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US4981690A Expired / Lapsed US ⏱️ 0.0 years remaining

Liposome-incorporated mepartricin

Assignee: The University of Texas System
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Filing: 1987-10-27
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Granted: 1991-01-01
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Expires: 2007-10-27
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Abstract

Abstract The present invention involves a liposomal agent for treating disseminated fungal infection in an animal. This liposomal agent comprises the polyene antifungal compound mepartricin. The mepatricin is encapsulated within a liposome. The liposome in which the mepartricin is incorporated is preferably a stable multilamellar vesicle. The liposome broadly comprises one or more lipids one or more of phosphomonoglyceride, phosphatidic acid and sphingolipid. The lipids are preferably one or more of phosphatidylcholine, phosphatidylserine, phosphatidylglycerol, sphingomyelin or phosphatidic acid. The lipids are most preferably one or more of dimyristoylphosphatidylchlorine, dimyristoylphosphatidylglycerol, phosphatidylcholine and phosphatidylglycerol. The liposome of the present invention may comprise a sterol most preferably cholesterol. An important aspect of the present invention involves a method for treating disseminated fungal infection in an animal. This method comprises administering to an animal subject to disseminated fungal infection a fungicidally effective amount of mepartricin encapsulated within a liposome. The liposome is composed as described above. The administering is preferably parenteral in most instances but may be oral or topical if specific colonies of fungus are thereby more directly reached. This treatment method is most useful when the animal is a human suffering from disseminated fungal infection. The method of treatment involves a fungicidally effective amount of liposome-incorporated mepartricin of between about 1 mg mepartricin/kg body weight and about 6 mg mepartricin/kg body weight.

Inventors

  • 👤 Gabriel Lopez-Berestein
  • 👤 Reeta Mehta
  • 👤 Roy L. Hopfer
  • 👤 Rudolph L. Juliano

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-02 21:19
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K9/00; A61K9/10; A61K9/127; A61P; A61P31/00; A61P31/04; Y; Y10; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 60 words
An antifungal composition comprising mepartricin, cholesterol, and phospholipid in multilamellar liposomal form, where the phospholipid and the weight ratio of phospholipid to cholesterol are selected from the group consisting of: phosphatidylcholine and cholesterol in a ratio of about 9:1; dioleoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6:3:1; and dielaidoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6.5:2.5:1.
Claim 2
Dependent Claim 60 words
An antifungal composition comprising mepartricin, cholesterol, and phospholipid in multilamellar liposomal form, where the phospholipid and the weight ratio of phospholipid to cholesterol are selected from the group consisting of: phosphatidylcholine and cholesterol in a ratio of about 9:1; dioleoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6:3:1; and dielaidoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6.5:2.5:1.
Claim 3
Dependent Claim 21 words
The composition of claim 1, where the mepartricin and the combined phospholipids and cholesterol have a weight ratio of about 1:10.
Claim 4
Dependent Claim 20 words
The composition of claim 1, where the mepartricin and phospholipids have a weight ratio between about 0.01:10 and about 0.7:10.
Claim 5
Dependent Claim 20 words
The composition of claim 1, where the mepartricin and phospholipids have a weight ratio between about 0.02:10 and about 0.08:10.
Claim 6
Independent Claim 79 words
A method of treating disseminated fungal infection in an animal, comprising administering to an animal a fungicidally effective amount of a composition comprising mepartricin, cholesterol, and phospholipid in multilamellar liposomal form, where the phospholipid and the weight ratio of phospholipid to cholesterol are selected from the group consisting of: phosphatidylcholine and cholesterol in a ratio of about 9:1; dioleoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6:3:1; and dielaidoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6.5:2.5:1.
Claim 7
Independent Claim 79 words
A method of treating disseminated fungal infection in an animal, comprising administering to an animal a fungicidally effective amount of a composition comprising mepartricin, cholesterol, and phospholipid in multilamellar liposomal form, where the phospholipid and the weight ratio of phospholipid to cholesterol are selected from the group consisting of: phosphatidylcholine and cholesterol in a ratio of about 9:1; dioleoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6:3:1; and dielaidoylphosphatidylcholine, phosphatidylethanolamine, and cholesterol in a ratio of about 6.5:2.5:1.
Claim 8
Dependent Claim 21 words
The method of claim 5, where the mepartricin and the combined phospholipids and cholesterol have a weight ratio of about 1:10.
Claim 9
Dependent Claim 20 words
The method of claim 5, where the mepartricin and phospholipids have a weight ratio between about 0.01:10 and about 0.7:10.
Claim 10
Dependent Claim 20 words
The method of claim 7, where the mepartricin and phospholipids have a weight ratio between about 0.02:10 and about 0.08:10.
Claim 11
Dependent Claim 17 words
The method of claim 5, where the administration is intravenous, intraarterial, subcutaneous, intramuscular, intralymphatic, intraperitoneal, or intrapleural.
Claim 12
Dependent Claim 11 words
The method of claim 5, where the animal is a human.
Claim 13
Dependent Claim 25 words
The method of claim 5, where the fungicidally effective amount is between about 1 mg mepartricin/kg body weight and about 20 mg mepartricin/kg body weight.
Claim 14
Dependent Claim 25 words
The method of claim 5, where the fungicidally effective amount is between about 2.5 mg mepartricin/kg body weight and about 6 mg mepartricin/kg body weight.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1993-12-31 1994-07-02 1995-01-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1997-12-31 1998-07-02 1999-01-01 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2001-12-31 2002-07-02 2003-01-01 $7700.00 Window Closed / Lapsed

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