# US 11,027,015 B2 · Antibodies specifically binding to MASP-3 for the treatment of various diseases and disorders

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- Number: US 11,027,015 B2
- Document ID: US11027015B2
- Status: Granted
- Kind: B2
- Application number: 16/909,578
- Filed: 2020-06-23
- Published: 2020-10-08
- Granted: 2021-06-08
- Earliest claimed: 2016-08-01
- Assignees: Omeros Corporation
- Applicants: Omeros Corporation
- Inventors: W. Jason Cummings; Gregory A. Demopulos; Thomas Dudler; Larry W. Tjoelker; Christi L. Wood; Munehisa Yabuki
- Web page: https://patentgrep.com/patent/US11027015B2

## CPC

- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61K 39/00: Medicinal preparations containing antigens or antibodies (materials for immunoassay G01N33/53)
- A61P 7/06: Antianaemics
- A61P 7/08: Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock (artificial tears A61P27/04)
- 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 11/16: Central respiratory analeptics
- A61P 13/12: of the kidneys
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 21/04: for myasthenia gravis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- 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 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 39/02: Antidotes
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- B82Y 25/00: Nanomagnetism, e.g. magnetoimpedance, anisotropic magnetoresistance, giant magnetoresistance or tunneling magnetoresistance
- C01F 17/206: oxide or hydroxide being the only anion
- C07K 16/40: against enzymes
- C09K 11/77: containing rare earth metals
- C09K 11/7728: {containing europium}
- C12N 9/6424: {Serine endopeptidases (3.4.21)}
- C12Y 304/21104: Mannan-binding lectin-associated serine protease-2 (3.4.21.104)
- H01F 1/0054: {Coated nanoparticles, e.g. nanoparticles coated with organic surfactant}
- A61K 2039/505: {comprising antibodies}
- A61K 2039/54: {characterised by the route of administration}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- C01P 2002/54: one element only
- C01P 2002/84: by UV- or VIS- data
- C01P 2004/64: Nanometer sized, i.e. from 1-100 nanometer
- 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 2317/34: 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 2317/734: Complement-dependent cytotoxicity [CDC]
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/90: characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- 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
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- C01F: COMPOUNDS OF THE METALS BERYLLIUM, MAGNESIUM, ALUMINIUM, CALCIUM, STRONTIUM, BARIUM, RADIUM, THORIUM, OR OF THE RARE-EARTH METALS (metal hydrides {monoborane, diborane or addition complexes thereof} C01B6/00; salts of oxyacids of halogens C01B11/00; peroxides, salts of peroxyacids C01B15/00; sulfides or polysulfides of magnesium, calcium, strontium, or barium C01B17/42; thiosulfates, dithionites, polythionates C01B17/64; compounds containing selenium or tellurium C01B19/00; binary compounds of nitrogen with metals C01B21/06; azides C01B21/08; {compounds other than ammonia or cyanogen containing nitrogen and non-metals and optionally metals C01B21/082; amides or imides of silicon C01B21/087}; metal {imides or} amides C01B21/092, {C01B21/0923}; nitrites C01B21/50; {compounds of noble gases C01B23/0005}; phosphides C01B25/08; salts of oxyacids of phosphorus C01B25/16; carbides C01B32/90; compounds containing silicon C01B33/00; compounds containing boron C01B35/00; compounds having molecular sieve properties but not having base-exchange properties C01B37/00; compounds having molecular sieve and base-exchange properties, e.g. crystalline zeolites, C01B39/00; cyanides C01C3/08; salts of cyanic acid C01C3/14; salts of cyanamide C01C3/16; thiocyanates C01C3/20; {double sulfates of magnesium with sodium or potassium C01D5/12; with other alkali metals C01D15/00, C01D17/00})
- 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)
- C09K: MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- C12Y: ENZYMES
- H01F: MAGNETS; INDUCTANCES; TRANSFORMERS; SELECTION OF MATERIALS FOR THEIR MAGNETIC PROPERTIES
- C01P: INDEXING SCHEME RELATING TO STRUCTURAL AND PHYSICAL ASPECTS OF SOLID INORGANIC COMPOUNDS

## Abstract

The present invention relates to MASP-3 inhibitory antibodies and compositions comprising such antibodies for use in inhibiting the adverse effects of MASP-3 dependent complement activation.

## Claims

### Claim 1

An isolated antibody, or antigen-binding fragment thereof, that binds to human MASP-3 comprising:
a heavy chain variable region comprising a HC-CDR1 set forth as SEQ ID NO:72 (SYGMS) a HC-CDR2 set forth as SEQ ID NO:74 (WINTYSGVPTYADDFKG); and a HC-CDR3 set forth as SEQ ID NO:76 (GGEAMDY); and a light chain variable region comprising a LC-CDR1 selected from the group consisting of SEQ ID NO:153 (KSSQSLLDSDGKTYLN), SEQ ID NO:261 (KSSQSLLDSEGKTYLN), SEQ ID NO:262 (KSSQSLLDSAGKTYLN) and SEQ ID NO:263 (KSSQSLLDSDAKTYLN); a LC-CDR2 set forth as SEQ ID NO:155 (LVSKLDS); and a LC-CDR3 set forth as SEQ ID NO:157 (WQGTHFPWT).

### Claim 2 (depends on 1)

The isolated antibody, or antigen-binding fragment thereof of claim 1, wherein the LC-CDR1 comprises SEQ ID NO:261 (KSSQSLLDSEGKTYLN).

### Claim 3 (depends on 1)

The isolated antibody, or antigen-binding fragment thereof of claim 1, wherein the LC-CDR1 comprises SEQ ID NO:262 (KSSQSLLDSAGKTYLN).

### Claim 4 (depends on 1)

The isolated antibody, or antigen-binding fragment thereof of claim 1, wherein the LC-CDR1 comprises SEQ ID NO:263 (KSSQSLLDSDAKTYLN).

### Claim 5 (depends on 1)

The isolated antibody or antigen-binding fragment thereof of claim 1, wherein the HC-CDR1 comprises SEQ ID NO:72, the HC-CDR2 comprises SEQ ID NO:74, the HC-CDR3 comprises SEQ ID NO:76, the LC-CDR1 comprises SEQ ID NO:153, the LC-CDR2 comprises SEQ ID NO:155 and the LC-CDR3 comprises SEQ ID NO:157.

### Claim 6 (depends on 1)

The isolated antibody or antigen-binding fragment thereof of claim 1, wherein the HC-CDR1 comprises SEQ ID NO:72, the HC-CDR2 comprises SEQ ID NO:74, the HC-CDR3 comprises SEQ ID NO:76, the LC-CDR1 comprises SEQ ID NO:263, the LC-CDR2 comprises SEQ ID NO:155 and the LC-CDR3 comprises SEQ ID NO:157.

### Claim 7 (depends on 1)

The isolated antibody or antigen-binding fragment thereof of claim 1, wherein the heavy chain variable region comprises an amino acid sequence selected from the group consisting of SEQ ID NO:28, SEQ ID NO:251 and SEQ ID NO:252.

### Claim 8 (depends on 1)

The isolated antibody or antigen-binding fragment thereof of claim 1, wherein the light chain variable region comprises an amino acid sequence selected from the group consisting of SEQ ID NO:43, SEQ ID NO:253 and SEQ ID NO:279.

### Claim 9 (depends on 1)

The antibody or antigen binding fragment thereof of claim 1, wherein the antibody or antigen-binding fragment is selected from the group consisting of a humanized antibody, a chimeric antibody, a murine antibody, and an antigen-binding fragment of any of the foregoing.

### Claim 10 (depends on 1)

The antibody or antigen-binding fragment thereof of claim 1, wherein said antibody or antigen binding fragment thereof is selected from the group consisting of a single chain antibody, an ScFv, a Fab fragment, an Fab′ fragment, an F(ab′)2 fragment, a univalent antibody lacking a hinge region and a whole antibody.

### Claim 11 (depends on 1)

The antibody or antigen-binding fragment thereof of claim 1, wherein said antibody inhibits alternative pathway activation in mammalian blood.

### Claim 12 (depends on 1)

A composition comprising the antibody or antigen-binding fragment of claim 1 and a pharmaceutically acceptable excipient.

### Claim 13

An isolated antibody or antigen-binding fragment thereof that binds to human MASP-3, comprising a heavy chain variable region selected from the group consisting of SEQ ID NO:28, SEQ ID NO:251 and SEQ ID NO:252 and a light chain variable region selected from the group consisting of SEQ ID NO:43, SEQ ID NO:253 and SEQ ID NO:279.

### Claim 14 (depends on 13)

The isolated antibody or antigen-binding fragment thereof of claim 13, wherein the heavy chain variable region comprises SEQ ID NO:28 and the light chain variable region comprises SEQ ID NO:43.

### Claim 15 (depends on 13)

The isolated antibody or antigen-binding fragment thereof of claim 13, wherein the heavy chain variable region comprises SEQ ID NO:251 or SEQ ID NO:252 and the light chain variable region comprises SEQ ID NO:253.

### Claim 16 (depends on 13)

The isolated antibody or antigen-binding fragment thereof of claim 13, wherein the heavy chain variable region comprises SEQ ID NO:251 or SEQ ID NO:252 and the light chain variable region comprises SEQ ID NO:279.

### Claim 17 (depends on 13)

The isolated antibody of claim 13, wherein the antibody is selected from the group consisting of a single chain antibody, an ScFv, a Fab fragment, an Fab′ fragment, an F(ab′)2 fragment, a univalent antibody lacking a hinge region and a whole antibody.

### Claim 18 (depends on 13)

The isolated antibody or antigen-binding fragment thereof of claim 13, wherein said antibody inhibits alternative pathway activation in mammalian blood.

### Claim 19 (depends on 13)

A composition comprising the antibody or antigen-binding fragment of claim 13 and a pharmaceutically acceptable excipient.