US2006178331A1PendingUtilityA1

Antisense oligonucleotides targeting folate receptor alpha, and the use thereof

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Individually held — no corporate assignee on recordPriority: Mar 9, 2001Filed: Jan 10, 2006Published: Aug 10, 2006
Est. expiryMar 9, 2021(expired)· nominal 20-yr term from priority
Inventors:Mona JhaveriPatrick ElwoodKoong-Nah Chung
C12N 2310/111C12N 15/1138A61K 38/00C12N 2310/121C12N 2310/315C12N 2310/12
36
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Claims

Abstract

The invention relates to treatment of cancers and cancerous cells which over-express α folate receptor (FRα) compared to the normal cells of the same tissue. The invention is directed to antisense oligonucleotides which are complimentary to the coding region of FRα, as well as the pharmaceutical compositions made thereof, and the methods of using the same for treatment of cancers, e.g. cancers of ovary, cervix, uterus, and brain.

Claims

exact text as granted — not AI-modified
1 . An antisense oligonucleotide complementary to a region of the open reading frame of αhFR as shown in  FIG. 9 .  
     
     
         2 . The antisense oligonucleotide of  claim 1  which is 10-50 nucleotides long.  
     
     
         3 . The antisense oligonucleotide of  claim 1  which is a 21-mer.  
     
     
         4 . The antisense oligonucleotide of  claim 3  which is AS1 (Sequence ID No. 2).  
     
     
         5 . The antisense oligonucleotide of  claim 3  which is AS2 (Sequence ID No. 3).  
     
     
         6 . The antisense oligonucleotide of  claim 3  which is AS6 (Sequence ID No. 4).  
     
     
         7 . An oligonucleotide which is a structural derivative of any one of oligonucleotides claimed in claims  1 - 6 .  
     
     
         8 . The oligonucleotide of  claim 7 , wherein the internucleotide linkages are phosphodiesters.  
     
     
         9 . The oligonucleotide of  claim 7 , wherein the internucleotide linkages are phosphorothioate phosphodiesters.  
     
     
         10 . A pharmaceutical composition comprising at least one antisense oligonucleotide of  claim 1  and a pharmaceutically acceptable carrier.  
     
     
         11 . The pharmaceutical composition of  claim 10  comprising two antisense oligonucleotides which are complementary to adjacent regions in the open reading frame of αhFR as shown in  FIG. 9 , and a pharmaceutically acceptable carrier.  
     
     
         12 . A method for inhibiting growth of cancer cells susceptible to growth inhibition comprising administering to said cells an effective amount of at least one antisense oligonucleotide which is complementary to a region of the open reading frame of αhFR as shown in  FIG. 9 .  
     
     
         13 . The method of  claim 12 , wherein said cancer cells, compared to normal cells of the same tissue, over-express FRα.  
     
     
         14 . The method of  claim 12 , wherein said cancer is selected from the group consisting of cancers of ovary, cervix, uterus, and brain.  
     
     
         15 . The method of  claim 12 , wherein said antisense oligonucleotide is 10-50 nucleotides long.  
     
     
         16 . The method of  claim 12 , wherein said antisense oligonucleotide is a 21-mer.  
     
     
         17 . The method of  claim 12 , wherein said antisense oligonucleotide is AS1 (Sequence ID No. 2).  
     
     
         18 . The method of  claim 12 , wherein said antisense oligonucleotide is AS2 (Sequence ID No. 3).  
     
     
         19 . The method of  claim 12 , wherein said antisense oligonucleotide is AS6 (Sequence ID No. 4).  
     
     
         20 . The method of claims  15 - 19 , wherein said antisense oligonucleotide has at least one internucleotide linkage that is a phosphodiester.  
     
     
         21 . The method of claims  15 - 19 , wherein said antisense oligonucleotide has at least one internucleotide linkage that is a phosphorothioate phosphodiester.  
     
     
         22 . A ribozyme containing the antisense oligonucleotide of  claim 1 .  
     
     
         23 . The ribozyme of  claim 22 , wherein said ribozyme is a hammerhead ribozyme.  
     
     
         24 . A multimeric ribozyme comprising two or more ribozymes as claimed in  claim 22 .  
     
     
         25 . A pharmaceutical composition comprising the ribozyme of any one of claims  22 - 24  and a pharmaceutically acceptable carrier.  
     
     
         26 . A method for inhibiting growth of cancer cells susceptible to growth inhibition comprising administering to said cells an effective amount of the ribozymes claimed in any one of claims  22 - 24 .  
     
     
         27 . The method as claimed in  claim 26 , wherein said cancer is selected from the group consisting of cancers of ovary, cervix, uterus, and brain.  
     
     
         28 . The pharmaceutical composition as claimed in  claim 24 , further comprising magnesium.  
     
     
         29 . The method as claimed in  claim 26 , further comprising co-administration of magnesium.  
     
     
         30 . A vector containing the antisense oligonucleotide of  claim 1.

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