# US 12,599,645 B2 · Antibodies which bind to lysophosphatidic acid receptor 1 (LPAR1) > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,599,645 B2 - Document ID: US12599645B2 - Status: Granted - Kind: B2 - Application number: 17/902,449 - Filed: 2022-09-02 - Published: 2023-06-15 - Granted: 2026-04-14 - Earliest claimed: 2021-09-02 - Assignees: DJS Antibodies Ltd - Applicants: Djs Antibodies Ltd - Inventors: Joseph Illingworth; David Llewellyn; Megan Ingham; Michael Steward - Web page: https://patentgrep.com/patent/US12599645B2 ## CPC - A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) - C07K 16/28: against receptors, cell surface antigens or cell surface determinants - A61P 19/02: for joint disorders, e.g. arthritis, arthrosis - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)} - A61K 2039/505: {comprising antibodies} - C07K 2317/565: Complementarity determining region [CDR] - C07K 2317/75: Agonist effect on antigen - 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 - 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) - 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 ## Abstract There is provided inter alia polypeptides such as antibodies or fragments thereof which bind to LPAR1. ## Claims ### Claim 1 An antibody which binds to Lysophosphatidic Acid Receptor 1 (“LPAR1”), wherein the antibody is an inhibitor of LPAR1, wherein the antibody comprises three heavy chain CDRs (HCDR1-3) and three light chain CDRs (LCDR1-3), wherein the antibody comprises a HCDR1 comprising the amino acid sequence set forth in SEQ ID NO: 1, a HCDR2 comprising the amino acid sequence set forth in SEQ ID NO: 100, a HCDR3 comprising the amino acid sequence set forth in SEQ ID NO: 101, a LCDR1 comprising the amino acid sequence set forth in SEQ ID NO: 4, a LCDR2 comprising the amino acid sequence set forth in SEQ ID NO: 98 and a LCDR3 comprising the amino acid sequence set forth in SEQ ID NO: 6. ### Claim 2 (depends on 1) The antibody of claim 1, wherein the antibody comprises a heavy chain variable region comprising the amino acid sequence set forth in SEQ ID NO: 102 and a light chain variable region comprising the amino acid sequence set forth in SEQ ID NO: 99. ### Claim 3 (depends on 2) The antibody of claim 2, wherein the antibody comprises a heavy chain comprising the heavy chain variable region comprising the amino acid sequence set forth in SEQ ID NO: 102 and a heavy chain constant region comprising the amino acid sequence as set forth in SEQ ID NO: 1239, and a light chain comprising the light chain variable domain comprising the amino acid sequence set forth in SEQ ID NO: 99 and a light chain constant region comprising the amino acid sequence as set forth in SEQ ID NO: 57. ### Claim 4 (depends on 1) The antibody of claim 1, wherein the antibody is a full-length IgG1 antibody. ### Claim 5 (depends on 1) The antibody of claim 1, wherein the antibody comprises an Fc region that has been mutated to reduce effector function, extend half-life, alter ADCC or improve hinge stability. ### Claim 6 (depends on 1) A pharmaceutical composition comprising the antibody of claim 1, together with a pharmaceutically acceptable diluent or carrier. ### Claim 7 An antibody which binds to LPAR1, wherein the antibody comprises: a. two heavy chain polypeptides, wherein each of the heavy chain polypeptides comprises a heavy chain variable region comprising three heavy chain CDRs (HCDR1-3) wherein HCDR1 comprises the amino acid sequence set forth in SEQ ID NO: 1, HCDR2 comprises the amino acid sequence set forth in SEQ ID NO: 100, and HCDR3 comprises the amino acid sequence set forth in SEQ ID NO: 101; and b. two light chain polypeptides, wherein each of the light chain polypeptides comprises a light chain variable region comprising three light chain CDRs (LCDR1-3) wherein LCDR1 comprises the amino acid sequence set forth in SEQ ID NO: 4, LCDR2 comprises the amino acid sequence set forth in SEQ ID NO: 98, and LCDR3 comprises the amino acid sequence set forth in SEQ ID NO: 6; and wherein the antibody is an IgG1 antibody. ### Claim 8 An antibody which binds to LPAR1, wherein the antibody comprises a. two heavy chain polypeptides, each of the heavy chain polypeptides comprising a heavy chain variable region comprising the amino acid sequence set forth in SEQ ID NO: 102; and b. two light chain polypeptides, each of the light chain polypeptides comprising a light chain variable domain comprising the amino acid sequence set forth in SEQ ID NO: 99; and wherein the antibody is an IgG1 antibody. ### Claim 9 An antibody which binds to LPAR1, wherein the antibody comprises two heavy chain polypeptides and two light chain polypeptides, wherein each of the heavy chain polypeptides comprises the amino acid sequence set forth in SEQ ID NO: 1220 and each of the light chain polypeptides comprises the amino acid sequence set forth in SEQ ID NO: 1219, provided that the residue corresponding to position 255 of SEQ ID NO: 1220 is “Y”, the residue corresponding to position 257 of SEQ ID NO: 1220 is “T” and the residue corresponding to position 259 of SEQ ID NO: 1220 is “E”.