# US 9,751,947 B2 · Antibodies and derivatives thereof

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- Number: US 9,751,947 B2
- Document ID: US9751947B2
- Status: Granted
- Kind: B2
- Application number: 12/866,184
- Filed: 2009-02-04
- Published: 2011-06-16
- Granted: 2017-09-05
- Earliest claimed: 2008-02-04
- Assignees: Lay Line Genomics S.p.A.
- Applicants: Fabio Benigni; Daniele D'Ambrosio
- Inventors: Fabio Benigni; Daniele D'Ambrosio
- Web page: https://patentgrep.com/patent/US9751947B2

## CPC

- C07K 16/2863: {against receptors for growth factors, growth regulators}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/08: for leprosy
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 2039/505: {comprising antibodies}
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- Y02E 50/10: Biofuels, e.g. bio-diesel
- Y02E 50/30: Fuel from waste, e.g. synthetic alcohol or diesel
- 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)
- Y02E: REDUCTION OF GREENHOUSE GAS [GHG] EMISSIONS, RELATED TO ENERGY GENERATION, TRANSMISSION OR DISTRIBUTION

## Abstract

An anti-TrkA antibody is provided that comprises: a) a variable heavy chain comprising a sequence selected from any of BXhVH1, BXhVH2, BXhVH3, BXhVH4, BXhVH5, or HuVHWOv as shown in FIG. 1a; or from variants of any of said sequences and/or b) a variable light chain comprising a sequence selected from any of BXhVL1, BXhVL2, BXhVL3, BXhVL4, BXhVL5, BXhVL6, BXhVL7 or BXhVL8; as shown in FIG. 1b, or from variants of any of said sequences. TrkA-binding derivatives are also provided. Antibodies or derivatives of the present invention are useful in a number of therapies, including pain therapy.

## Claims

### Claim 1

An anti-TrkA antibody comprising:
a) a variable heavy chain consisting of the sequence BXhVH5 (SEQ ID NO: 5); and
b) a variable light chain consisting of the sequence BXhVL1(SEQ ID NO: 7);
or an antigen binding fragment thereof.

### Claim 2 (depends on 1)

The antibody of claim 1 that is PEGylated.

### Claim 3 (depends on 1)

The antibody of claim 1 in immobilised form.

### Claim 4 (depends on 1)

The antibody of claim 1 for use in medicine.

### Claim 5 (depends on 1)

A method for the treatment of pain, said method comprising:
administering to a subject the antibody of claim 1.

### Claim 6 (depends on 5)

The method of claim 5, wherein the pain is chronic pain.

### Claim 7 (depends on 5)

The method of claim 5, wherein the pain is acute pain.

### Claim 8 (depends on 1)

A combination of the antibody of claim 1 and an analgesic, for simultaneous, sequential or concerted administration in medicine.

### Claim 9 (depends on 1)

A combination of the antibody of claim 1 and NGF, for simultaneous, sequential or concerted administration in medicine.

### Claim 10 (depends on 1)

A combination of the antibody of claim 1 and a further anti-TrkA antibody or derivative thereof, for simultaneous, sequential or concerted administration in medicine.

### Claim 11 (depends on 1)

A pharmaceutical composition comprising the antibody of claim 1 and a pharmaceutically acceptable carrier or excipient.

### Claim 12 (depends on 1)

A pharmaceutical composition comprising the antibody of claim 1 and another pharmaceutically active agent.

### Claim 13 (depends on 12)

The pharmaceutical composition of claim 12; wherein said another agent is one or more of:
a) an analgesic agent
b) another anti-TrkA antibody or derivative thereof
c) NGF
d) an anti-cancer agent.

### Claim 14 (depends on 1)

The antibody of claim 1 for use in diagnosis or prognosis.

### Claim 15 (depends on 1)

The antibody of claim 1 for use in the diagnosis or prognosis of a condition involving aberrant expression of TrkA or an aberrant activity involving TrkA.

### Claim 16 (depends on 1)

An antibody or antigen binding fragment thereof according to claim 1 for use in the diagnosis or prognosis of any of the diseases or disorders selected from the group consisting of: chronic pain and acute pain.

### Claim 17 (depends on 1)

A method comprising obtaining a biological sample and contacting the sample to detect binding of an antibody or antigen binding fragment thereof according to claim 1 thereto.

### Claim 18 (depends on 17)

A method according to claim 17 further comprising comparing the results for binding of said antibody or antigen binding fragment thereof to said sample with a positive or negative control sample.

### Claim 19 (depends on 1)

A non-human transgenic mammal that expresses the antibody of claim 1 or that can be induced to provide such expression.

### Claim 20 (depends on 1)

A kit of parts comprising the antibody of claim 1 together with instructions directing the use thereof by a subject as an analgesic.