# US 10,308,712 B2 · Antibodies that bind human cannabinoid 1 (CB1) receptor

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- Number: US 10,308,712 B2
- Document ID: US10308712B2
- Status: Granted
- Kind: B2
- Application number: 14/774,582
- Filed: 2015-03-27
- Published: 2017-07-27
- Granted: 2019-06-04
- Earliest claimed: 2014-03-27
- Assignees: Bird Rock Bio, Inc.
- Applicants: Bird Rock Bio, Inc.
- Inventors: Anke Kretz-Rommel; Lei Shi; Roger Ferrini; Teddy Yang; Fei Xu; Brian Campion
- Web page: https://patentgrep.com/patent/US10308712B2

## CPC

- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 13/12: of the kidneys
- A61P 19/10: for osteoporosis
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- 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 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 2039/505: {comprising antibodies}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/526: CH3 domain
- C07K 2317/53: Hinge
- C07K 2317/55: Fab or Fab'
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/71: Decreased effector function due to an Fc-modification
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- C07K 2317/734: Complement-dependent cytotoxicity [CDC]
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/77: Internalization into the cell
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- 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)
- 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

## Abstract

The present invention relates to novel antibodies and fragments thereof that binds cannabinoid 1 (CB1) receptor. The antibodies and fragments thereof as disclosed herein include humanized antibodies that bind CB1 receptor. The invention also includes uses of the antibodies for treating a disease or disorder responsive to antagonism or agonism of the CB1 receptor.

## Claims

### Claim 1

An isolated antibody or antigen binding fragment thereof that binds to cannabinoid receptor 1 (CB1), wherein the antibody or antigen binding fragment comprises:
a heavy chain comprising a CDR1 amino acid sequence of SEQ ID NO: 352, a CDR2 amino acid sequence of SEQ ID NO: 353, and a CDR3 amino acid sequence of SEQ ID NO: 354; and
a light chain comprising a CDR1 amino acid sequence of SEQ ID NO: 355, a CDR2 amino acid sequence of SEQ ID NO: 356, and a CDR3 amino acid sequence of SEQ ID NO: 357.

### Claim 2 (depends on 1)

The isolated antibody or antigen binding fragment of claim 1, comprising:
a heavy chain variable region comprising SEQ ID NO: 2; and
a light chain variable region comprising SEQ ID NO: 6.

### Claim 3 (depends on 1)

The isolated antibody or antigen binding fragment of claim 1, comprising:
a heavy chain variable region comprising SEQ ID NO: 339, and
a light chain variable region comprising SEQ ID NO:337.

### Claim 4 (depends on 1)

The isolated antibody or antigen binding fragment of claim 1, comprising:
a heavy chain variable region comprising SEQ ID NO: 340, and
a light chain variable region comprising SEQ ID NO:337.

### Claim 5 (depends on 1)

The isolated antibody or antigen binding fragment of claim 1, comprising:
a heavy chain variable region comprising SEQ ID NO: 341, and
a light chain variable region comprising SEQ ID NO:337.

### Claim 6 (depends on 1)

The isolated antibody or antigen binding fragment of claim 1, comprising:
a heavy chain amino acid sequence comprising an amino acid sequence selected from the group consisting of SEQ ID NO: 436-441, and
a light chain amino acid sequence comprising SEQ ID NO:338.

### Claim 7 (depends on 1)

The isolated antibody or antigen binding fragment of claim 1, comprising:
a heavy chain amino acid sequence comprising SEQ ID NO: 437, and
a light chain amino acid sequence comprising SEQ ID NO:338.

### Claim 8 (depends on 1)

The isolated antibody or antigen binding fragment of claim 1, wherein the antibody is conjugated to a therapeutic agent, a cytotoxic agent, an immunoadhesion molecule, or an imaging agent.

### Claim 9 (depends on 2)

The isolated antibody or antigen binding fragment of claim 2, further comprising:
a heavy chain constant region comprising SEQ ID NO: 4, and
a light chain constant region comprising SEQ ID NO: 8.
