Method of administrating an anticancer drug containing α, α, α-trifluorothymidine and thymidine phosphorylase inhibitor

• US 7,799,783 B2
• Filed: 01/26/2005
• Issued: 09/21/2010
• Est. Priority Date: 01/26/2005
• Status: Expired

• Current Assignee: Taiho Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
• Original Assignee: Taiho Pharmaceutical Company Limited (Otsuka Holdings Company Limited)
• Inventors: Emura, Tomohiro, Mita, Akira
• Primary Examiner(s): Anderson; James D
• Application Number:
  US11/042,059
• Publication Number:
  US 20060167031A1
• Time in Patent Office: 2,064 Days
• Field of Search: 514/235.8
• US Class Current: 514/235.8
• CPC Class Codes: A61K 31/513 having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

The present invention relates to a method for treating a cancer comprising orally administering a composition containing α,α,α-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/m²/day in terms of FTD in 2 to 4 divided portions per to patients in need of the treatment.

Claims

1. A method for treating at least one of a digestive cancer and a breast cancer, comprising

orally administering a composition comprising α

,α

,α

-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/m²/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.

2. The method according to 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.

7. The method according to claim 1, wherein the cancer is breast cancer.

10. The method according to claim 1, wherein the cancer is digestive cancer.

3. A method for treating at least one of a digestive cancer and a breast cancer, comprising

orally administering a composition comprising

α

,α

,α

-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/m²/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 α

,α

,α

-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 α

,α

,α

-trifluorothymidine incorporated into the target site DNA of the cancer after an equal amount of α

,α

,α

-trifluorothymidine is orally administered in a single dose after one day.

5. The method according to claim 3, wherein the composition is orally administered in 3 equally divided portions per day.

8. The method according to claim 3, wherein the cancer is breast cancer.

11. The method according to claim 3, wherein the cancer is digestive cancer.

4. A method for treating at least one of a digestive cancer and a breast cancer, comprising:

orally administering a composition comprising

α

,α

,α

-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/m²/day in terms of α

,α

,α

-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 α

,α

,α

-trifluorothymidine incorporated into the target site DNA of the cancer after three days of orally administering the α

,α

,α

-trifluorothymidine is present in an amount that is at least a factor of 1.69 greater than the amount of the α

,α

,α

-trifluorothymidine incorporated into the target site DNA when the oral administration is carried out in a single dose for three days.

6. The method according to claim 4, wherein the composition is orally administered in 3 equally divided portions per day.

9. The method according to claim 4, wherein the cancer is breast cancer.

12. The method according to claim 4, wherein the cancer is digestive cancer.