# US 2021/0277098 A1 · RGMa BINDING PROTEIN AND USE THEREOF

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2021/0277098 A1
- Document ID: US20210277098A1
- Status: Published application
- Kind: A1
- Application number: 17/322,482
- Filed: 2021-05-17
- Published: 2021-09-09
- Earliest claimed: 2015-04-28
- Assignees: Mitsubishi Tanabe Pharma Corporation; Osaka University; National University Corporation Chiba University
- Applicants: Mitsubishi Tanabe Pharma Corporation; Osaka University; National University Corporation Chiba University
- Inventors: Motonori HASHIMOTO; Toshihide YAMASHITA
- Web page: https://patentgrep.com/patent/US20210277098A1

## CPC

- C07K 16/22: against growth factors {; against growth regulators}
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 7/04: Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
- A61P 11/06: Antiasthmatics
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- 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 27/06: Antiglaucoma agents or miotics
- A61P 37/00: Drugs for immunological or allergic disorders
- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- C07K 16/46: Hybrid immunoglobulins (hybrids of an immunoglobulin with a peptide not being an immunoglobulin C07K19/00)
- C12N 5/10: Cells modified by introduction of foreign genetic material
- C12N 15/09: Recombinant DNA-technology
- A61K 2039/505: {comprising antibodies}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- 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 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

The present invention aims to obtain an anti-repulsive guidance molecule a (RGMa) antibody having a high binding activity and few side effects which can be used as a medicine for preventing, treating, or preventing the relapse of neurological or immunological diseases. The problem is solved by providing an isolated RGMa binding protein which does not inhibit binding between RGMa and neogenin but neutralizes the neurite outgrowth inhibiting activity of RGMa, preferably by providing an anti-RGMa antibody which has complementarity determining regions having amino acid sequences of SEQ ID NOS: 30-35 or SEQ ID NOS: 36-40 in Sequence Listing, and SFG.

## Claims

### Claim 1

An RGMa-binding protein, which competes with an anti-RGMa antibody, wherein the anti-RGMa antibody has the amino acid sequence of each of the light chain complementarity determining region 1 (LCDR1), the light chain complementarity determining region 2 (LCDR2), the light chain complementarity determining region 3 (LCDR3), the heavy chain complementarity determining region 1 (HCDR1), the heavy chain complementarity determining region 2 (HCDR2) and the heavy chain complementarity determining region 3 (HCDR3) comprises the following:
LCDR1:
(SEQ ID NO: 30)
RASQDISSYLN,
LCDR2:
(SEQ ID NO: 31)
YTSRLHS,
LCDR3:
(SEQ ID NO: 32)
QQLNTLP,
HCDR1:
(SEQ ID NO: 33)
DAWMD,
HCDR2:
(SEQ ID NO: 34)
EIRSKANNHATYYAESVKG
and
HCDR3:
(SEQ ID NO: 35)
RDGAY;
or
LCDR1:
(SEQ ID NO: 36)
RSSQSLVHSNGNTYLH
LCDR2:
(SEQ ID NO: 37)
KVSNRFS
LCDR3:
(SEQ ID NO: 38)
SQSTHVP
HCDR1:
(SEQ ID NO: 39)
TSYYWN
HCDR2:
(SEQ ID NO: 40)
YISYDGTNNYNPSLKN
and
HCDR3:
SFG.

### Claim 2 (depends on 1)

A nucleic acid molecule coding for the RGMa-binding protein according to claim 1.

### Claim 3 (depends on 2)

A recombinant vector comprising the nucleic acid molecule according to claim 2.

### Claim 4 (depends on 3)

A host cell containing the recombinant vector according to claim 3.

### Claim 5 (depends on 1)

A method for producing the RGMa-binding protein according to claim 1, the method comprising a step of culturing a host cell, wherein the host cell contains a recombinant vector, and wherein the recombinant vector comprises a nucleic acid molecule coding for the RGMa-binding protein according to claim 1.

### Claim 6 (depends on 1)

A pharmaceutical composition comprising RGMa-binding protein according to claim 1.

### Claim 7 (depends on 6)

The pharmaceutical composition according to claim 6 for use in treating or reducing the relapse of neurological or immunological diseases.

### Claim 8 (depends on 7)

The pharmaceutical composition according to claim 7, wherein the neurological diseases are selected from the group consisting of amyotrophic lateral sclerosis, brachial plexus injury, brain damage, cerebral palsy, Guillain-Barre syndrome, cerebral leukodystrophy, multiple sclerosis, neuromyelitis optica, post-polio syndrome, spina bifida, spinal cord injury, spinal muscular atrophy, spinal neoplasm, transverse myelitis, dementia, Huntington's disease, tardive dyskinesia, mania, Parkinson's disease, Steele-Richardson syndrome, Down's syndrome, myasthenia gravis, neurotrauma, vascular amyloidosis, cerebral hemorrhage associated with amyloidosis, brain infarction, cerebritis, acute confusional state, glaucoma, schizophrenia and retinal nerve fiber layer degeneration.

### Claim 9 (depends on 7)

The pharmaceutical composition according to claim 7, wherein the immunological diseases are selected from the group consisting of multiple sclerosis, neuromyelitis optica, psoriasis, arthritis, Guillain-Barre syndrome, neuro-Behcet disease, pernicious anemia, type I (insulin-dependent)diabetes mellitus, systemic lupus erythematosus (SLE), inflammatory bowel disease (IBD), Sjogren's syndrome, Goodpasture's syndrome, Graves' disease, autoimmune hemolytic anemia, autoimmune thrombocytopenic purpura, asthma, pollinosis, atopic dermatitis, glomerulonephritis, myasthenia gravis, Hashimoto's disease, and sarcoidosis.

### Claim 10 (depends on 7)

The pharmaceutical composition according to claim 7, wherein the neurological or immunological diseases are selected from the group consisting of spinal cord injury, neurotrauma, and multiple sclerosis.