US6995165B2
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: 2004-08-13
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Granted: 2006-02-07
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Expires: 2024-08-13
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 12:55
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: 40
Claim 1
Independent Claim
121 words
A kit for the administration of at least one dose of an orally administrable fluoropyrimidine prodrug or precursor with reduced cutaneous toxicity, the kit comprising: at least one dose of an orally administrable fluoropyrimidine prodrug or precursor; and at least one dose of a topical composition comprising uracil and a pharmaceutically acceptable carrier or excipient, wherein each dose of topical composition contains uracil in an amount that is both (i) sufficient, at the site of topical application, to reduce the development of cutaneous side-effects, and (ii) insufficient to produce a circulating uracil concentration capable of causing clinically observable diminution in potency or efficacy of the kit's fluoropyrimidine prodrug or precursor, or metabolite thereof, at a neoplastic tissue desired to be treated.
Claim 2
Dependent Claim
121 words
A kit for the administration of at least one dose of an orally administrable fluoropyrimidine prodrug or precursor with reduced cutaneous toxicity, the kit comprising: at least one dose of an orally administrable fluoropyrimidine prodrug or precursor; and at least one dose of a topical composition comprising uracil and a pharmaceutically acceptable carrier or excipient, wherein each dose of topical composition contains uracil in an amount that is both (i) sufficient, at the site of topical application, to reduce the development of cutaneous side-effects, and (ii) insufficient to produce a circulating uracil concentration capable of causing clinically observable diminution in potency or efficacy of the kit's fluoropyrimidine prodrug or precursor, or metabolite thereof, at a neoplastic tissue desired to be treated.
Claim 3
Dependent Claim
18 words
The kit of claim 1 , comprising a plurality of doses of orally administrable fluoropyrimidine prodrug or precursor.
Claim 4
Dependent Claim
15 words
The kit of claim 2 , comprising a plurality of doses of topical uracil composition.
Claim 5
Dependent Claim
41 words
The kit of claim 3 , wherein the number of doses of topical uracil composition is sufficient to reduce cutaneous toxicity for the duration of concurrent systemic therapy with the doses of orally administered fluoropyrimidine prodrug or precursor in the kit.
Claim 6
Dependent Claim
32 words
The kit of claim 4 , wherein the kit comprises sufficient doses of orally administrable fluoropyrimidine prodrug or precursor and topical uracil composition for at least a 14 day course of treatment.
Claim 7
Dependent Claim
32 words
The kit of claim 5 , wherein the kit comprises sufficient doses of orally administrable fluoropyrimidine prodrug or precursor and topical uracil composition for at least a 21 day course of treatment.
Claim 8
Dependent Claim
23 words
The kit of claim 1 , wherein uracil is present within said topical composition at a concentration of at least about 0.1% (w/w).
Claim 9
Dependent Claim
23 words
The kit of claim 7 , wherein uracil is present within said topical composition at a concentration of at least about 0.5% (w/w).
Claim 10
Dependent Claim
23 words
The kit of claim 8 , wherein uracil is present within said topical composition at a concentration of at least about 1.0% (w/w).
Claim 11
Dependent Claim
23 words
The kit of claim 9 , wherein uracil is present within said topical composition at a concentration of at least about 2.5% (w/w).
Claim 12
Dependent Claim
23 words
The kit of claim 10 , wherein uracil is present within said topical composition at a concentration of at least about 5.0% (w/w).
Claim 13
Dependent Claim
23 words
The kit of claim 11 , wherein uracil is present within said topical composition at a concentration of at least about 10% (w/w).
Claim 14
Dependent Claim
23 words
The kit of claim 12 , wherein uracil is present within said topical composition at a concentration of at least about 20% (w/w).
Claim 15
Dependent Claim
23 words
The kit of claim 13 , wherein uracil is present within said topical composition at a concentration of at least about 30% (w/w).
Claim 16
Dependent Claim
24 words
The kit of claim 1 , wherein uracil is present within said topical composition at a concentration of no more than about 60% (w/w).
Claim 17
Dependent Claim
24 words
The kit of claim 15 , wherein uracil is present within said topical composition at a concentration of no more than about 50% (w/w).
Claim 18
Dependent Claim
24 words
The kit of claim 16 , wherein uracil is present within said topical composition at a concentration of no more than about 40% (w/w).
Claim 19
Dependent Claim
24 words
The kit of claim 17 , wherein uracil is present within said topical composition at a concentration of no more than about 10% (w/w).
Claim 20
Dependent Claim
24 words
The kit of claim 18 , wherein uracil is present within said topical composition at a concentration of no more than about 5% (w/w).
Claim 21
Dependent Claim
20 words
The kit of claim 1 , wherein uracil is present within said composition at a concentration of about 1% (w/w).
Claim 22
Dependent Claim
17 words
The kit of claim 1 , wherein said topical uracil composition is anhydrous, aqueous, or an emulsion.
Claim 23
Dependent Claim
12 words
The kit of claim 21 , wherein said composition is an emulsion.
Claim 24
Dependent Claim
36 words
The kit of claim 1 , wherein said carrier or excipient comprises at least one agent selected from the group consisting of emollients, water, inorganic powders, foaming agents, emulsifiers, fatty alcohols, fatty acids, and combinations thereof.
Claim 25
Dependent Claim
16 words
The kit of claim 23 , wherein said carrier or excipient comprises at least one emollient.
Claim 26
Dependent Claim
23 words
The kit of claim 24 , wherein said at least one emollient is selected from the group consisting of polyols, esters, and hydrocarbons.
Claim 27
Dependent Claim
41 words
The kit of claim 25 , wherein said polyol is selected from the group consisting of propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3-butylene glycol, 1,2,6-hexanetriol, glycerin, ethoxylated glycerin, propoxylated glycerin, xylitol, and mixtures thereof.
Claim 28
Dependent Claim
27 words
The kit of claim 25 , wherein said ester is selected from the group consisting of alkyl esters of fatty acids having 10 to 20 carbon atoms.
Claim 29
Dependent Claim
49 words
The kit of claim 25 , wherein said ester is selected from the group consisting of hexyl laurate, isohexyl laurate, isohexyl palmitate, isopropyl palmitate, decyl oleate, isodecyl oleate, hexadecyl stearate, decyl stearate, isopropyl isostearate, diisopropyl adipate, diisohexyl adipate, dihexyldecyl adipate, diisopropyl sebacate, lauryl lactate, myristyl lactate and cetyl lactate.
Claim 30
Dependent Claim
15 words
The kit of claim 25 , wherein said ester is a C12–C15 alcohol benzoate ester.
Claim 31
Dependent Claim
17 words
The kit of claim 25 , wherein said ester is oleyl myristate, oleyl stearate or oleyl oleate.
Claim 32
Dependent Claim
19 words
The kit of claim 25 , wherein said ester is a fatty acid ester of an ethoxylated fatty alcohol.
Claim 33
Dependent Claim
14 words
The kit of claim 25 , wherein said ester is a polyhydric alcohol ester.
Claim 34
Dependent Claim
65 words
The kit of claim 32 , wherein said ester is selected from the group consisting of ethylene glycol mono- and di-fatty acid esters, diethylene glycol mono- and di-fatty acid esters, polyethylene glycol (200–6000) mono- and di-fatty acid esters, polyglycerol poly-fatty esters, ethoxylated glyceryl monostearate, 1,3-butylene glycol monostearate, 1,3-butylene glycol distearate, polyoxyethylene polyol fatty acid ester, sorbitan fatty acid esters, and polyoxyethylene sorbitan fatty acid esters.
Claim 35
Dependent Claim
13 words
The kit of claim 25 , wherein said ester is a wax ester.
Claim 36
Dependent Claim
24 words
The kit of claim 34 , wherein said wax ester is selected from the group consisting of beeswax, spermaceti, myristyl myristate and stearyl stearate.
Claim 37
Dependent Claim
13 words
The kit of claim 25 , wherein said ester is a sterol ester.
Claim 38
Dependent Claim
15 words
The kit of claim 23 , wherein said carrier or excipient comprises an inorganic powder.
Claim 39
Dependent Claim
34 words
The kit of claim 37 , wherein said inorganic powder is selected from the group consisting of clays, talc, mica, silica, alumina, zeolites, sodium sulfate, sodium bicarbonate, sodium carbonate, calcium sulfate and mixtures thereof.
Claim 40
Dependent Claim
21 words
The kit of any one of claims 1 – 21 , 22 – 38 , wherein said fluoropyrimidine precursor is capecitabine.
References Cited (Backward Citations)
US5326764A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 2009-02-06 | 2009-08-08 | 2010-02-07 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2013-02-06 | 2013-08-08 | 2014-02-07 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2017-02-06 | 2017-08-08 | 2018-02-07 | $7700.00 | Window Closed / Lapsed |