# US 2020/0399363 A1 · Pharmaceutical formulations of fcrn inhibitors suitable for subcutaneous administration > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2020/0399363 A1 - Document ID: US20200399363A1 - Status: Published application - Kind: A1 - Application number: 16/893,863 - Filed: 2020-06-05 - Published: 2020-12-24 - Earliest claimed: 2019-06-07 - Assignees: argenx BVBA - Applicants: argenx BVBA - Inventors: Filip Borgions - Web page: https://patentgrep.com/patent/US20200399363A1 ## CPC - C07K 16/247: {IL-4} - 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 39/39591: {Stabilisation, fragmentation} - A61K 47/02: Inorganic compounds - A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame} - A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids - A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones - 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 - C07K 16/00: Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies - A61K 2039/505: {comprising antibodies} - A61K 2039/54: {characterised by the route of administration} - C07K 2317/52: Constant or Fc region; Isotype - 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) ## Abstract Provided are various aqueous formulations of the neonatal Fc receptor (FcRn) antagonist ARGX-113, including formulations useful as pharmaceutical compositions, methods for their preparation, devices comprising the various formulations, and uses thereof. In certain embodiments the formulations are suitable and useful for administration of ARGX-113 to a human subject. In certain embodiments the formulations are suitable and useful for subcutaneous administration of ARGX-113 to a human subject. The formulations can be used in the treatment of any condition that would benefit from inhibition of FcRn-mediated antibody recycling. Such conditions can include any one or more of various antibody-mediated autoimmune diseases, including, for example and without limitation, myasthenia gravis (MG) and immune thrombocytopenia (ITP). ## Claims ### Claim 1 An aqueous formulation comprising about 100-300 mg/mL of an isolated neonatal Fc receptor (FcRn) antagonist in 20-60 mM histidine/histidine HCl, 0-70 mM sucrose, 0-150 mM NaCl, 0-250 mM arginine HCl, 0.02%-0.05% (w/v) polysorbate 20 or polysorbate 80, 0-15 mM L-methionine, pH 6.0-6.5, wherein the isolated FcRn antagonist consists of a variant Fc region, wherein said variant Fc region consists of two Fc domains which form a homodimer, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1, SEQ ID NO: 2, or SEQ ID NO: 3. ### Claim 2 (depends on 1) The aqueous formulation according to claim 1, comprising about 100-200 mg/mL of the isolated neonatal Fc receptor (FcRn) antagonist in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, and 0.02%-0.04% (w/v) polysorbate 20 or polysorbate 80, pH 6.0, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1, SEQ ID NO: 2, or SEQ ID NO: 3. ### Claim 3 (depends on 1) The aqueous formulation according to claim 1, comprising 150 mg/mL ARGX-113 in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, and 0.04% (w/v) polysorbate 20, pH 6.0, wherein ARGX-113 is the isolated FcRn antagonist, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1. ### Claim 4 (depends on 1) The aqueous formulation according to claim 1, comprising 175 mg/mL ARGX-113 in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, and 0.04% (w/v) polysorbate 20, pH 6.0, wherein ARGX-113 is the isolated FcRn antagonist, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1. ### Claim 5 (depends on 1) The aqueous formulation according to claim 1, comprising 200 mg/mL ARGX-113 in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, and 0.04% (w/v) polysorbate 20, pH 6.0, wherein ARGX-113 is the isolated FcRn antagonist, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1. ### Claim 6 (depends on 1) The aqueous formulation according to claim 1, comprising about 100-200 mg/mL of the isolated neonatal Fc receptor (FcRn) antagonist in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, 10 mM L-methionine, and 0.02%-0.04% (w/v) polysorbate 20 or polysorbate 80, pH 6.0, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1, SEQ ID NO: 2, or SEQ ID NO: 3. ### Claim 7 (depends on 1) The aqueous formulation according to claim 1, comprising about 165 mg/mL of the isolated neonatal Fc receptor (FcRn) antagonist in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, 10 mM L-methionine, and 0.04% (w/v) polysorbate 20, pH 6.0, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1, SEQ ID NO: 2, or SEQ ID NO: 3. ### Claim 8 (depends on 1) The aqueous formulation according to claim 1, comprising 175 mg/mL ARGX-113 in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, 10 mM L-methionine, and 0.03% (w/v) polysorbate 20, pH 6.0, wherein ARGX-113 is the isolated FcRn antagonist, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1. ### Claim 9 (depends on 1) The aqueous formulation according to claim 1, comprising 200 mg/mL ARGX-113 in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM NaCl, 10 mM L-methionine, and 0.03% (w/v) polysorbate 20, pH 6.0, wherein ARGX-113 is the isolated FcRn antagonist, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1. ### Claim 10 (depends on 1) The aqueous formulation according to claim 1, comprising about 100-200 mg/mL of the isolated neonatal Fc receptor (FcRn) antagonist in 50 mM histidine/histidine HCl, 60 mM sucrose, 150 mM arginine HCl, and 0.02%-0.04% (w/v) polysorbate 20 or polysorbate 80, pH 6.0, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1, SEQ ID NO: 2, or SEQ ID NO: 3. ### Claim 11 (depends on 1) The aqueous formulation according to claim 1, comprising about 100-200 mg/mL of the isolated neonatal Fc receptor (FcRn) antagonist in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM arginine HCl, 10 mM L-methionine, and 0.02%-0.04% (w/v) polysorbate 20 or polysorbate 80, pH 6.0, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1, SEQ ID NO: 2, or SEQ ID NO: 3. ### Claim 12 An aqueous formulation comprising 175 mg/mL ARGX-113 in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM arginine HCl, 10 mM L-methionine, and 0.03% (w/v) polysorbate 20, pH 6.0, wherein ARGX-113 is the isolated FcRn antagonist, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1. ### Claim 13 (depends on 1) The aqueous formulation according to claim 1, comprising 200 mg/mL ARGX-113 in 20 mM histidine/histidine HCl, 60 mM sucrose, 100 mM arginine HCl, 10 mM L-methionine, and 0.03% (w/v) polysorbate 20, pH 6.0, wherein ARGX-113 is the isolated FcRn antagonist, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1. ### Claim 14 (depends on 1) The aqueous formulation according to claim 1, comprising about 100-300 mg/mL of the isolated neonatal Fc receptor (FcRn) antagonist in 50 mM histidine/histidine HCl, 200 mM arginine HCl, pH 6.5, wherein the amino acid sequence of each of the Fc domains consists of SEQ ID NO: 1, SEQ ID NO: 2, or SEQ ID NO: 3. ### Claim 15 (depends on 1) A packaged pharmaceutical product comprising a sterile container comprising a therapeutically effective amount of the aqueous formulation of claim 1. ### Claim 16 (depends on 1) A device comprising a therapeutically effective amount of the aqueous formulation of claim 1. ### Claim 17 (depends on 16) The device according to claim 16, wherein the device comprises a syringe comprising the aqueous formulation. ### Claim 18 (depends on 12) A packaged pharmaceutical product comprising a sterile container comprising a therapeutically effective amount of the aqueous formulation of claim 12. ### Claim 19 (depends on 12) A device comprising a therapeutically effective amount of the aqueous formulation of claim 12. ### Claim 20 (depends on 19) The device according to claim 19, wherein the device comprises a syringe comprising the aqueous formulation.