# US 2014/0193424 A1 · Method and medicament for inhibiting lymphangiogenesis > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0193424 A1 - Document ID: US20140193424A1 - Status: Published application - Kind: A1 - Application number: 13/962,111 - Filed: 2013-08-08 - Published: 2014-07-10 - Earliest claimed: 2012-08-09 - Applicants: Beijing Protgen Ltd.; Tsinghua University - Inventors: Yongzhang LUO; Wei ZHUO; Lin JIA; Yan FU; Guodong CHANG - Web page: https://patentgrep.com/patent/US20140193424A1 ## CPC - C07K 16/22: against growth factors {; against growth regulators} - A61K 38/179: {for growth factors; for growth regulators} - 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 35/04: specific for metastasis - A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection - C07K 16/2863: {against receptors for growth factors, growth regulators} - C07K 16/2866: {against receptors for cytokines, lymphokines, interferons} - A61K 2039/505: {comprising antibodies} - A61K 2039/507: {Comprising a combination of two or more separate antibodies} - C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding - 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 The present invention provides a method for inhibiting lymphangiogenesis in a subject, comprising administering a therapeutically effective amount of a CXCR4 inhibitor and/or a CXCL12 inhibitor to the subject. The invention further provides a method for inhibiting tumor lymphatic metastasis in a cancer patient, comprising administering to the subject (a) a therapeutically effective amount of a CXCR4 inhibitor and/or a CXCL12 inhibitor, in combination with (b) a therapeutically effective amount of a VEGF-C inhibitor and/or a VEGF-D inhibitor and/or a VEGFR-3 inhibitor. ## Claims ### Claim 1 Use of a CXCR4 inhibitor and/or a CXCL12 inhibitor in the manufacture of a preparation for inhibiting lymphangiogenesis in a subject. ### Claim 2 (depends on 1) The use according to claim 1, wherein said CXCR4 inhibitor is selected from the group consisting of an anti-CXCR4 antibody or an active fragment thereof, and CXCR4 antagonist AMD3100; and said CXCL12 inhibitor is selected from the group consisting of an anti-CXCL12 antibody, a CXCL12 antagonist, and a soluble CXCR4 fragment which competitively binds to CXCL12. ### Claim 3 (depends on 1, 2) The use according to claim 1 or 2, wherein said subject suffers from a cancer, inflammation and/or transplant rejection. ### Claim 4 Use of a CXCR4 inhibitor and/or a CXCL12 inhibitor in the preparation of a medicament for inhibiting tumor lymphatic metastasis in a cancer patient. ### Claim 5 (depends on 4) The use according to claim 4, wherein said CXCR4 inhibitor is selected from the group consisting of an anti-CXCR4 antibody or an active fragment thereof, and CXCR4 antagonist AMD3100; and said CXCL12 inhibitor is selected from the group consisting of an anti-CXCL12 antibody, a CXCL12 antagonist, and a soluble CXCR4 fragment which competitively binds to CXCL12. ### Claim 6 Use of (a) a CXCR4 inhibitor and/or a CXCL12 inhibitor, and (b) a VEGF-C inhibitor and/or a VEGF-D inhibitor and/or a VEGFR-3 inhibitor, in the preparation of a medicament for inhibiting tumor lymphatic metastasis in a cancer patient. ### Claim 7 (depends on 6) The use according to claim 6, wherein said CXCR4 inhibitor is selected from the group consisting of an anti-CXCR4 antibody or an active fragment thereof, and CXCR4 antagonist AMD3100; said CXCL12 inhibitor is selected from the group consisting of an anti-CXCL12 antibody, a CXCL12 antagonist, and a soluble CXCR4 fragment which competitively binds to CXCL12; said VEGF-C inhibitor is selected from the group consisting of an anti-VEGF-C antibody, a VEGF-C antagonist, and a soluble fragment of VEGFR-3 or VEGFR-2 which competitively binds to VEGF-C; said VEGF-D inhibitor is selected from the group consisting of an anti-VEGF-D antibody, a VEGF-D antagonist, and a soluble fragment of VEGFR-3 or VEGFR-2 which competitively binds to VEGF-D; and said VEGFR-3 inhibitor is selected from the group consisting of an anti-VEGFR-3 antibody and an antagonist which inhibits the activity of VEGFR-3 tyrosine kinase. ### Claim 8 A pharmaceutical composition for inhibiting tumor lymphatic metastasis in a cancer patient, comprising: (a) a CXCR4 inhibitor and/or a CXCL12 inhibitor, and (b) a VEGF-C inhibitor and/or a VEGF-D inhibitor and/or a VEGFR-3 inhibitor, as active ingredients; and optionally a pharmaceutically acceptable carrier. ### Claim 9 A kit for inhibiting tumor lymphatic metastasis in a cancer patient, comprising: (a) a CXCR4 inhibitor and/or a CXCL12 inhibitor; and (b) a VEGF-C inhibitor and/or a VEGF-D inhibitor and/or a VEGFR-3 inhibitor.