US4863739A
Expired / Lapsed
US
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Liposome compositions of anthracycline derivatives
Assignee: The University of Texas System
•
Filing: 1987-05-19
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Granted: 1989-09-05
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Expires: 2007-05-19
Abstract
Abstract Disclosed are liposomal antitumor compositions having improved pharmacological characteristics. Liposomes described herein are formed through the incorporation of a particular class of anthracyclines, the 4-demethoxy-3'-desamino-2'-iodo analogs, shown to have extremely high incorporatio efficiencies of greater than 95%. These liposomes demonstrate an improved antitumor efficacy, with much reduced toxicity, against accepted tumor models, and further exhibit excellent stability upon storage, for example, in the form of a dried powder.
Inventors
- 👤 Roman Perez-Soler
- 👤 Waldemar Priebe
- 👤 Gabriel Lopez-Berestein
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 12:25
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/185; A61K31/19; A61K31/20; A61K31/203; A61K9/00; A61K9/10; A61K9/127; A61P; A61P35/00; Y; Y10; Y10S; Y10S436/00; Y10S436/829; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
12 words
A composition comprising liposomal vesicles having incorporated therein a 4-demethoxy-3'-desamino-2'-iodo anthracycline analog.
Claim 2
Dependent Claim
12 words
A composition comprising liposomal vesicles having incorporated therein a 4-demethoxy-3'-desamino-2'-iodo anthracycline analog.
Claim 3
Dependent Claim
58 words
The composition of claim 1 wherein the anthracycline analog is selected from compounds of the formula: ##STR3## wherein R 1 is hydroxy; one of X and X' is hydrogen and the other is iodine; one of Y and Y' is hydrogen and the other is hydroxy; one of Z and Z' is hydrogen and the other is hydroxy.
Claim 4
Dependent Claim
10 words
The composition of claim 2 wherein said compound is 4-demethoxy-7-O-(2-iodo-2,6-dideoxy-alpha-L-mannohexopyranosyl)adriamycinone.
Claim 5
Dependent Claim
17 words
The composition of claim 1 wherein said liposomal vesicles are dispersed in a pharmaceutically acceptable aqueous diluent.
Claim 6
Dependent Claim
20 words
The composition of claim 1 comprising a ratio of incorporated anthracycline to lipid of between about 1:5 to about 1:50.
Claim 7
Dependent Claim
15 words
The composition of claim 5 wherein the incorporated anthracycline to lipid ratio is about 1:15.
Claim 8
Dependent Claim
19 words
The composition of claim 1 wherein the liposomal vesicles include one or more of phosphomonoglyceride, phosphatidic acid and sphingolipid.
Claim 9
Dependent Claim
22 words
The composition agent of claim 1 wherein the liposomal vesicles include one or more of phosphatidylcholine, phosphatidylserine, phosphatidylglycerol, sphingomyelin and phosphatidic acid.
Claim 10
Dependent Claim
19 words
The composition of claim 1 wherein the liposomal vesicles include one or more of dimyristoylphosphatidylcholine, dimyristoylphosphatidylglycerol, phosphatidylcholine and phosphatidylglycerol.
Claim 11
Dependent Claim
15 words
The composition of claim 1 wherein the liposomal vesicles consist essentially of dimyristoylphosphatidylcholine and dimyristoylphosphatidylglycerol.
Claim 12
Dependent Claim
33 words
The composition of claim 10 wherein the liposomal vesicles are defined further as consisting essentially of dimyristoylphosphatidycholine and dimyristoylphosphatidylglycerol in a ratio of between about 1 to 10 and about 10 to 1.
Claim 13
Dependent Claim
21 words
The composition of claim 1 wherein the liposomal vesicles consist essentially of dimyristoylphosphatidylcholine and dimyristoylphosphatidylglycerol in a ratio of about 7:3.
Claim 14
Dependent Claim
17 words
The composition of claim 1 wherein the liposomal vesicles are defined further as being stable multilamellar vesicles.
Claim 15
Dependent Claim
16 words
The composition of claim 1 wherein the liposomal vesicles are defined further as comprising a sterol.
Claim 16
Dependent Claim
10 words
The composition of claim 14 wherein the sterol is cholesterol.
Claim 17
Dependent Claim
12 words
The composition of claim 1 in the form of a dried powder.
Claim 18
Dependent Claim
70 words
A process for preparing an improved anthracycline containing composition comprising: (a) selecting n anthracycline analog from compounds having the formula: ##STR4## wherein R 1 is hydroxy; one of X and X' is hydrogen and the other is iodine; one of Y and Y' is hydrogen and the other is hydroxy; one of Z and Z' is hydrogen and the other is hydroxy; and (b) incorporating said anthracycline analog with lipids.
Claim 19
Dependent Claim
70 words
A process for preparing an improved anthracycline containing composition comprising: (a) selecting n anthracycline analog from compounds having the formula: ##STR4## wherein R 1 is hydroxy; one of X and X' is hydrogen and the other is iodine; one of Y and Y' is hydrogen and the other is hydroxy; one of Z and Z' is hydrogen and the other is hydroxy; and (b) incorporating said anthracycline analog with lipids.
Claim 20
Dependent Claim
11 words
The method of claim 17 wherein step (b) comprises forming liposomes.
Claim 21
Dependent Claim
16 words
The method of claim 17 further comprising drying the anthracycline and lipids to form a powder.
Claim 22
Dependent Claim
15 words
The method of claim 18 further comprising drying the anthracycline-incorporated liposomes to form a powder.
Claim 23
Dependent Claim
18 words
The method of claim 19 or 20 further comprising hydrating the dried powder with a pharmaceutically acceptable diluent.
Claim 24
Independent Claim
28 words
A method of treating cancer in a patient comprising administering to the patient an effective dose of a composition according to any one of claims 1 through 16.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-09-04 | 1993-03-06 | 1993-09-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-09-04 | 1997-03-06 | 1997-09-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-09-04 | 2001-03-06 | 2001-09-05 | $7700.00 | Window Closed / Lapsed |