Claims for Patent: RE46284

Summary for Patent: RE46284

Title:	Method of administrating an anticancer drug containing .alpha., .alpha., .alpha.-trifluorothymidine and thymidine phosphorylase inhibitor
Abstract:	The present invention relates to a method for treating a cancer comprising orally administering a composition containing .alpha.,.alpha.,.alpha.-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 20 to 80 mg/m.sup.2/day in terms of FTD in 2 to 4 divided portions per to patients in need of the treatment.
Inventor(s):	Emura; Tomohiro (Hanno, JP), Mita; Akira (Tokyo, JP)
Assignee:	TAIHO PHARMACEUTICAL CO., LTD. (Tokyo, JP)
Application Number:	14/985,148
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent RE46284
Patent Claims:	1. A method for treating at least one of a digestive cancer and a breast cancer, comprising orally administering a composition comprising .alpha.,.alpha.,.alpha.-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 50 to 70 mg/m.sup.2/day in terms of FTD in 2 .[.or 3.]. divided portions per day to a human patient in need of treatment of at least one of a digestive cancer and a breast cancer, wherein the administration of a daily dose of said composition is in 2 .[.or 3.]. portions per day for 5 days followed by 2 days off treatment in the week on a one-week dosing schedule .Iadd.wherein m.sup.2 is the human patient's body surface area.Iaddend.. 2. The method .[.according to.]. .Iadd.of .Iaddend.claim 1, further comprising two cycles of administration of a daily dose of said composition in 2 .[.or 3.]. portions per day for 5 days followed by 2 days off treatment in the week, and subsequent 2 weeks off treatment on a dosing schedule. .[.3. A method for treating at least one of a digestive cancer and a breast cancer, comprising orally administering a composition comprising .alpha.,.alpha.,.alpha.-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 50 to 70 mg/m.sup.2/day in terms of FTD in 2 or 3 divided portions per day to a human patient in need of treatment of at least one of a digestive cancer and a breast cancer, wherein the .alpha.,.alpha.,.alpha.-trifluorothymidine incorporated into the target site DNA of the cancer one day after the oral administration is present in an amount that is at least a factor of 1.72 greater than the amount of .alpha.,.alpha.,.alpha.-trifluorothymidine incorporated into the target site DNA of the cancer after an equal amount of .alpha.,.alpha.,.alpha.-trifluorothymidine is orally administered in a single dose after one day..]. .[.4. A method for treating at least one of a digestive cancer and a breast cancer, comprising: orally administering a composition comprising .alpha.,.alpha.,.alpha.-trifluorothymidine and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 50 to 70 mg/m.sup.2/day in terms of .alpha.,.alpha.,.alpha.-trifluorothymidine in 2 or 3 divided portions per day to a human patient in need of treatment of at least one of a digestive cancer and a breast cancer, wherein the .alpha.,.alpha.,.alpha.-trifluorothymidine incorporated into the target site DNA of the cancer after three days of orally administering the .alpha.,.alpha.,.alpha.-trifluorothymidine is present in an amount that is at least a factor of 1.69 greater than the amount of the .alpha.,.alpha.,.alpha.-trifluorothymidine incorporated into the target site DNA when the oral administration is carried out in a single dose for three days..]. .[.5. The method according to claim 3, wherein the composition is orally administered in 3 equally divided portions per day..]. .[.6. The method according to claim 4, wherein the composition is orally administered in 3 equally divided portions per day..]. 7. The method .[.according to.]. .Iadd.of .Iaddend.claim 1, wherein the .[.cancer.]. .Iadd.method .Iaddend.is .Iadd.for treating .Iaddend.breast cancer. .[.8. The method according to claim 3, wherein the cancer is breast cancer..]. .[.9. The method according to claim 4, wherein the cancer is breast cancer..]. 10. The method .[.according to.]. .Iadd.of .Iaddend.claim 1, wherein the .[.cancer.]. .Iadd.method .Iaddend.is .Iadd.for treating .Iaddend.digestive cancer .Iadd.which is selected from the group consisting of esophageal, gastric, liver, gallbladder-bile duct, pancreatic, and colorectal cancers.Iaddend.. .[.11. The method according to claim 3, wherein the cancer is digestive cancer..]. .[.12. The method according to claim 4, wherein the cancer is digestive cancer..]. .Iadd.13. The method of claim 10, wherein the digestive cancer is colorectal cancer. .Iaddend. .Iadd.14. The method of claim 10, wherein the digestive cancer is gastric cancer. .Iaddend. .Iadd.15. The method of claim 10, wherein the digestive cancer is pancreatic cancer. .Iaddend. .Iadd.16. The method of claim 10, wherein the digestive cancer is esophageal cancer. .Iaddend. .Iadd.17. The method of claim 10, wherein the digestive cancer is liver cancer. .Iaddend. .Iadd.18. A method for treating colorectal cancer in a human patient, comprising orally administering a composition comprising .alpha.,.alpha.,.alpha.-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 70 mg/m.sup.2/day in terms of FTD in 2 divided portions per day at a dosing interval of 6 hours or more wherein the administration of said dose is for 5 days followed by 2 days off treatment in a one-week dosing schedule wherein m.sup.2 is the human patient's body surface area. .Iaddend. .Iadd.19. A method for treating colorectal cancer in a human patient, comprising orally administering a composition comprising .alpha.,.alpha.,.alpha.-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 70 mg/m.sup.2/day in terms of FTD in 2 divided portions per day at a dosing interval of 6 hours or more comprising two cycles of daily administration of said composition for 5 days followed by 2 days off treatment in a week, and subsequent 2 weeks off treatment dosing schedule wherein m.sup.2 is the human patient's body surface area. .Iaddend. .Iadd.20. The method of claim 19, wherein the patient's body surface area is calculated by a formula selected from the group consisting of: i.) body surface area (m.sup.2)=([Height(cm).times.Weight(kg)]/3600).sup.1/2 ii.) body surface area (m.sup.2)=0.20247.times.Height(m).sup.0.725.times.Weight(kg).sup.0.425 iii.) body surface area (m.sup.2)=0.007184.times.Height(cm).sup.0.725.times.Weight(kg).sup.0.425 iv.) body surface area (m.sup.2)=0.024265.times.Height(cm).sup.0.3964.times.Weight(kg).sup.0.537- 8 v.) body surface area (m.sup.2)=0.0235.times.Height(cm).sup.0.42246.times.Weight(kg).sup.0.5145- 6 vi.) body surface area(m.sup.2)=0.0003207.times.Height(cm).sup.0.3.times.Weight(gram).sup.(- 0.7285-(0.0188.times.LOG(gram)). .Iaddend. .Iadd.21. The method of claim 19, wherein the patient's body surface area is calculated by the formula body surface area (m.sup.2)=([Height(cm).times.Weight(kg)]/3600).sup.1/2. .Iaddend. .Iadd.22. The method of claim 19, wherein the patient's body surface area is calculated by the formula body surface area (m.sup.2)=0.20247.times.Height(m).sup.0.725.times.Weight(kg).sup.0.425. .Iaddend. .Iadd.23. The method of claim 7, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.24. The method of claim 7, wherein the dose is 50 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.25. The method of claim 1, wherein the two divided portions are administered at a dosage interval of six hours or more. .Iaddend. .Iadd.26. The method of claim 23, wherein the two divided portions are administered at a dosage interval of six hours or more. .Iaddend. .Iadd.27. The method of claim 24 wherein the two divided portions are administered at a dosage interval of six hours or more. .Iaddend. .Iadd.28. A method for treating at least one of a digestive cancer and a breast cancer in a human patient, comprising orally administering a composition comprising .alpha.,.alpha.,.alpha.-trifluorothymidine (FTD) and 5-chloro-6-(1-(2-iminopyrrolidinyl)methyl)uracil hydrochloride in a molar ratio of 1:0.5 at a dose of 70 mg/m.sup.2/day in terms of FTD in 2 divided portions per day at a dosing interval of 6 hours or more comprising two cycles of daily administration of said composition for 5 days followed by 2 days off treatment in a week, and subsequent 2 weeks off treatment dosing schedule wherein m.sup.2 is the human patient's body surface area. .Iaddend. .Iadd.29. The method of claim 13, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.30. The method of claim 14, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.31. The method of claim 15, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.32. The method of claim 16, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.33. The method of claim 17, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.34. The method of claim 13, wherein the 2 divided portions are administered at a dosage interval of 6 hours or more. .Iaddend. .Iadd.35. The method of claim 14, wherein the 2 divided portions are administered at a dosage interval of 6 hours or more. .Iaddend. .Iadd.36. The method of claim 15, wherein the 2 divided portions are administered at a dosage interval of 6 hours or more. .Iaddend. .Iadd.37. The method of claim 16, wherein the 2 divided portions are administered at a dosage interval of 6 hours or more. .Iaddend. .Iadd.38. The method of claim 17, wherein the 2 divided portions are administered at a dosage interval of 6 hours or more. .Iaddend. .Iadd.39. The method of claim 35, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.40. The method of claim 36, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.41. The method of claim 37, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend. .Iadd.42. The method of claim 38, wherein the dose is 70 mg/m.sup.2/day of FTD. .Iaddend.