# US 7,744,874 B2 · Anti-sclerostin antibodies > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,744,874 B2 - Document ID: US7744874B2 - Status: Granted - Kind: B2 - Application number: 12/160,472 - Filed: 2008-03-11 - Published: 2009-03-05 - Granted: 2010-06-29 - Earliest claimed: 2008-03-11 - Assignees: Eli Lilly and Company - Inventors: Andrew Ihor Korytko; David Matthew Marquis; Eric Michael Smith; Barbara Anne Swanson - Web page: https://patentgrep.com/patent/US7744874B2 ## CPC - C07K 16/22: against growth factors {; against growth regulators} - A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis - A61P 19/00: Drugs for skeletal disorders - A61P 19/02: for joint disorders, e.g. arthritis, arthrosis - A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease - A61P 19/10: for osteoporosis - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 35/00: Antineoplastic agents - A61P 37/00: Drugs for immunological or allergic disorders - A61K 2039/505: {comprising antibodies} - C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered - 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) - 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) ## Abstract Humanized and chimeric antibodies are provided that specifically bind human sclerostin and are characterized as having high affinity and strong neutralizing properties. The antibodies of the invention are useful for increasing bone mass, bone mineral density and bone strength and for the treatment of various disorders, e.g., osteoporosis, in human subject. ## Claims ### Claim 1 An antibody, or antigen-binding portion thereof, that specifically binds human sclerostin, and comprises a heavy chain variable region and a light chain variable region, wherein: i) the heavy chain variable region has the amino acid sequence of SEQ ID NO: 14 and the light chain variable region has the amino acid sequence of SEQ ID NO: 17; ii) the heavy chain variable region has the amino acid sequence of SEQ ID NO: 15 and the light chain variable region has the amino acid sequence of SEQ ID NO: 18. ### Claim 2 An antibody that specifically binds human sclerostin, and comprises a heavy chain polypeptide and a light chain polypeptide wherein: i) the heavy chain polypeptide has the amino acid sequence of SEQ ID NO: 2 and the light chain polypeptide has the amino acid sequence of SEQ ID NO: 5; ii) the heavy chain polypeptide has the amino acid sequence of SEQ ID NO: 3 and the light chain polypeptide has the amino acid sequence of SEQ ID NO: 6. ### Claim 3 An antibody that specifically binds human sclerostin, and comprises a heavy chain polypeptide with the amino acid sequence of SEQ ID NO: 3 and a light chain polypeptide with the amino acid sequence of SEQ ID NO: 6. ### Claim 4 (depends on 1) The antibody of claim 1, wherein said antibody comprises a heavy chain constant region selected from the group consisting of the heavy chain constant region of human IgG1, IgG2, IgG3, IgG4, and a polypeptide with the amino acid sequence of SEQ ID NO: 38. ### Claim 5 (depends on 1) A method of increasing at least one of bone mass, bone mineral density, bone mineral content, or bone strength in a human subject in need thereof, comprising administering to said human subject an effective amount of an antibody or antigen-binding portion thereof of claim 1. ### Claim 6 A method of treating osteoporosis in a human subject in need thereof, comprising administering to said human subject an effective amount of an antibody comprising a heavy chain polypeptide with SEQ ID NO: 3, and a light chain polypeptide with SEQ ID NO: 6. ### Claim 7 (depends on 1) A pharmaceutical composition comprising the antibody or antigen-binding portion thereof of claim 1, and a pharmaceutically acceptable carrier, diluent, or excipient. ### Claim 8 (depends on 1) The antigen-binding portion of claim 1, which is a member selected from the group consisting of a Fab fragment, a Fab′ fragment, a F(ab′)2 fragment, and a single chain Fv fragment. ### Claim 9 A method of increasing at least one of bone mass, bone mineral density, bone mineral content, or bone strength in a human subject in need thereof, comprising administering to said human subject an effective amount of an antibody comprising two heavy chains and two light chains, wherein each heavy chain has the amino acid sequence of SEQ ID NO: 3 and each light chain has the amino acid sequence of SEQ ID NO: 6. ### Claim 10 A pharmaceutical composition, comprising an antibody comprising two heavy chains and two light chains, wherein each heavy chain has the amino acid sequence of SEQ ID NO:3 and each light chain has the amino acid sequence of SEQ ID NO:6, and a pharmaceutically acceptable carrier, diluent, or excipient.