# US 2025/0084178 A1 · Anti-cd39 antibodies 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 2025/0084178 A1 - Document ID: US20250084178A1 - Status: Published application - Kind: A1 - Application number: 18/616,056 - Filed: 2024-03-25 - Published: 2025-03-13 - Earliest claimed: 2022-03-03 - Assignees: Arcus Biosciences, Inc.; Wuxi Biologics Ireland Limited - Applicants: Arcus Biosciences, Inc.; Wuxi Biologics Ireland Limited - Inventors: Christine Elizabeth Bowman; Ada Pei Xian Chen; Ester Fernandez-Salas; Nigel Pelham Clinton Walker; Xiaoning Zhao; Yaohua Hu; Siwei Nie; Jijie Gu - Web page: https://patentgrep.com/patent/US20250084178A1 ## CPC - C07K 16/2896: {against molecules with a "CD"-designation, not provided for elsewhere} - A61K 31/555: containing heavy metals, e.g. hemin, hematin, melarsoprol - A61K 39/39558: {against tumor tissues, cells, antigens} - A61P 35/00: Antineoplastic agents - 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 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity - C07K 2317/52: Constant or Fc region; Isotype - 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: 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 Provided herein are anti-CD39 antibodies that inhibit the enzymatic activity of human CD39 and methods of using the same. ## Claims ### Claim 1 An anti-CD39 antibody that specifically binds to human CD39, comprising (a) a heavy chain variable region comprising a complementarity determining region 1 (H1) having an amino acid sequence comprising SEQ ID NO: 10, a complementarity determining region 2 (H2) having an amino acid sequence comprising SEQ ID NO: 11, and a complementarity determining region 3 (H3) having an amino acid sequence comprising SEQ ID NO: 12; and a light chain variable region comprising a complementarity determining region 1 (L1) having an amino acid sequence comprising SEQ ID NO: 14, a complementarity determining region 2 (L2) having an amino acid sequence comprising SEQ ID NO: 15, and a complementarity determining region 3 (L3) having an amino acid sequence comprising ID NO: 16; (b) a heavy chain variable region comprising an H1 having an amino acid sequence comprising SEQ ID NO: 18, an H2 having an amino acid sequence comprising SEQ ID NO: 19, and an H3 having an amino acid sequence comprising SEQ ID NO: 20; and a light chain variable region comprising an L1 having an amino acid sequence comprising SEQ ID NO: 22, SEQ ID NO: 23, or SEQ ID NO: 24, an L2 having an amino acid sequence comprising SEQ ID NO: 25, and an L3 having an amino acid sequence comprising SEQ ID NO: 26; or (c) a heavy chain variable region comprising an H1 having an amino acid sequence comprising SEQ ID NO: 28, an H2 having an amino acid sequence comprising SEQ ID NO: 29, and an H3 having an amino acid sequence comprising SEQ ID NO: 30; and a light chain variable region comprising an L1 having an amino acid sequence comprising SEQ ID NO: 32, an L2 having an amino acid sequence comprising SEQ ID NO: 33, and an L3 having an amino acid sequence comprising SEQ ID NO: 34. ### Claim 2 (depends on 1) The anti-CD39 antibody of claim 1, wherein the antibody has a heavy chain variable region and a light chain variable region according to claim 1(a) and the heavy chain variable region has at least 90% sequence identity to SEQ ID NO: 9, and a light chain variable region has at least 90% sequence identity to SEQ ID NO: 13; or wherein the antibody has a heavy chain variable region and a light chain variable region according to claim 1(b) and the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 17, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 21; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 43, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 45; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 43, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 46; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 43, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 47; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 43, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 48; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 43, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 49; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 44, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 48; or the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 44, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 49; wherein the antibody has a heavy chain variable region and a light chain variable region according to claim 1(c) and the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 27, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 31; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 58, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 60; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 58, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 61; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 58, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 62; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 58, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 63; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 59, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 61; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 59, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 60; the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 59, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 62; or the heavy chain variable region having at least 90% sequence identity to SEQ ID NO: 59, and a light chain variable region having at least 90% sequence identity to SEQ ID NO: 63. ### Claim at position 3 3-5. (canceled) ### Claim 6 (depends on 1) The anti-CD39 antibody of claim 1, wherein the anti-CD39 antibody is a monoclonal antibody or an antigen-binding fragment thereof. ### Claim 7 (depends on 1) The anti-CD39 antibody of claim 1, wherein the anti-CD39 antibody is a human, chimeric, humanized, or veneered antibody or an antigen-binding fragment thereof. ### Claim 8 (canceled) ### Claim 9 (depends on 1) The anti-CD39 antibody of claim 1, wherein the antibody further comprises a variant heavy chain constant region selected from a variant human IgG1 constant region, a variant human IgG2 constant region, a variant human IgG3 constant region, or a variant human IgG4 constant region. ### Claim 10 (canceled) ### Claim 11 (depends on 9) The anti-CD39 antibody of claim 9, wherein the variant human IgG heavy chain constant region comprises SEQ ID NO: 2, SEQ ID NO: 3, or SEQ ID NO: 5. ### Claim 12 (depends on 1) The anti-CD39 antibody of claim 1, wherein the antibody further comprises a wild-type human IgG heavy chain constant region. ### Claim 13 (depends on 12) The anti-CD39 antibody of claim 12, wherein the wild-type human IgG heavy chain constant region comprises SEQ ID NO: 1 or SEQ ID NO: 4. ### Claim 14 (depends on 9) The anti-CD39 antibody of claim 9 comprising a human light chain kappa constant region. ### Claim 15 (depends on 1) The anti-CD39 antibody of claim 1, wherein the antibody has a heavy chain comprising the heavy chain variable region and a light chain comprising the light chain variable region, wherein (a) the heavy chain has an amino acid sequence comprising SEQ ID NO: 50, and the light chain has an amino acid sequence comprising SEQ ID NO: 53; (b) the heavy chain has an amino acid sequence comprising SEQ ID NO: 50, and the light chain has an amino acid sequence comprising SEQ ID NO: 54; (c) the heavy chain has an amino acid sequence comprising SEQ ID NO: 50, and the light chain has an amino acid sequence comprising SEQ ID NO: 55; (d) the heavy chain has an amino acid sequence comprising SEQ ID NO: 50, and the light chain has an amino acid sequence comprising SEQ ID NO: 56; (e) the heavy chain has an amino acid sequence comprising SEQ ID NO: 51, and the light chain has an amino acid sequence comprising SEQ ID NO: 56; (f) the heavy chain has an amino acid sequence comprising SEQ ID NO: 50, and the light chain has an amino acid sequence comprising SEQ ID NO: 57; (g) the heavy chain has an amino acid sequence comprising SEQ ID NO: 52, and the light chain has an amino acid sequence comprising SEQ ID NO: 56; or (h) the heavy chain has an amino acid sequence comprising SEQ ID NO: 52, and the light chain has an amino acid sequence comprising SEQ ID NO: 57. ### Claim 16 (depends on 1) The anti-CD39 antibody of claim 1, wherein the antibody has a heavy chain comprising the heavy chain variable region and a light chain comprising the light chain variable region, wherein (a) the heavy chain has an amino acid sequence comprising SEQ ID NO: 64, and the light chain has an amino acid sequence comprising SEQ ID NO: 67; (b) the heavy chain has an amino acid sequence comprising SEQ ID NO: 64, and the light chain has an amino acid sequence comprising SEQ ID NO: 68; (c) the heavy chain has an amino acid sequence comprising SEQ ID NO: 64, and the light chain has an amino acid sequence comprising SEQ ID NO: 69; (d) the heavy chain has an amino acid sequence comprising SEQ ID NO: 64, and the light chain has an amino acid sequence comprising SEQ ID NO: 70; (e) the heavy chain has an amino acid sequence comprising SEQ ID NO: 65, and the light chain has an amino acid sequence comprising SEQ ID NO: 68; (f) the heavy chain has an amino acid sequence comprising SEQ ID NO: 65, and the light chain has an amino acid sequence comprising SEQ ID NO: 67; (g) the heavy chain has an amino acid sequence comprising SEQ ID NO: 66, and the light chain has an amino acid sequence comprising SEQ ID NO: 67; (h) the heavy chain has an amino acid sequence comprising SEQ ID NO: 65, and the light chain has an amino acid sequence comprising SEQ ID NO: 69; or (i) the heavy chain has an amino acid sequence comprising SEQ ID NO: 65, and the light chain has an amino acid sequence comprising SEQ ID NO: 70. ### Claim at position 15 17-20. (canceled) ### Claim 21 (depends on 1) A method of inhibiting CD39 enzymatic activity comprising contacting CD39 with the anti-CD39 antibody of claim 1. ### Claim 22 (depends on 1) A method for increasing extracellular ATP or activating the immune system in a subject in need thereof comprising administering to the subject an effective regime or a therapeutically effective amount of any one of the anti-CD39 antibodies of claim 1. ### Claim 23 (depends on 1) A method of treating or effecting prophylaxis of cancer comprising administering to a subject having or at risk of cancer an effective regime or a therapeutically effective amount of any one of the anti-CD39 antibodies of claim 1. ### Claim at position 19 24-30. (canceled) ### Claim 31 (depends on 1) A combination comprising an anti-CD39 antibody of claim 1 and one or more additional therapeutic agent. ### Claim at position 21 32-47. (canceled) ### Claim 48 (depends on 1) A pharmaceutical composition comprising the antibody of claim 1 and a pharmaceutically acceptable carrier. ### Claim 49 (depends on 1) An isolated polynucleotide encoding the antibody of claim 1. ### Claim 50 (canceled) ### Claim 51 (depends on 49) A host cell comprising the isolated polynucleotide of claim 49. ### Claim 52 (depends on 1) A method of expressing the antibody of claim 1, comprising culturing a host cell comprising a vector or polynucleotide encoding the antibody of claim 1 under conditions at which the polynucleotide is expressed. ### Claim 53 (depends on 1) A kit comprising the antibody of claim 1.