Methods for increasing blood plasma 2′-deoxyuridine (dUrd) and thymidylate synthase inhibition
First Claim
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1. A method of increasing plasma concentration of 2′
- -deoxyuridine (dUrd) in a human subject comprising;
a. a step of administering 500 mg/m2 5-fluorouracil (5-FU) intravenously as a bolus injection to said human subject;
b. following (a), a step of administering 30, 60, 120, or 240 mg/m2 [6R]-5, 10-methylene tetrahydrofolate (6R-MTHF) intravenously as one or more bolus injections to said human subject; and
c. optionally administering a therapeutically effective amount of at least one anticancer agent selected from the group consisting of oxaliplatin, irinotecan, and bevacizumab;
wherein said administration produces an increased plasma concentration of dUrd relative to dUrd plasma concentration in a human subject following administration of an equimolar dose of 5-formyl tetrahydrofolate (LV).
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Abstract
The present invention provides methods for increasing plasma dUrd levels comprising the administration of 6R-MTHF. The methods of increasing plasma dUrd increase dUrd levels compared to equimolar concentrations of LV. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF.
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Citations
16 Claims
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1. A method of increasing plasma concentration of 2′
- -deoxyuridine (dUrd) in a human subject comprising;
a. a step of administering 500 mg/m2 5-fluorouracil (5-FU) intravenously as a bolus injection to said human subject; b. following (a), a step of administering 30, 60, 120, or 240 mg/m2 [6R]-5, 10-methylene tetrahydrofolate (6R-MTHF) intravenously as one or more bolus injections to said human subject; and c. optionally administering a therapeutically effective amount of at least one anticancer agent selected from the group consisting of oxaliplatin, irinotecan, and bevacizumab; wherein said administration produces an increased plasma concentration of dUrd relative to dUrd plasma concentration in a human subject following administration of an equimolar dose of 5-formyl tetrahydrofolate (LV). - View Dependent Claims (2, 3, 7, 8, 9, 10, 15)
- -deoxyuridine (dUrd) in a human subject comprising;
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4. A method of inhibiting thymidylate synthase (TS) in a human subject comprising:
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a. a step of administering 500 mg/m2 5-FU intravenously as a bolus injection to said human subject; b. following (a), a step of administering 30, 60, 120, or 240 mg/m2 6R-MTHF intravenously as one or more bolus injections to said human subject; and c. optionally administering a therapeutically effective amount of at least one anticancer agent selected from the group consisting of oxaliplatin, irinotecan, and bevacizumab; wherein said administration produces an increased inhibition of TS relative to TS inhibition in a human subject following administration of an equimolar dose of LV. - View Dependent Claims (5, 6, 11, 12, 13, 14, 16)
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Specification