# US 12,600,780 B2 · Anti-CD3 antibodies, bispecific antigen-binding molecules that bind CD3 and CD20, and uses thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,600,780 B2 - Document ID: US12600780B2 - Status: Granted - Kind: B2 - Application number: 18/512,432 - Filed: 2023-11-17 - Published: 2024-10-24 - Granted: 2026-04-14 - Earliest claimed: 2012-09-21 - Assignees: Regeneron Pharmaceuticals, Inc. - Applicants: Regeneron Pharmaceuticals, Inc. - Inventors: Eric Smith; Nicholas J. Papadopoulos - Web page: https://patentgrep.com/patent/US12600780B2 ## CPC - C07K 16/2809: {against the T-cell receptor (TcR)-CD3 complex} - A61P 35/00: Antineoplastic agents - A61P 35/02: specific for leukemia - A61P 37/04: Immunostimulants - C07K 16/2887: {against CD20} - A61K 2039/505: {comprising antibodies} - C07K 2317/21: from primates, e.g. man - C07K 2317/31: multispecific - C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity - C07K 2317/35: Valency - C07K 2317/734: Complement-dependent cytotoxicity [CDC] - C07K 2317/74: Inducing cell proliferation - C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value - Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - 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) - Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE ## Abstract The present invention provides antibodies that bind to CD3 and methods of using the same. According to certain embodiments, the antibodies of the invention bind human CD3 with high affinity and induce human T cell proliferation. The invention includes antibodies that bind CD3 and induce T cell-mediated killing of tumor cells. According to certain embodiments, the present invention provides bispecific antigen-binding molecules comprising a first antigen-binding domain that specifically binds human CD3, and a second antigen-binding molecule that specifically binds human CD20. In certain embodiments, the bispecific antigen-binding molecules of the present invention are capable of inhibiting the growth of B-cell tumors expressing CD20. The antibodies and bispecific antigen-binding molecules of the invention are useful for the treatment of diseases and disorders in which an upregulated or induced targeted immune response is desired and/or therapeutically beneficial. For example, the antibodies of the invention are useful for the treatment of various cancers as well as other CD20-related diseases and disorders. ## Claims ### Claim 1 An antigen-binding molecule that binds human CD3, wherein the antigen-binding molecule comprises a heavy chain variable region (HCVR) comprising three heavy chain complementarity determining regions, HCDR1, HCDR2, and HCDR3, comprising the amino acid sequences of SEQ ID NOs: 1052, 1054 and 1056, respectively, and a light chain variable region (LCVR) comprising three light chain complementarity determining regions, LCDR1, LCDR2 and LCDR3, comprising the amino acid sequences of SEQ ID NO: 1236, AAS and SEQ ID NO: 1240, respectively. ### Claim 2 (depends on 1) The antigen-binding molecule of claim 1, wherein the HCVR comprises the amino acid sequence of SEQ ID NO: 1050. ### Claim 3 (depends on 2) The antigen-binding molecule of claim 2 that is an antibody or antigen-binding fragment thereof. ### Claim 4 (depends on 2) A pharmaceutical composition comprising the antigen-binding molecule of claim 2, and a pharmaceutically acceptable carrier or diluent. ### Claim 5 (depends on 1) The antigen-binding molecule of claim 1, wherein the LCVR comprises the amino acid sequence of SEQ ID NO: 1234. ### Claim 6 (depends on 5) The antigen-binding molecule of claim 5 that is an antibody or antigen-binding fragment thereof. ### Claim 7 (depends on 5) A pharmaceutical composition comprising the antigen-binding molecule of claim 5, and a pharmaceutically acceptable carrier or diluent. ### Claim 8 (depends on 1) The antigen-binding molecule of claim 1, wherein the HCVR comprises the amino acid sequence of SEQ ID NO: 1050, and the LCVR comprises the amino acid sequence of SEQ ID NO: 1234. ### Claim 9 (depends on 8) The antigen-binding molecule of claim 8 that is an antibody or antigen-binding fragment thereof. ### Claim 10 (depends on 8) A pharmaceutical composition comprising the antigen-binding molecule of claim 8, and a pharmaceutically acceptable carrier or diluent. ### Claim 11 (depends on 8) The antigen-binding molecule of claim 8, wherein the antigen-binding molecule comprises a scFv comprising the HCVR and the LCVR. ### Claim 12 (depends on 1) The antigen-binding molecule of claim 1 that is an antibody or antigen-binding fragment thereof. ### Claim 13 (depends on 1) A pharmaceutical composition comprising the antigen-binding molecule of claim 1, and a pharmaceutically acceptable carrier or diluent. ### Claim 14 (depends on 1) The antigen-binding molecule of claim 1, wherein the antigen-binding molecule comprises a single chain variable fragment (scFv) comprising the HCVR and the LCVR. ### Claim 15 (depends on 14) A pharmaceutical composition comprising the antigen-binding molecule of claim 14, and a pharmaceutically acceptable carrier or diluent. ### Claim 16 (depends on 1) A method of treating cancer in a subject in need thereof, the method comprising administering the antigen-binding molecule of claim 1 to the subject. ### Claim 17 A pair of nucleic acid molecules comprising: a first nucleic acid molecule encoding a heavy chain variable region (HCVR) comprising three heavy chain complementarity determining regions, HCDR1, HCDR2, and HCDR3, comprising the amino acid sequences of SEQ ID NOs: 1052, 1054 and 1056, respectively; and a second nucleic acid molecule encoding a light chain variable region (LCVR) comprising three light chain complementarity determining regions, LCDR1, LCDR2 and LCDR3, comprising the amino acid sequences of SEQ ID NO: 1236, AAS and SEQ ID NO: 1240, respectively. ### Claim 18 (depends on 17) The pair of nucleic acid molecules of claim 17, wherein the HCVR comprises the amino acid sequence of SEQ ID NO: 1050, and the LCVR comprises the amino acid sequence of SEQ ID NO: 1234. ### Claim 19 (depends on 17) An isolated host cell comprising the pair of nucleic acid molecules of claim 17. ### Claim 20 A method of producing an antigen-binding molecule that binds human CD3, the method comprising: (a) culturing a host cell comprising a first nucleic acid molecule encoding a heavy chain variable region (HCVR) comprising three heavy chain complementarity determining regions, HCDR1, HCDR2, and HCDR3, comprising the amino acid sequences of SEQ ID NOs: 1052, 1054 and 1056, respectively, and a second nucleic acid molecule encoding a light chain variable region (LCVR) comprising three light chain complementarity determining regions, LCDR1, LCDR2 and LCDR3, comprising the amino acid sequences of SEQ ID NO: 1236, AAS and SEQ ID NO: 1240, respectively, under conditions permitting production of the antigen-binding molecule; and (b) recovering the antigen-binding molecule so produced.