# US 8,540,977 B2 · IL-11 muteins

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- Number: US 8,540,977 B2
- Document ID: US8540977B2
- Status: Granted
- Kind: B2
- Application number: 13/189,850
- Filed: 2011-07-25
- Published: 2011-12-08
- Granted: 2013-09-24
- Earliest claimed: 2007-10-26
- Assignees: CSL Limited
- Applicants: Manuel Baca
- Inventors: Manuel Baca
- Web page: https://patentgrep.com/patent/US8540977B2

## CPC

- C07K 14/5431: {IL-11}
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 7/04: Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
- A61P 15/08: for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
- A61P 15/16: Masculine contraceptives
- A61P 15/18: Feminine contraceptives
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 35/04: specific for metastasis
- 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)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

The present invention relates generally to the treatment of an interleukin-11 (IL-11)-mediated condition. More particularly, the present invention provides the use of modified forms of IL-11 which modulate IL-11 signaling in the treatment of IL-11-mediated conditions.

## Claims

### Claim 1

A human IL-11 mutein comprising:
i. an amino acid sequence that has at least 95% identity to amino acids 10 to 175 of SEQ ID NO:11; and
ii. the amino acid sequence PAIDY (SEQ ID NO:24) at the amino acid positions of said mutein that correspond to positions 58 to 62 of SEQ ID NO:11.

### Claim 2 (depends on 1)

The human IL-11 mutein of claim 1 wherein the mutein comprises at least one amino acid substitution, addition or deletion, relative to the amino acid sequence of SEQ ID NO:11, outside of positions 58 to 62 of SEQ ID NO:11.

### Claim 3 (depends on 1)

The human IL-11 mutein of claim 1 further comprising an amino acid substitution of the cysteine (C) at amino acid position 147 of SEQ ID NO:11 to alanine (A) or tryptophan (W).

### Claim 4 (depends on 1)

The human IL-11 mutein of claim 1 which IL-11 mutein is PEGylated.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising the IL-11 mutein of claim 1 and further comprising one or more pharmaceutically acceptable carriers, diluents and/or excipients.

### Claim 6

A human IL-11 mutein comprising:
i. an amino acid sequence that has at least 95% identity to amino acids 10 to 178 of SEQ ID NO:11; and
ii. the amino acid sequence PAIDY (SEQ ID NO:24) at the amino acid positions of said mutein that correspond to positions 58 to 62 of SEQ ID NO:11.

### Claim 7 (depends on 2)

The human IL-11 mutein of claim 2 wherein the at least one amino acid substitution, addition or deletion inhibits or reduces binding of the mutein to gp130.

### Claim 8 (depends on 6)

The human IL-11 mutein of claim 6 wherein the mutein comprises at least one amino acid substitution, addition or deletion, relative to the amino acid sequence of SEQ ID NO:11, outside of positions 58 to 62 of SEQ ID NO:11.

### Claim 9 (depends on 8)

The human IL-11 mutein of claim 8 wherein the at least one amino acid substitution, addition or deletion inhibits or reduces binding of the mutein to gp130.

### Claim 10 (depends on 6)

The human IL-11 mutein of claim 6 further comprising an amino acid substitution of the cysteine (C) at amino acid position 147 of SEQ ID NO:11 to alanine (A) or tryptophan (W).

### Claim 11 (depends on 6)

The human IL-11 mutein of claim 6 which IL-11 mutein is PEGylated.

### Claim 12 (depends on 6)

A pharmaceutical composition comprising the IL-11 mutein of claim 6 and further comprising one or more pharmaceutically acceptable carriers, diluents and/or excipients.
