US7368456B2
Expired / Lapsed
US
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Methods, compositions, and kits for organ protection during systemic anticancer therapy
Assignee: Asymmetric Therapeutics LLC
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Filing: 2005-08-03
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Granted: 2008-05-06
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Expires: 2025-08-03
Abstract
Abstract Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.
Inventors
- 👤 John P. Ford
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 16:42
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/513; A61K31/335; A61K31/337; A61K31/555; A61K31/70; A61K31/7028; A61K31/7034; A61K31/704; A61K31/7042; A61K31/7052; A61K31/706; A61K31/7064; A61K31/7068; A61K31/7072; A61P; A61P17/00; A61P39/00; A61P43/00
Claims Analysis
Total Claims: 53
Claim 1
Independent Claim
81 words
A method of protecting a desired body tissue from toxic effects of an anticancer composition comprising 5-fluorouracil, or a prodrug thereof, the method comprising: administering nonsystemically a pharmaceutical composition comprising uracil to the tissue desired to be protected so as to establish a concentration of uracil in said tissue sufficient to protect said tissue from said toxic effects, with the circulating uracil concentration induced by administration of the pharmaceutical composition being insufficient to abrogate the clinical efficacy of said anticancer composition.
Claim 2
Independent Claim
81 words
A method of protecting a desired body tissue from toxic effects of an anticancer composition comprising 5-fluorouracil, or a prodrug thereof, the method comprising: administering nonsystemically a pharmaceutical composition comprising uracil to the tissue desired to be protected so as to establish a concentration of uracil in said tissue sufficient to protect said tissue from said toxic effects, with the circulating uracil concentration induced by administration of the pharmaceutical composition being insufficient to abrogate the clinical efficacy of said anticancer composition.
Claim 3
Dependent Claim
12 words
The method of claim 1 , wherein the anticancer composition comprises 5-fluorouracil.
Claim 4
Dependent Claim
24 words
The method of claim 1 , wherein the anticancer composition comprises a 5-fluorouracil prodrug selected from the group consisting of ftorafur, doxifluridine, and capecitabine.
Claim 5
Dependent Claim
13 words
The method of claim 1 , wherein the anticancer composition further comprises 5-chloro-2,4-dihydroxypyridine.
Claim 6
Dependent Claim
17 words
The method of claim 4 , wherein the anticancer composition further comprises ftorafur, 5-chloro-2,4-dihydroxypyridine, and oxonic acid.
Claim 7
Dependent Claim
24 words
The method of claim 1 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 0.1%.
Claim 8
Dependent Claim
24 words
The method of claim 1 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 1.0%.
Claim 9
Dependent Claim
25 words
The method of claim 1 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than about 60%.
Claim 10
Dependent Claim
24 words
The method of claim 1 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than 5%.
Claim 11
Dependent Claim
43 words
The method of claim 1 , wherein uracil is applied as a pharmaceutical composition comprising a carrier or carriers selected to generate any one of a cream, a lotion, an ointment, an aerosol spray, a roll-on liquid, a roll-on stick or a pad.
Claim 12
Independent Claim
101 words
A method of protecting a desired body tissue from hand-foot syndrome, the method comprising: systemically administering 5-fluorouracil, or a prodrug thereof; and administering nonsystemically a protectant agent to the tissue desired to be protected by administering topically to the palmar and/or plantar skin surface said protectant agent so as to establish a concentration of said protectant agent in said tissue sufficient to protect said tissue from hand-foot syndrome, with the circulating concentration of said protectant agent being insufficient to abrogate the clinical efficacy of said systemically administered 5-fluorouracil, or prodrug thereof, wherein the protectant agent is a pharmaceutical composition comprising uracil.
Claim 13
Independent Claim
101 words
A method of protecting a desired body tissue from hand-foot syndrome, the method comprising: systemically administering 5-fluorouracil, or a prodrug thereof; and administering nonsystemically a protectant agent to the tissue desired to be protected by administering topically to the palmar and/or plantar skin surface said protectant agent so as to establish a concentration of said protectant agent in said tissue sufficient to protect said tissue from hand-foot syndrome, with the circulating concentration of said protectant agent being insufficient to abrogate the clinical efficacy of said systemically administered 5-fluorouracil, or prodrug thereof, wherein the protectant agent is a pharmaceutical composition comprising uracil.
Claim 14
Dependent Claim
24 words
The method of claim 11 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 0.1%.
Claim 15
Dependent Claim
24 words
The method of claim 11 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 1.0%.
Claim 16
Dependent Claim
25 words
The method of claim 11 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than about 60%.
Claim 17
Dependent Claim
24 words
The method of claim 11 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than 5%.
Claim 18
Dependent Claim
43 words
The method of claim 11 , wherein uracil is applied as a pharmaceutical composition comprising a carrier or carriers selected to generate any one of a cream, a lotion, an ointment, an aerosol spray, a roll-on liquid, a roll-on stick or a pad.
Claim 19
Independent Claim
127 words
A method of protecting a desired body tissue from hand-foot syndrome, the method comprising: systemically administering a fluoropyrimidine selected from the group consisting of ftorafur, Carmofur, capecitabine, doxifluridine, the combination of uracil and ftorafur known as UFT, the combination of tegafur, 5-chloro-2,4-dihydropyridine and potassium oxonate known as S-1 and Emitefur; and nonsystemically administering a pharmaceutical composition comprising uracil and a pharmaceutically acceptable carrier to the tissue desired to be protected by administering topically to the palmar and/or plantar skin surface said pharmaceutical composition so as to establish a concentration of uracil in said tissue sufficient to protect said tissue from hand-foot syndrome, with the circulating concentration of uracil induced by administration of said pharmaceutical composition being insufficient to abrogate the clinical efficacy of said systemically administered fluoropyrimidine.
Claim 20
Independent Claim
127 words
A method of protecting a desired body tissue from hand-foot syndrome, the method comprising: systemically administering a fluoropyrimidine selected from the group consisting of ftorafur, Carmofur, capecitabine, doxifluridine, the combination of uracil and ftorafur known as UFT, the combination of tegafur, 5-chloro-2,4-dihydropyridine and potassium oxonate known as S-1 and Emitefur; and nonsystemically administering a pharmaceutical composition comprising uracil and a pharmaceutically acceptable carrier to the tissue desired to be protected by administering topically to the palmar and/or plantar skin surface said pharmaceutical composition so as to establish a concentration of uracil in said tissue sufficient to protect said tissue from hand-foot syndrome, with the circulating concentration of uracil induced by administration of said pharmaceutical composition being insufficient to abrogate the clinical efficacy of said systemically administered fluoropyrimidine.
Claim 21
Dependent Claim
11 words
The method of claim 17 , wherein the fluoropyrimidine is capecitabine.
Claim 22
Dependent Claim
21 words
The method of claim 18 , wherein the pharmaceutical composition comprises a carrier or carriers necessary to form a hydrophilic ointment.
Claim 23
Dependent Claim
24 words
The method of claim 17 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 0.1%.
Claim 24
Dependent Claim
24 words
The method of claim 17 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 1.0%.
Claim 25
Dependent Claim
25 words
The method of claim 17 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than about 60%.
Claim 26
Dependent Claim
24 words
The method of claim 17 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than 5%.
Claim 27
Dependent Claim
43 words
The method of claim 17 , wherein uracil is applied as a pharmaceutical composition comprising a carrier or carriers selected to generate any one of a cream, a lotion, an ointment, an aerosol spray, a roll-on liquid, a roll-on stick or a pad.
Claim 28
Independent Claim
96 words
A method of treating neoplasia, the method comprising: systemically administering 5-fluorouracil, or a precursor thereof; and concurrently administering nonsystemically a pharmaceutical composition comprising uracil to a tissue desired to be protected from toxic effects of said systemically administered 5-fluorouracil, or a precursor thereof, wherein the concentration of uracil in the tissue desired to be protected is sufficient to protect said tissue from toxic effects of said 5-fluorouracil, or precursor thereof, and the circulating concentration of uracil induced by said concurrent administering is insufficient to abrogate the clinical efficacy of said systemically administered 5-fluorouracil or precursor thereof.
Claim 29
Independent Claim
96 words
A method of treating neoplasia, the method comprising: systemically administering 5-fluorouracil, or a precursor thereof; and concurrently administering nonsystemically a pharmaceutical composition comprising uracil to a tissue desired to be protected from toxic effects of said systemically administered 5-fluorouracil, or a precursor thereof, wherein the concentration of uracil in the tissue desired to be protected is sufficient to protect said tissue from toxic effects of said 5-fluorouracil, or precursor thereof, and the circulating concentration of uracil induced by said concurrent administering is insufficient to abrogate the clinical efficacy of said systemically administered 5-fluorouracil or precursor thereof.
Claim 30
Dependent Claim
24 words
The method of claim 25 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 0.1%.
Claim 31
Dependent Claim
24 words
The method of claim 25 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 1.0%.
Claim 32
Dependent Claim
25 words
The method of claim 25 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than about 60%.
Claim 33
Dependent Claim
24 words
The method of claim 25 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than 5%.
Claim 34
Dependent Claim
43 words
The method of claim 25 , wherein uracil is applied as a pharmaceutical composition comprising a carrier or carriers selected to generate any one of a cream, a lotion, an ointment, an aerosol spray, a roll-on liquid, a roll-on stick or a pad.
Claim 35
Independent Claim
114 words
A method of treating neoplasia, the method comprising: systemically administering a fluoropyrimidine selected from the group consisting of ftorafur, Carmofur, capecitabine, doxifluridine, the combination of uracil and ftorafur known as UFT, the combination of tegafur, 5-chloro-2,4-dihydropyridine and potassium oxonate known as S-1, and Emitefur; and concurrently administering nonsystemically a pharmaceutical composition comprising uracil to a tissue desired to be protected from toxic effects of said systemically administered fluoropyrimidine, wherein the concentration of uracil in the tissue desired to be protected following said concurrent administering is sufficient to protect said tissue from toxic effects of said fluoropyrimidine, and the circulating concentration of uracil is insufficient to abrogate the clinical efficacy of said systemically administered fluoropyrimidine.
Claim 36
Independent Claim
114 words
A method of treating neoplasia, the method comprising: systemically administering a fluoropyrimidine selected from the group consisting of ftorafur, Carmofur, capecitabine, doxifluridine, the combination of uracil and ftorafur known as UFT, the combination of tegafur, 5-chloro-2,4-dihydropyridine and potassium oxonate known as S-1, and Emitefur; and concurrently administering nonsystemically a pharmaceutical composition comprising uracil to a tissue desired to be protected from toxic effects of said systemically administered fluoropyrimidine, wherein the concentration of uracil in the tissue desired to be protected following said concurrent administering is sufficient to protect said tissue from toxic effects of said fluoropyrimidine, and the circulating concentration of uracil is insufficient to abrogate the clinical efficacy of said systemically administered fluoropyrimidine.
Claim 37
Dependent Claim
11 words
The method of claim 31 , wherein said fluoropyrimidine is capecitabine.
Claim 38
Dependent Claim
24 words
The method of claim 31 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 0.1%.
Claim 39
Dependent Claim
24 words
The method of claim 31 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 1.0%.
Claim 40
Dependent Claim
25 words
The method of claim 31 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than about 60%.
Claim 41
Dependent Claim
24 words
The method of claim 31 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than 5%.
Claim 42
Dependent Claim
43 words
The method of claim 31 , wherein uracil is applied as a pharmaceutical composition comprising a carrier or carriers selected to generate any one of a cream, a lotion, an ointment, an aerosol spray, a roll-on liquid, a roll-on stick or a pad.
Claim 43
Dependent Claim
110 words
A kit for oral delivery of an anticancer therapeutic agent or precursor thereof with reduced toxicity to a desired tissue, the kit comprising: at least one dose of a fluoropyrimidine selected from the group consisting of ftorafur, Carmofur, capecitabine, doxifluridine, the combination of ftorafur and uracil known as UFT, the combination of tegafur, 5-chloro-2,4-dihydropyridine and potassium oxonate known as S-1, and Emitefur; and at least one dose of a pharmaceutical composition comprising uracil for topical administration to establish a uracil concentration sufficient to protect said tissue from toxic effects of said fluoropyrimidine, and the circulating concentration of uracil is insufficient to abrogate the clinical efficacy of said systemically administered fluoropyrimidine.
Claim 44
Dependent Claim
110 words
A kit for oral delivery of an anticancer therapeutic agent or precursor thereof with reduced toxicity to a desired tissue, the kit comprising: at least one dose of a fluoropyrimidine selected from the group consisting of ftorafur, Carmofur, capecitabine, doxifluridine, the combination of ftorafur and uracil known as UFT, the combination of tegafur, 5-chloro-2,4-dihydropyridine and potassium oxonate known as S-1, and Emitefur; and at least one dose of a pharmaceutical composition comprising uracil for topical administration to establish a uracil concentration sufficient to protect said tissue from toxic effects of said fluoropyrimidine, and the circulating concentration of uracil is insufficient to abrogate the clinical efficacy of said systemically administered fluoropyrimidine.
Claim 45
Dependent Claim
11 words
The kit of claim 38 , wherein the fluoropyrimidine is 5-fluorouracil.
Claim 46
Dependent Claim
11 words
The kit of claim 38 , wherein the fluoropyrimidine is capecitabine.
Claim 47
Dependent Claim
20 words
The kit of claim 38 , wherein the pharmaceutical composition comprising uracil is suitable for topical delivery to the skin.
Claim 48
Dependent Claim
24 words
The kit of claim 38 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 0.1%.
Claim 49
Dependent Claim
24 words
The kit of claim 38 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of at least about 1.0%.
Claim 50
Dependent Claim
25 words
The kit of claim 38 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than about 60%.
Claim 51
Dependent Claim
24 words
The kit of claim 38 , wherein uracil is present in the pharmaceutical composition at a concentration by weight of no more than 5%.
Claim 52
Dependent Claim
22 words
The kit of claim 40 , wherein the pharmaceutical composition comprising uracil is suitable for topical delivery of uracil to the skin.
Claim 53
Dependent Claim
21 words
The kit of claim 46 , wherein uracil is present in the pharmaceutical composition within a weight concentration of between 0.1-10%.
References Cited (Backward Citations)
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