# US 2023/0054413 A1 · Stable anti-pd1 antibody pharmaceutical formulations > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2023/0054413 A1 - Document ID: US20230054413A1 - Status: Published application - Kind: A1 - Application number: 17/784,251 - Filed: 2020-12-14 - Published: 2023-02-23 - Earliest claimed: 2019-12-13 - Assignees: Samsung Bioepis Co., Ltd. - Applicants: Samsung Bioepis Co., Ltd. - Inventors: Young Seok JUNG; Ja Hye HONG; Kyung Hee JOO; Young Wook HA; In Young OH; In Ae KIM - Web page: https://patentgrep.com/patent/US20230054413A1 ## CPC - A61P 35/00: Antineoplastic agents - C07K 16/2818: {against CD28 or CD152} - 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 31/70: Carbohydrates; Sugars; Derivatives thereof (sorbitol A61K31/047) - 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 - C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered - C07K 2317/565: Complementarity determining region [CDR] - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - 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 The present disclosure relates to a stable anti-PD-1 antibody pharmaceutical formulation and a method for preparing the same, the pharmaceutical formulation comprising: an anti-PD-1 antibody or an antigen binding fragment thereof; and a stabilizer, and not comprising a buffer. ## Claims ### Claim 1 A stable anti-PD-1 antibody pharmaceutical formulation, comprising: (a) an anti-PD-1 antibody or an antigen binding fragment thereof; and (b) a stabilizer, wherein the formulation does not comprise a buffer and has a pH of about 4.5 to about 6.5. ### Claim 2 (depends on 1) The pharmaceutical formulation of claim 1, wherein the formulation has a pH of about 5.0 to about 5.5. ### Claim 3 (depends on 1) The pharmaceutical formulation of claim 1, wherein the anti-PD-1 antibody includes a heavy chain CDR1 having the amino acid sequence of SEQ ID NO: 1, a heavy chain CDR2 having the amino acid sequence of SEQ ID NO: 2, and a heavy chain CDR3 having the amino acid sequence of SEQ ID NO: 3; and a light chain CDR1 having the amino acid sequence of SEQ ID NO: 4, a light chain CDR2 having the amino acid sequence of SEQ ID NO: 5, and a light chain CDR3 having the amino acid sequence of SEQ ID NO: 6. ### Claim 4 (depends on 1) The pharmaceutical formulation of claim 1, wherein the anti-PD-1 antibody is a pembrolizumab. ### Claim 5 (depends on 1) The pharmaceutical formulation of claim 1, wherein the concentration of the anti-PD-1 antibody or the antigen binding fragment thereof is about 5 to about 200 mg/ml. ### Claim 6 (depends on 1) The pharmaceutical formulation of claim 1, wherein the stabilizer is a polyol, an amino acid or a pharmaceutically acceptable salt, or a mixture thereof. ### Claim 7 (depends on 6) The pharmaceutical formulation of claim 6, wherein the polyol is sorbitol, sucrose, trehalose, mannose, maltose, mannitol, or a mixture thereof. ### Claim 8 (depends on 6) The pharmaceutical formulation of claim 6, wherein the amino acid is glycine, proline, phenylalanine, tyrosine, tryptophan, lysine, arginine, a pharmaceutically acceptable salt thereof, or a mixture thereof. ### Claim 9 (depends on 1) The pharmaceutical formulation of claim 1, wherein the stabilizer is about 1.0 to about 15.0% (w/v) of a sugar, about 1.0 to about 20.0% (w/v) of a sugar alcohol, about 0.1 to about 300.0 mM of an amino acid, or about 1.0 to about 300.0 mM of a metal salt. ### Claim 10 (depends on 1) The pharmaceutical formulation of claim 1, wherein the stabilizer is about 1.0 to about 15.0% (w/v) of a sugar and about 0.1 to about 300.0 mM of an amino acid. ### Claim 11 (depends on 1) The pharmaceutical formulation of claim 1, wherein the buffer is histidine, phosphoric acid, maleic acid, tartaric acid, succinic acid, citric acid, acetic acid, carbonic acid, a pharmaceutically acceptable salt thereof, or a mixture thereof. ### Claim 12 (depends on 1) The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation does not comprise a surfactant or further comprises a surfactant. ### Claim 13 (depends on 12) The pharmaceutical formulation of claim 12, wherein the surfactant is polysorbate, poloxamer, sorbitan ester of another fatty acid, or a mixture thereof. ### Claim 14 (depends on 1) The pharmaceutical formulation of claim 1, further comprising an antioxidant. ### Claim 15 (depends on 14) The pharmaceutical formulation of claim 14, wherein the antioxidant is methionine. ### Claim 16 (depends on 1) The pharmaceutical formulation of claim 1, wherein the pharmaceutical formulation is for administration by intravenous or subcutaneous injection. ### Claim 17 (depends on 1) The pharmaceutical formulation of claim 1, wherein the concentration of the anti-PD-1 antibody or the antigen binding fragment thereof is about 5 to about 200 mg/mL, and the stabilizer is: about 1.0 to about 15.0% (w/v) of sucrose, trehalose, a hydrate thereof, or a mixture thereof; about 1.0 to about 20.0% (w/v) of sorbitol, mannitol, a hydrate thereof, or a mixture thereof; about 0.1 to about 300.0 mM of arginine, lysine, proline, glycine, phenylalanine, tyrosine, tryptophan, a pharmaceutically acceptable salt thereof; or a mixture thereof; or a mixture of two or more thereof. ### Claim 18 (depends on 1) A method for treating a cancer in a subject, comprising administering a therapeutically effective amount of the pharmaceutical formulation according to claim 1 to the subject. ### Claim 19 A method for preparing a stable pharmaceutical formulation, comprising: preparing a mixed solution by adding a stabilizer to a solvent; and adding a pembrolizumab or an antigen binding fragment thereof to the mixed solution, or comprising: preparing a solution of a pembrolizumab or an antigen binding fragment thereof by adding the pembrolizumab or the antigen binding fragment thereof to a solvent; and adding a stabilizer to the solution, wherein the method is performed without adding a buffer. ### Claim 20 (depends on 12) The pharmaceutical formulation of claim 12, wherein the surfactant is a non-ionic surfactant.