# US 5,710,257 A · Method of causing selective immunosuppression using HL-60-related lectins

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- Number: US 5,710,257 A
- Document ID: US5710257A
- Status: Granted
- Kind: A
- Application number: 08/719,551
- Filed: 1996-09-25
- Granted: 1998-01-20
- Earliest claimed: 1988-04-14
- Inventors: Jeffrey J. Seilhamer; Glenn Nedwin; Tim Bringman; Pierre-Olivier Couraud
- Web page: https://patentgrep.com/patent/US5710257A

## CPC

- A61K 38/1709: {from mammals}
- A61K 38/168: {from plants}
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61K 47/6415: {Toxins or lectins, e.g. clostridial toxins or Pseudomonas exotoxins}
- A61K 47/646: {the entire peptide or protein drug conjugate elicits an immune response, e.g. conjugate vaccines}
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07K 14/4726: {Lectins}
- Y10S 530/827: Proteins from mammals or birds
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)
- Y10S: TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS

## Abstract

Pharmaceutical compositions useful in the treatment of autoimmune conditions include as an active ingredient a soluble lectin having a molecular weight of about 14 kilodaltons or a fragment thereof. The lectin or fragment binds .beta.-galactoside-containing moieties independent of the presence or absence of Ca.sup.+2, stimulates hemagglutination of trypsinized rabbit erythrocytes in standard lectin assays wherein the stimulation is inhibited by lactose or thiogalactoside, has an amino acid sequence containing at least one N-glycosylation site and is at least 90% homologous to the amino acid sequence shown in positions 2-135 of FIG. 1 or the relevant portions thereof. The composition is used for treatment of autoimmune conditions such as rheumatoid arthritis, myasthenia gravis, and multiple sclerosis, as well as modulating the immune response in an allergic reactions or to organ or tissue transplant rejection. The inventive composition can be combined with general immunosuppressants.

## Claims

### Claim 1

A method to prepare a pharmaceutical composition comprising a
(a) human HL-60 lectin in purified and isolated form, said lectin having an amino acid sequence consisting of positions 2-135 in FIG. 1 including a glycosylation site within positions 96-98, wherein said lectin binds beta-galactoside-containing moieties independent of the presence or absence or Ca.sup.+2, and has a molecular weight of about 14 Kd; and wherein said lectin is homogenous using the criterion of producing a single peak when subjected to C4-HPLC, is capable of binding to asialofetuin and lypsinized rabbit erythrocytes and wherein agglutination of said lectin is inhibited by thiodigalactoside and beta-lactose; and
(b) a carbohydrate; in admixture with at least one pharmaceutically acceptable excipient,
which method comprises lyophilizing said soluble lectin in an aqueous solution containing about 1-40% concentration wt./volume of a protective carbohydrate at a pH of about 4-8.

### Claim 2 (depends on 1)

The method of claim 1 wherein said carbohydrate is about 5-15%.

### Claim 3 (depends on 1)

The method of claim 1 wherein said carbohydrate is about 10%.

### Claim 4 (depends on 1)

The method of claim 1 wherein said protective carbohydrate is a disaccharide or monosaccharide.

### Claim 5 (depends on 1)

The method of claim 1 wherein said protective carbohydrate is lactose.

### Claim 6 (depends on 1)

The method of claim 1 wherein said pH is about 4.5 to 6.

### Claim 7 (depends on 1)

The method of claim 1 wherein said pH is about 5.

### Claim 8 (depends on 1)

The method of claim 1 wherein said pH is maintained in about 10 mM citrate buffer.