US2013184205A1PendingUtilityA1

Antitumor combinations containing a vegf-inhibiting agent and 5fu or a derivative thereof

Assignee: REGENERON PHARMAPriority: Dec 3, 2004Filed: Mar 4, 2013Published: Jul 18, 2013
Est. expiryDec 3, 2024(expired)· nominal 20-yr term from priority
A61P 43/00A61P 35/02A61P 35/00A61K 31/505A61K 31/513A61K 31/519A61K 38/18A61K 45/00A61K 38/179A61K 31/7068A61K 38/17A61K 31/525
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Claims

Abstract

This invention relates to antitumor combinations comprising a VEGF inhibitor combined with 5-fluorouracil or with a 5-fluoropyrimidine derivative that are therapeutically useful in the treatment of neoplastic diseases, and pharmaceutical compositions comprising such combinations.

Claims

exact text as granted — not AI-modified
What is clamed is: 
     
         1 . A pharmaceutical composition comprising a pharmaceutically effective amount of a VEGF inhibitor and a pharmaceutically effective amount of 5-fluorouracil, and a pharmaceutically acceptable excipient. 
     
     
         2 . A pharmaceutical composition comprising a pharmaceutically effective amount of a VEGF inhibitor and a pharmaceutically effective amount 5-fluoropyrimidine derivative, and a pharmaceutically acceptable excipient. 
     
     
         3 . A method of treating a neoplastic disease, in a patient in need of such treatment, comprising administering to such patient a pharmaceutically effective amount of a combination of a VEGF inhibitor and 5-fluorouracil, 
     
     
         4 . A method of treating a neoplastic disease, in a patient in need of such treatment, comprising administering to such patient a pharmaceutically effective amount of a combination of a VEGF inhibitor and a 5-fluoropyrimidine derivative. 
     
     
         5 . A pharmaceutical composition according to  claim 2  wherein the 5-fluoropyrimidine derivative is capecitabine or gemcitabine. 
     
     
         6 . A method according to  claim 4  wherein the 5-fluoropyrimidine derivative is capecitabine or gemcitabine. 
     
     
         7 . A method according to either of  claim 3  or  4 , wherein the VEGF inhibitor is VEGF-Trap. 
     
     
         8 . A pharmaceutical composition according to either of  claims 1  or  2  wherein the VEGF inhibitor is VEGF-Trap. 
     
     
         9 . A pharmaceutical composition according to  claim 5  wherein the VEGF inhibitor is VEGF-Trap. 
     
     
         10 . A method according to  claim 6  wherein the VEGF inhibitor is VEGF-Trap. 
     
     
         11 . A pharmaceutical composition according to either of  claim 1  or  2 , further comprising folinic acid. 
     
     
         12 . A method according to either of  claim 3  or  4 , further comprising administering a pharmaceutically effective amount of folinic acid. 
     
     
         13 . A method according to  claim 3  wherein the VEGF inhibitor and 5-fluorouracil are administered simultaneously. 
     
     
         14 . A method according to  claim 3  wherein the VEGF inhibitor and 5-flourouracil are administered separately. 
     
     
         15 . A method according to  claim 4  wherein the VEGF inhibitor and the 5-fluoropyrimidine inhibitor are administered simultaneously. 
     
     
         16 . A method according to  claim 4  wherein the VEGF inhibitor and the 5-fluoropyrimidine inhibitor are administered separately. 
     
     
         17 . A pharmaceutical composition according to  claim 1  wherein the VEGF inhibitor is VEGF-Trap, and wherein the VEGF-Trap is present in the amount of 2% to 80% by weight of the total weight of VEGF-Trap and 5-fluorouracil. 
     
     
         18 . A pharmaceutical composition according to  claim 2  wherein the VEGF inhibitor is VEGF-Trap, and wherein the VEGF-Trap is present in the amount of 2% to 80% by weight of the total weight of VEGF-Trap and the 5-fluoropyrimidine derivative. 
     
     
         19 . A method according to  claim 3  wherein the VEGF inhibitor is VEGF-Trap, and wherein the VEGF-Trap is administered in an amount of 2% to 80% by weight of the total weight of VEGF-Trap and 5-fluorouracil. 
     
     
         20 . A method according to  claim 4  wherein the VEGF inhibitor is VEGF-Trap, and wherein VEGF-Trap is administered in an amount of 2% to 80% by weight of the total weight of VEGF-Trap and the 5-fluoropyrimidine derivative. 
     
     
         21 . A pharmaceutical composition according to  claim 1 , further comprising folinic acid, provided that no other chemotoxic derivative is present, and which exhibits a therapeutically synergistic effect in the treatment of neoplastic disease. 
     
     
         22 . A pharmaceutical composition according to  claim 2 , further comprising folinic acid, provided that no other chemotoxic derivative is present, and which exhibits a therapeutically synergistic effect in the treatment of neoplastic disease. 
     
     
         23 . A method according to  claim 3 , further comprising administering a pharmaceutically effective amount of folinic acid, provided that no other chemotoxic derivative is administered, and wherein the amounts of the VEGF inhibitor, 5-fluorouracil and folinic acid administered exhibit a therapeutically synergistic effect in the treatment of the neoplastic disease. 
     
     
         24 . A method according to  claim 4 , further comprising administering a pharmaceutically effective amount of folinic acid, provided that no other chemotoxic derivative is administered, and wherein the amounts of the VEGF inhibitor, the 5-fluoropyrimidine derivative and folinic acid administered exhibit a therapeutically synergistic effect in the treatment of the neoplastic disease. 
     
     
         25 . Combinations containing a VEGF inhibitor with at least 5-fluorouracil or a 5-fluoropyrimidine derivative that is therapeutically useful in the treatment of neoplastic diseases. 
     
     
         26 . Combinations containing a VEGF inhibitor with 5-fluorouracil or capecitabine or gemcitabine. 
     
     
         27 . The combinations as claimed in  claim 26 , containing a VEGF inhibitor with fluorouracil. 
     
     
         28 . The combinations as claimed in  claim 27 , containing a VEGF-Trap inhibitor with 5-fluorouracil. 
     
     
         29 . The combinations as claimed in any one of  claims 25  to  28 , which also contain folinic acid. 
     
     
         30 . The combinations as claimed in one of  claims 25  to  28 , which contain from 2 to 80% by weight of VEGF-Trap. 
     
     
         31 . The combinations as claimed in  claim 25 , which also contain folinic acid, and which contain from 2 to 80% of VEGF-Trap. 
     
     
         32 . The combinations as claimed in  claim 26 , which also contain folinic acid, and which contain from 2 to 80% of VEGF-Trap. 
     
     
         33 . The combinations as claimed in  claim 27 , which also contain folinic acid, and which contain from 2 to 80% of VEGF-Trap. 
     
     
         34 . The combinations as claimed in  claim 28 , which also contain folinic acid, and which contain from 2 to 80% of VEGF-Trap. 
     
     
         35 . Products containing a VEGF inhibitor and at least one therapeutically useful substance as defined in one of  claims 25  to  28 , in the treatment of neoplastic diseases, as a combined preparation for simultaneous use, separate use or use spread out over time in anticancer therapy. 
     
     
         36 . Products containing a VEGF inhibitor and at least one therapeutically useful substance as defined  claim 25 , and which may contain folinic acid, in the treatment of neoplastic diseases, as a combined preparation for simultaneous use, separate use or use spread out over time in anticancer therapy. 
     
     
         37 . Products containing a VEGF inhibitor and at least one therapeutically useful substance as defined  claim 26 , and which may contain folinic acid, in the treatment of neoplastic diseases, as a combined preparation for simultaneous use, separate use or use spread out over time in anticancer therapy. 
     
     
         38 . Products containing a VEGF inhibitor and at least one therapeutically useful substance as defined  claim 27 , and which may contain folinic acid, in the treatment of neoplastic diseases, as a combined preparation for simultaneous use, separate use or use spread out over time in anticancer therapy. 
     
     
         39 . Products containing a VEGF inhibitor and at least one therapeutically useful substance as defined  claim 28 , and which may contain folinic acid, in the treatment of neoplastic diseases, as a combined preparation for simultaneous use, separate use or use spread out over time in anticancer therapy. 
     
     
         40 . Combinations containing a VEGF inhibitor with at least 5-flurorouracil or a 5-fluoropyrimidine derivative and folinic acid with the exclusion of any other chemotoxic derivative exhibiting a therapeutically synergistic effect in the treatment of neoplastic diseases.

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