Claims for Patent: 9,364,475

Summary for Patent: 9,364,475

Title:	Tablet formulation of a phosphatidylinositol 3-kinase inhibitor
Abstract:	The present invention is directed to compositions and methods that target the PI3K signaling pathway for the treatment or prevention of cancer. In one aspect, there is provided a pharmaceutical formulation comprising Polymorph E of N-(3-{[(2Z)-3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]s- ulfamoyl}phenyl)-2-methylalaninamide.
Inventor(s):	Parikh; Darshan (Bridgewater, NJ), Raju; Praveen (Bangalore, IN)
Assignee:	SANOFI (Paris, FR)
Application Number:	14/645,947
Patent Claims:	1. A pharmaceutical formulation comprising Polymorph E of N-(3-{[(2Z)-3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]s- ulfamoyl}phenyl)-2-methylalaninamide, a hydrogel polymer and a diluent. 2. The pharmaceutical formulation of claim 1, wherein the hydrogel is selected from the group consisting of microcrystalline cellulose, methyl cellulose, hydroxymethyl cellulose, polyvinyl pyrrolidone, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyethylene oxides, gums, acrylate polymers and methacrylate polymers. 3. The pharmaceutical formulation of claim 1, wherein the hydrogel is microcrystalline cellulose. 4. The pharmaceutical formulation of claim 1, wherein the diluent is selected from the group consisting of sugars, starches, vegetable oils, lactose monohydrate, calcium phosphate, dextrin, dextrose, maltitol, maltose, starch, sucrose and talc. 5. The pharmaceutical formulation of claim 1, wherein the diluent is a starch, and the starch is pregelatinized starch or sodium starch glycolate. 6. The pharmaceutical formulation of claim 1 comprising, by weight, 40-60% Polymorph E; 15-35% microcrystalline cellulose; 5-15% pregelatinized starch and between 0.1-10.0% each of hypromellose, silicon dioxide and sodium starch glycolate. 7. The pharmaceutical formulation of claim 1 comprising, by weight, about 50% Polymorph E; about 27% microcrystalline cellulose; about 10% pregelatinized starch, about 3% hypromellose, about 1% silicon dioxide and about 4% sodium starch glycolate. 8. The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is in tablet form. 9. The pharmaceutical formulation of claim 8, wherein the pharmaceutical formulation is in caplet form. 10. The pharmaceutical formulation of claim 8, wherein the pharmaceutical formulation is an immediate-release tablet form. 11. The pharmaceutical formulation of claim 1, wherein the formulation comprises about 50 mg, 100 mg, 150 mg, or 200 mg of Polymorph E. 12. A compressed solid dosage form comprising Polymorph E of N-(3-{[(2Z)-3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]s- ulfamoyl}phenyl)-2-methylalaninamide, a hydrogel polymer and a diluent. 13. The dosage form of claim 12, comprising, by weight, 40-60% Polymorph E; 15-35% microcrystalline cellulose; 5-15% pregelatinized starch and between 0.1-10.0% each of hypromellose, silicon dioxide and sodium starch glycolate. 14. The dosage form of claim 13 comprising, by weight, about 50% Polymorph E; about 27% microcrystalline cellulose; about 10% pregelatinized starch, about 3% hypromellose, about 1% silicon dioxide and about 4% sodium starch glycolate. 15. The dosage form of claim 12, wherein the dosage form comprises about 40 to 250 mg of Polymorph E. 16. The dosage form of claim 12, wherein the dosage form comprises about 50 mg, 100 mg, 150 mg or 200 mg of Polymorph E. 17. The dosage form of claim 12, wherein the dosage form is a tablet. 18. The dosage form of claim 17, wherein the dosage form is a caplet. 19. A compressed solid dosage form comprising: A) an active agent containing Polymorph E of N-(3-{[(2Z)-3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]s- ulfamoyl}phenyl)-2-methylalaninamide, and B) at least one pharmaceutically acceptable additive, wherein the active agent is present in an amount of more than about 40% by weight based upon the total weight of the compressed solid dosage form. 20. The dosage form of claim 19, comprising, by weight, 40-60% Polymorph E; 15-35% microcrystalline cellulose; 5-15% pregelatinized starch and between 0.1-10.0% each of hypromellose, silicon dioxide and sodium starch glycolate. 21. The dosage form of claim 20 comprising, by weight, about 50% Polymorph E; about 27% microcrystalline cellulose; about 10% pregelatinized starch, about 3% hypromellose, about 1% silicon dioxide and about 4% sodium starch glycolate. 22. The dosage form of claim 19, wherein the active agent comprises at least 95% Polymorph E. 23. The dosage form of claim 22, wherein the active agent comprises at least 97% Polymorph E. 24. The dosage form of claim 23, wherein the active agent comprises at least 99% Polymorph E. 25. A method of treating cancer in a subject, comprising administering to the subject the pharmaceutical formulation of claim 1. 26. A method of treating cancer in a subject, comprising administering to the subject the dosage form of claim 1. 27. The method of claim 25, wherein the cancer is a solid tumor or lymphoma. 28. The method of claim 27, wherein the lymphoma is a relapsed or refractory lymphoma. 29. The method of claim 27, wherein the lymphoma is chronic lymphocytic lymphoma (CLL) or small lymphocytic lymphoma (SLL). 30. The method of claim 25, wherein the cancer is breast cancer, colon cancer, rectal cancer, endometrial cancer, gastric carcinoma, glioblastoma, hepatocellular carcinoma, small cell lung cancer, non-small cell lung cancer, melanoma, ovarian cancer, cervical cancer, pancreatic cancer, prostate carcinoma, acute myelogenous leukemia (AML), chronic myelogenous leukemia (CML), or thyroid carcinoma. 31. The method of claim 25, wherein the treatment comprises the administration of an additional anticancer agent. 32. The method of claim 31, wherein the anticancer agent is carboplatin, paclitaxel, erlotinib, or trastuzumab.

Details for Patent 9,364,475

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2033-07-22
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2033-07-22
Genentech, Inc.	HERCEPTIN HYLECTA	trastuzumab and hyaluronidase-oysk	Injection	761106	02/28/2019		2033-07-22