# US 5,753,260 A · Vaccines against sterols

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- Number: US 5,753,260 A
- Document ID: US5753260A
- Status: Granted
- Kind: A
- Application number: 08/422,633
- Filed: 1995-04-14
- Granted: 1998-05-19
- Earliest claimed: 1986-06-17
- Assignees: EntreMed, Inc.
- Inventors: Carl R. Alving; Julie Kenner; Glenn M. Swartz, Jr.; John W. Madsen
- Web page: https://patentgrep.com/patent/US5753260A

## CPC

- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 31/66: Phosphorus compounds
- A61K 39/0002: {Fungal antigens, e.g. Trichophyton, Aspergillus, Candida}
- A61K 39/0012: {Lipids; Lipoproteins}
- A61K 39/02: Bacterial antigens
- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- C07K 14/445: Plasmodium
- C07K 16/1203: Gram-negative bacteria
- C07K 16/18: against material from animals or humans
- C07K 16/44: against material not provided for elsewhere {, e.g. haptens, metals, DNA, RNA, amino acids}
- G01N 33/92: involving lipids, e.g. cholesterol {, lipoproteins, or their receptors (steroid hormones G01N33/743)}
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- A61K 39/00: Medicinal preparations containing antigens or antibodies (materials for immunoassay G01N33/53)
- A61K 2039/55505: {Inorganic adjuvants}
- A61K 2039/5555: {Muramyl dipeptides}
- A61K 2039/55555: {Liposomes; Vesicles, e.g. nanoparticles; Spheres, e.g. nanospheres; Polymers}
- A61K 2039/55572: {Lipopolysaccharides; Lipid A; Monophosphoryl lipid A}
- G01N 2800/044: Hyperlipemia or hypolipemia, e.g. dyslipidaemia, obesity
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

The present invention relates to immunoreactive compositions and methods for immunizing humans or animals against sterols, such as cholesterol and its derivatives, and their use in methods for reducing the serum cholesterol levels of the immunized individuals and to retard or reduce the severity of atherosclerosis or atherosclerosis plaques caused by ingestion of dietary cholesterol. Another embodiment of the present invention encompasses ergosterol or ergosterol derivative compositions useful for the treatment or prevention of fungal infection, and methods of use thereof. Yet another aspect of the invention is dairy products containing anti-ergosterol antibodies produced by dairy animals immunized against ergosterol according to the present invention and methods of making thereof. A further aspect of the invention is a diagnostic assay for determining whether a human or animal has a fungal infection.

## Claims

### Claim 1

A vaccine comprising a liposome comprising between about 55.5 mol % and 71 mol % cholesterol, and either phosphatidyl choline or dimyristoyl phosphatidyl choline, for immunizing or hyperimmunizing a mammal against cholesterol.

### Claim 2 (depends on 1)

The vaccine of claim 1, wherein the liposome contains phosphatidyl choline.

### Claim 3 (depends on 1)

The vaccine of claim 1, wherein the liposome contains dimyristoyl phosphatidyl choline.

### Claim 4 (depends on 1)

The vaccine of claim 1, further comprising an adjuvant.

### Claim 5 (depends on 4)

The vaccine of claim 4, wherein the adjuvant is selected from the group consisting of lipophilic muramyl dipeptide derivatives, nonionic block polymers, aluminum hydroxide, aluminum phosphate, and lipid A.

### Claim 6 (depends on 5)

The vaccine of claim 5, wherein the adjuvant is lipid A.

### Claim 7

A therapeutic method for vaccinating a mammal against cholesterol to treat or prevent hypercholesterolemia or atherosclerosis comprising, administering to the mammal an amount effective to immunize the mammal against cholesterol of a vaccine comprising a liposome comprising between about 43 mol % and 71 mol % cholesterol, and either phosphatidyl choline or dimyristoyl phosphatidyl choline.

### Claim 8 (depends on 7)

The method of claim 7, wherein the liposome contains phosphatidyl choline.

### Claim 9 (depends on 7)

The method of claim 7, wherein the liposome contains dimyristoyl phosphatidyl choline.

### Claim 10 (depends on 7)

The method of claim 7, wherein the vaccine further comprises an adjuvant.

### Claim 11 (depends on 10)

The method of claim 10, wherein the adjuvant is selected from the group consisting of lipophilic muramyl dipeptide derivatives, nonionic block polymers, aluminum hydroxide, aluminum phosphate, and lipid A.

### Claim 12 (depends on 11)

The method of claim 11, wherein the adjuvant is lipid A.

### Claim 13 (depends on 1)

The vaccine of claim 1, wherein the mammal is a human.

### Claim 14 (depends on 1)

The vaccine of claim 1, wherein the liposome comprises greater than 60 mol % cholesterol.

### Claim 15 (depends on 1)

The vaccine of claim 1, wherein the liposome comprises approximately 71 mol % cholesterol.

### Claim 16 (depends on 7)

The method of claim 7, wherein the mammal is a human.

### Claim 17 (depends on 7)

The method of claim 7, wherein the liposome comprises greater than 50 mol % cholesterol.

### Claim 18 (depends on 7)

The method of claim 7, wherein the liposome comprises greater than 60 mol % cholesterol.

### Claim 19 (depends on 7)

The method of claim 7, wherein the liposome comprises approximately 71 mol % cholesterol.