# US 10,479,837 B2 · Methods for treating subjects having a CXC chemokine receptor 5 (CXCR5)-responsive cancer by administering fully human anti-CXCR5 antibodies

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- Number: US 10,479,837 B2
- Document ID: US10479837B2
- Status: Granted
- Kind: B2
- Application number: 15/674,401
- Filed: 2017-08-10
- Published: 2017-11-30
- Granted: 2019-11-19
- Earliest claimed: 2014-08-22
- Assignees: Sorrento Therapeutics, Inc.
- Applicants: Sorrento Therapeutics, Inc.
- Inventors: Dingqiu Huang; Barbara A. Swanson; Heyue Zhou
- Web page: https://patentgrep.com/patent/US10479837B2

## CPC

- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
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- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 7/06: Antianaemics
- 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 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/06: Antipsoriatics
- A61P 17/14: for baldness or alopecia
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- 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 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 31/08: for leprosy
- A61P 31/14: for RNA viruses
- A61P 31/16: for influenza or rhinoviruses
- A61P 31/18: for HIV
- A61P 31/20: for DNA viruses
- A61P 33/00: Antiparasitic agents
- A61P 33/06: Antimalarials
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- C07K 2317/21: from primates, e.g. man
- 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
- 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

## Abstract

There is disclosed compositions and methods relating to or derived from anti-CXCR5 antibodies. More specifically, there is disclosed fully human antibodies that bind CXCR5, CXCR5-binding fragments and derivatives of such antibodies, and CXCR5-binding polypeptides comprising such fragments. Further still, there is disclosed nucleic acids encoding such antibodies, antibody fragments and derivatives and polypeptides, cells comprising such polynucleotides, methods of making such antibodies, antibody fragments and derivatives and polypeptides, and methods of using such antibodies, antibody fragments and derivatives and polypeptides, including methods of treating or diagnosing subjects having CXCR5 related disorders or conditions, including various inflammatory disorders and various cancers.

## Claims

### Claim 1

A method for treating a subject having a C-X-C Motif Chemokine Receptor 5 (CXCR5)-positive cancer, said method comprising administering an effective amount of an anti-CXCR5 polypeptide to a subject in need thereof, wherein the anti-CXCR5 polypeptide is selected from the group consisting of a recombinant fully human anti-CXCR5 antibody that binds to CXCR5, a recombinant fully human anti-CXCR5 antibody Fab fragment, and a recombinant anti-CXCR5 single chain antibody, wherein the anti-CXCR5 polypeptide comprises a heavy chain variable domain comprising the amino acid sequence of SEQ ID NO. 108, and comprises a light chain variable domain comprising the amino acid sequence of SEQ ID NO. 109.

### Claim 2 (depends on 1)

The method of claim 1, wherein the recombinant fully human anti-CXCR5 antibody is classified as an isotype selected from the group consisting of: IgG, IgM, IgD, IgA, and IgE.

### Claim 3 (depends on 2)

The method of claim 2, wherein the IgG isotype antibody is an IgG1 or an IgG4.

### Claim 4 (depends on 1)

The method of claim 1, wherein the recombinant fully human anti-CXCR5 antibody, or an antigen-binding fragment thereof, is classified as an isotype selected from the group consisting of: IgG, IgM, IgD, IgA, and IgE.

### Claim 5 (depends on 1)

The method of claim 1, wherein the CXCR5-positive cancer is selected from the group consisting of colorectal cancer, head and neck cancer, small cell lung cancer, non-small cell lung cancer (NSCLC), pancreatic cancer, bladder cancer, blood cancer, bone cancer, brain cancer, breast cancer, cartilage cancer, colon cancer, endometrial cancer, gastric cancer, kidney cancer, liver cancer, lung cancer, lymph node cancer, nervous tissue cancer, ovarian cancer, pancreatic cancer, prostate cancer, skeletal muscle cancer, skin cancer, spinal cord cancer, spleen cancer, stomach cancer, testes cancer, thymus cancer, thyroid cancer, tracheal cancer, urogenital tract cancer, ureter cancer, urethral cancer, uterine cancer and vaginal cancer.