suitable for oral administration; wherein administration of the dosage form to a human results in a ratio of mean peak plasma concentration (Cmax) to mean 12-hour plasma concentration (C12h) of ruxolitinib of 10 or less, and wherein administration of the dosage form to a human results in a mean half-life (t1/2) of from 3.5 hours to 11 hours. 2. The oral sustained-release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 10 mg on a free base basis. 3. The oral sustained-release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 20 mg on a free base basis. 4. The oral sustained-release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 30 mg on a free base basis. 5. The oral sustained-release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 40 mg on a free base basis. 6. The oral sustained-release dosage form of claim 1, wherein the ruxolitinib phosphate is present in the dosage form in an amount of 50 mg on a free base basis. 7. The oral sustained-release dosage form of claim 1, wherein administration of the dosage form to a human results in a ratio of mean peak plasma concentration (Cmax) to mean 12-hour plasma concentration (C12h) of ruxolitinib of 1 to 10. 8. The oral sustained-release dosage form of claim 1, wherein administration of the sustained-release dosage form to a human results in a ratio of mean peak plasma concentration (Cmax) to mean 12-hour plasma concentration (C12h) of ruxolitinib of 2 to 7. 9. The oral sustained-release dosage form of claim 1, wherein administration of the dosage form to a human results in a mean half-life (t1/2) of from 4 hours to 8 hours. 10. The oral sustained-release dosage form of claim 1, wherein the dosage form is a tablet. 11. The oral sustained-release dosage form of claim 1, wherein the dosage form is a capsule. 12. The oral sustained-release dosage form of claim 1, wherein administration of the dosage form to a human results in a mean time to peak plasma concentration (tmax) of ruxolitinib of 1.5 hours to 5 hours. 13. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 1 once per day. 14. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 2 once per day. 15. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 3 once per day. 16. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 4 once per day. 17. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 5 once per day. 18. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 6 once per day. 19. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 7 once per day. 20. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 8 once per day. 21. The method of claim 13, wherein the disease is myelofibrosis. 22. The method of claim 21, wherein the myelofibrosis is primary myelofibrosis (PMF), post_polycythemia vera myelofibrosis (PV-MF), or post-essential thrombocythemia myelofibrosis (post ET-MF). 23. The method of claim 13, wherein the disease is polycythemia vera. 24. The method of claim 13, wherein the disease is graft versus host disease. 25. An oral sustained-release dosage form comprising: ruxolitinib phosphate, and a sustained-release matrix former, which is hydroxypropyl methylcellulose; wherein the ruxolitinib phosphate is present in the dosage form in an amount of 10 to 60 mg on a free base basis; wherein the dosage form is suitable for oral administration; wherein administration of the dosage form to a human results in a ratio of mean peak plasma concentration (Cmax) to mean 12-hour plasma concentration (C12h) of ruxolitinib of 10 or less, and wherein administration of the dosage form to a human results in a mean half-life (t1/2) of from 3.5 hours to 11 hours. 26. A method of treating a disease selected from myelofibrosis, polycythemia vera, and graft versus host disease in a human patient in need thereof, comprising administering to the patient the oral sustained-release dosage form of claim 25 once per day. 27. The method of claim 26, wherein the disease is myelofibrosis. 28. The method of claim 27, wherein the myelofibrosis is primary myelofibrosis (PMF), post polycythemia vera myelofibrosis (PV-MF), or post-essential thrombocythemia myelofibrosis (post ET-MF). 29. The method of claim 26, wherein the disease is polycythemia vera. 30. The method of claim 26, wherein the disease is graft versus host disease.