# US 6,297,215 B1 · Antimicrobial cationic peptides

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- Number: US 6,297,215 B1
- Document ID: US6297215B1
- Status: Granted
- Kind: B1
- Application number: 09/307,200
- Filed: 1999-05-07
- Granted: 2001-10-02
- Earliest claimed: 1995-06-02
- Assignees: The University of British Columbia
- Inventors: Robert E. W. Hancock; Nedra Karunaratne
- Web page: https://patentgrep.com/patent/US6297215B1

## CPC

- A61K 38/16: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof {(enzyme inhibitors A61K38/005)}
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K 14/001: {by chemical synthesis}
- C07K 14/43563: {from insects}
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- 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)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

A novel class of cationic peptides having antimicrobial activity is provided. Examples of such peptides include NH2-KWKSFIKKLTTAVKKVLTTGLPALIS-COOH (SEQ ID NO:1) and NH2-KWKSFIKKLTSAAKKVVTTAKPLISS-COOH (SEQ ID NO:2). Also provided are methods for inhibiting the growth of bacteria utilizing the peptides of the invention. The peptides are particularly useful for inhibiting endotoxemia in a subject.

## Claims

### Claim 1

A method of treating an endotoxemia or sepsis associated disorder in a subject having or at risk of having such a disorder, comprising administering to the subject a therapeutically effective amount of a peptide having an amino acid sequence selected from the group consisting of:
NH2-KWKSFIKKLTTAVKKVLTTGLPALIS-COOH (SEQ ID NO:1),
NH2-KWKSFIKKLTSAAKKVVTTAKPLISS-COOH (SEQ ID NO:2),
NH2-KWKSFIKNLTKGGSKILTTGLPALIS-COOH (SEQ ID NO:3),
NH2-KWKKFIKNLTKGGSKILTTGLPALIS-COOH (SEQ ID NO:4),
NH2-KWKSFIKNLEKVLKPGGLLSNIVTSL-COOH (SEQ ID NO:5),
NH2-KWKSFIKNLEKVLKKGPILANLVSIV-COOH (SEQ ID NO:6),
NH2-KWKEFIKKLTTAVKKVLTTGLPALIS-COOH (SEQ ID NO:7),
NH2-KWKKFIKELQKVLAPGGLLSNIVTSL-COOH (SEQ ID NO:8),
NH2-KWKSFIKKLTSVLKKVVTTALPALIS-COOH (SEQ ID NO:9),
NH2-KWKSFIKNLTKVLKKVVTTALPALIS-COOH (SEQ ID NO:10),
NH2-KWKLFKKKGTGAVLTVLTTGLPALIS-COOH (SEQ ID NO:11),
NH2-KWKSFIKKLTSVLKKVVTTAKPLISS-COOH (SEQ ID NO:12),
NH2-KKKSFIKLLTSAKVSVLTTAKPLISS-COOH (SEQ ID NO:13),
NH2-KWKKFIKELQKVLKPGGLLSNIVTSL-COOH (SEQ ID NO:14),
NH2-KKWWRRVLSGLKTGPALSNV-COOH (SEQ ID NO:15),
NH2-KKWWRRVLKGLSSGPALSNV-COOH (SEQ ID NO:16),
NH2-KKWWRRALQALKNGPALSNV-COOH (SEQ ID NO:17),
NH2-KKWWRRVLSGLKTAGPAIQSVLNK-COOH (SEQ ID NO:18),
NH2-KKWWRRALQGLKTAGPAIQSVLNK-COOH (SEQ ID NO:19),
NH2-KKWWKAQKAVNSGPNALQTLAQ-COOH (SEQ ID NO:20)
NH2-KKWWKAKKFANSGPNALQTLAQ-COOH (SEQ ID NO:21), and
NH2-KKWWKFIKKAVNSGTTGLQTLAS-COOH (SEQ ID NO:22).

### Claim 2 (depends on 1)

The method of claim 1, wherein the disorder is septic shock.

### Claim 3 (depends on 1)

The method of claim 1, further comprising administering an antibiotic.

### Claim 4 (depends on 3)

The method of claim 3, wherein the class of antibiotic is selected from the group consisting of aminoglycosides, penicillins, cephalosporins, carbapenems, m-onobactams, quinolones, tetracyclines, glycopeptides, chloramphenicol, clindamycin, trimethoprim, sulfamethoxazole, nitrofurantoin, rifampin and mupirocin.

### Claim 5 (depends on 4)

The method of claim 4, wherein the antibiotic is selected from the group consisting of amikacin, gentamicin, kanamycin, netilmicin, tobramycin, streptomycin, azithromycin, clarithromycin, erythromycin, erythromycin estolate/ethylsuccinate/gluceptate/lactobionate/stearate, penicillin G, penicillin V, methicillin, nafcillin, oxacillin, cloxacillin, dicloxacillin, ampicillin, amoxicillin, ticarcillin, carbenicillin, mezlocillin, azlocillin, piperacillin, cephalothin, cefazolin, cefaclor, c-efamandole, cefoxitin, cefuroxime, cefonicid, cefmetazole, cefotetan, cefprozil, loracarbef, cefetamet, cefoperazone, cefotaxime, ceftizoxime, ceftriaxone, ceftazidime, cefepime, cefixime, cefpodoxime, cefsulodin, imipenem, aztreonam, fleroxacin, nalidixic acid, norfloxacin, ciprofloxacin, ofloxacin, enoxacin, lomefloxacin, cinoxacin, doxycycline, minocycline, tetracycline, vancomycin, and teicoplanin.