# US 9,751,951 B2 · Methods of treatment by administering an anti-BAFFR antibody therapeutic formulation

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- Number: US 9,751,951 B2
- Document ID: US9751951B2
- Status: Granted
- Kind: B2
- Application number: 14/942,388
- Filed: 2015-11-16
- Published: 2016-05-26
- Granted: 2017-09-05
- Earliest claimed: 2012-06-12
- Assignees: Novartis AG
- Applicants: Marta Cosenza; Christoph Stark
- Inventors: Marta Cosenza; Christoph Stark
- Web page: https://patentgrep.com/patent/US9751951B2

## CPC

- C07K 16/2878: {against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 39/39591: {Stabilisation, fragmentation}
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/02: specific for leukemia
- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- A61K 2039/505: {comprising antibodies}
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- 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: 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

Anti-BAFFR antibodies are formulated as liquid formulation comprising a high concentration of the antibody active ingredient for delivery to a patient without high levels of antibody aggregation. The aqueous pharmaceutical composition may include one or more sugars, a buffering agent, a surfactant, and/or a free amino acid.

## Claims

### Claim 1

A method of treating an autoimmune disease in a patient in need thereof comprising the step of administering to said patient an aqueous composition having a pH of 6.0 and comprising:
a hypofucosylated or non-fucosylated anti-B-cell Activating Factor Receptor (BAFFR) antibody wherein the antibody has a concentration of 150 mg/mL and wherein said anti-BAFFR antibody comprise heavy chain CDR1, CDR2 and CDR3 of SEQ ID NOs: 3, 4 and 5 respectively, and light chain CDR1, CDR2 and CDR3 of SEQ ID NOs: 6, 7 and 8, and:
(a) (i) 220 mM sucrose as a stabilizer,
(ii) 20 mM histidine as a buffering agent,
(iii) 0.04% polysorbate 20 as a surfactant; or
(b) (i) 220 mM trehalose as a stabilizer,
(ii) 20 mM histidine as a buffering agent,
(iii) 0.04% polysorbate 20 as a surfactant; or
(c) (i) 120 mM sucrose as a stabilizer,
(ii) 20 mM histidine as a buffering agent,
(iii) 0.04% polysorbate 20 as a surfactant, and
(iv) 50 mM arginine.

### Claim 2 (depends on 1)

The method of claim 1, wherein the autoimmune disease is selected from rheumatoid arthritis, systemic lupus erythematosus, Sjögren's syndrome, or Pemphigus vulgaris.

### Claim 3 (depends on 1)

The method of claim 1, wherein the anti-BAFFR antibody comprises a VH domain comprising the amino acid sequence of SEQ ID NO: 1 and a VL domain comprising the amino acid sequence of SEQ ID NO: 2.

### Claim 4 (depends on 1)

The method of claim 1, wherein the anti-BAFFR antibody comprises a heavy chain region comprising the amino acid sequence of SEQ ID NO: 9 and a light chain region comprising the amino acid sequence of SEQ ID NO: 10.

### Claim 5 (depends on 1)

The method of claim 1, wherein the arginine is arginine-HCl.