US2006147446A1PendingUtilityA1

Humanized antibodies to human GP39, compositions, and therapeutic uses thereof

59
Assignee: BLACK AMELIAPriority: Nov 7, 1995Filed: Mar 9, 2006Published: Jul 6, 2006
Est. expiryNov 7, 2015(expired)· nominal 20-yr term from priority
A61P 37/08A61P 37/00A61P 3/10A61P 35/02A61P 37/04A61P 35/00A61P 29/00A61P 3/00A61P 27/00C07K 2317/92A61P 11/00C07K 2317/24G01N 2800/24A61P 17/00C07K 2317/56C07K 2317/73G01N 2333/70578A61K 2039/505A61P 1/00A61K 38/00A61P 11/06A61P 1/04C07K 16/467C07K 16/2875C07K 2317/76A61P 17/06A61K 39/395C07K 16/46C07K 16/00C07K 16/28
59
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Claims

Abstract

The present invention is directed to humanized antibodies which bind human gp39 and their use as therapeutic agents. These humanized antibodies are especially useful for treatment of autoimmune diseases.

Claims

exact text as granted — not AI-modified
1 . A humanized antibody which is capable of competing with the murine 24-31 antibody for inhibiting CD40 binding to gp39.  
     
     
         2 . The antibody of  claim 1  which contains the complementarity determining regions of the 24-31 antibody as set forth in  FIGS. 4-8  or variants and equivalents which contain one or more conservative amino acid substitutions.  
     
     
         3 . A humanized antibody derived from murine monoclonal antibody 24-31.  
     
     
         4 - 6 . (canceled)  
     
     
         7 . The humanized antibody of  claim 1 , wherein said antibody contains a humanized variable light sequence selected from the following group.  
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   (1) 
                   DIVMTQSPSFLSASVGDRVTITC KASQNVITAVA WYQQK 
                     
                 
                     
                     
                   PGKSPKLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSL 
                 
                     
                     
                   QPEDFADYFC QQYNSYPYT FGGGTKLEIK; 
                 
                     
                     
                 
                     
                   (2) 
                   DIVMTQSPDSLAVSLGERATINC KASQNVITAVA WYQQK 
                 
                     
                     
                   PGQSPKLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSL 
                 
                     
                     
                   QAEDVADYFC QQYNSYPYT FGGGTKLEIK; 
                 
                     
                     
                 
                     
                   (3) 
                   DIVMTQSPSFMSTSVGDRVTITC KASQNVITAVA WYQQK 
                 
                     
                     
                   PGKSPKLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSM 
                 
                     
                     
                   QPEDFADYFC QQYNSYPYT FGGGTKLEIK; 
                 
                     
                     
                 
                     
                   (4) 
                   DIVMTQSPDSMATSLGERVTINC KASQNVITAVA WYQQK 
                 
                     
                     
                   PGQSPKLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSM 
                 
                     
                     
                   QAEDVADYFC QQYNSYPYT FGGGTKLEIK, 
                 
                     
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and variants and equivalents thereof which contain one or more conservative amino acid substitutions which do not substantially affect the ability of the resultant humanized antibody to bind the gp39 antigen.  
     
     
         8 . The humanized antibody of  claim 1 , wherein said antibody contains a humanized variable heavy sequence selected from the group consisting of:  
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   (1) 
                   EVQLQESGPGLVKPSETLSLTCTVSGDSIT NGFWI 
                     
                 
                     
                     
                   WIRKPPGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSK 
                 
                     
                     
                   NQFSLKLSSVTAADTGVYYCAC RSYGRTPYYFDF WGQGTT 
                 
                     
                     
                   LTVSS; 
                 
                     
                     
                 
                     
                   (2) 
                   EVQLQESGPGLVKPSQTLSLTCTVSGDSIT NGFWI WIRKH 
                 
                     
                     
                   PGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSKNQFSL 
                 
                     
                     
                   KLSSVTAADTGVYYCAC RSYGRTPYYFDF 
                 
                     
                     
                   WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (3) 
                   EVQLQESGPGLVKPSQTLSLTCAVSGDSIT NGFWI WIRKH 
                 
                     
                     
                   PGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSNNQFSL 
                 
                     
                     
                   NLNSVTRADTGVYYCAC RSYGRTPYYFDF 
                 
                     
                     
                   WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (4) 
                   EVQLQESGPGLVKPSETLSLTCAVYGDSIT NGFWI WIRKP 
                 
                     
                     
                   PGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSKNQFYL 
                 
                     
                     
                   KLSSVTAADTGVYYCAC RSYGRTPYYFDF 
                 
                     
                     
                   WGQGTTLTVSS. 
                 
                     
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and variants and equivalents thereof which contain one or more conservative amino acid substitutions which do not substantially affect the ability of the resultant humanized antibody to bind the gp39 antigen.  
     
     
         9 . The humanized antibody of  claim 1 , which contains a humanized variable light sequence selected from the group consisting of the following group:  
       
         
           
                 
                 
                 
               
                     
                 
                   (1) 
                   DIVMTQSPSFLSASVGDRVTITC KASQNVITAVA WYQQKPGKSP 
                     
                 
                     
                   KLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSLQPEDFADYFC 
                 
                     
                   QQYNSYPYT FGGGTKLEIK; 
                 
                     
                 
                   (2) 
                   DIVMTQSPDSLAVSLGERATINC KASQNVITAVA WYQQKPGQSP 
                 
                     
                   KLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSLQAEDVADYFC 
                 
                     
                   QQYNSYPYT FGGGTKLEIK; 
                 
                     
                 
                   (3) 
                   DIVMTQSPSFMSTSVGDRVTITC KASQNVITAVA WYQQKPGKSP 
                 
                     
                   KLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSMQPEDFADYFC 
                 
                     
                   QQYNSYPYT FGGGTKLEIK;. 
                 
                     
                 
                   (4) 
                   DIVMTQSPDSMATSLGERVTINC KASQNVITAVA WYQQKPGQSP 
                 
                     
                   KLLIY SASNRYT GVPDRFSGSGSGTDFTLTISSMQAEDVADYFC 
                 
                     
                   QQYNSYPYT FGGGTKLEIK 
                 
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and a humanized variable heavy sequence selected from the following group:  
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   (1) 
                   EVQLQESGPGLVKPSETLSLTCTVSGDSIT NGFWI WIRKP 
                     
                 
                     
                     
                   PGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSKNQFSL 
                 
                     
                     
                   KLSSVTAADTGVYYCAC RSYGRTPYYFDF 
                 
                     
                     
                   WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (2) 
                   EVQLQESGPGLVKPSQTLSLTCTVSGDSIT NGFWI WIRKH 
                 
                     
                     
                   PGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSKNQFSL 
                 
                     
                     
                   KLSSVTAADTGVYYCAC RSYGRTPYYFDF 
                 
                     
                     
                   WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (3) 
                   EVQLQESGPGLVKPSQTLSLTCAVSGDSIT NGFWI WIRKH 
                 
                     
                     
                   PGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSNNQFSL 
                 
                     
                     
                   NLNSVTRADTGVYYCAC RSYGRTPYYFDF 
                 
                     
                     
                   WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (4) 
                   EVQLQESGPGLVKPSETLSLTCAVYGDSIT NGFWI WIRKP 
                 
                     
                     
                   PGNKLEYMG YISYSGSTYYNPSLKS RISISRDTSKNQFYL 
                 
                     
                     
                   KLSSVTAADTGVYYCAC RSYGRTPYYFDF 
                 
                     
                     
                   WGQGTTLTVSS, 
                 
                     
                     
                   and 
                 
                     
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and variants and equivalents thereof which contain one or more conservative amino acid substitutions which do not substantially affect the ability of the resultant humanized antibody to bind the gp39 antigen.  
     
     
         10 . The humanized antibody of  claim 9 , which contains humanized variable light sequence (I) and humanized variable heavy sequence (1).  
     
     
         11 . The humanized antibody of  claim 9 , which contains humanized variable light sequence (2) and humanized variable heavy sequence (1).  
     
     
         12 - 13 . (canceled)  
     
     
         14 . The humanized antibody of  claim 1 , which contains the human kappa or lambda light chain constant region and either the human gamma 1 or gamma 4 heavy chain constant region.  
     
     
         15 - 16 . (canceled)  
     
     
         17 . A pharmaceutical composition which contains a humanized antibody derived from murine monoclonal antibody 24-31.  
     
     
         18 . The pharmaceutical composition of  claim 17 , wherein said humanized antibody contains a humanized variable light sequence selected from the following group:  
       
         
           
                 
                 
                 
               
                     
                 
                   (1) 
                   DIVMTQSPSFLSASVGDRVTITC KASQNVITAVA WYQQKPGKSPK 
                     
                 
                     
                   LLIY SASNRYT GVPDRFSGSGSGTDFTLTISSLQPEDFADYFC Q 
                 
                     
                   QYNSYPYT FGGGTKLEIK; 
                 
                     
                 
                   (2) 
                   DIVMTQSPDSLAVSLGERATINC KASQNVITAVA WYQQKPGQSPK 
                 
                     
                   LLIY SASNRYT GVPDRFSGSGSGTDFTLTISSLQAEDVADYFC Q 
                 
                     
                   QYNSYPYT FGGGTKLEIK; 
                 
                     
                 
                   (3) 
                   DIVMTQSPSFMSTSVGDRVTITC KASQNVITAVA WYQQKPGKSPK 
                 
                     
                   LLIY SASNRYT GVPDRFSGSGSGTDFTLTISSMQPEDFADYFC Q 
                 
                     
                   QYNSYPYT FGGGTKLEIK; 
                 
                     
                 
                   (4) 
                   DIVMTQSPDSMATSLGERVTINC KASQNVITAVA WYQQKPGQSPK 
                 
                     
                   LLIY SASNRYT GVPDRFSGSGSGTDFTLTISSMQAEDVADYFC Q 
                 
                     
                   QYNSYPYT FGGGTKLEIK. 
                 
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and variants and equivalents thereof which contain one or more conservative amino acid substitutions which do not substantially affect the ability of the resultant humanized antibody to bind the gp39 antigen.  
     
     
         19 . The pharmaceutical composition of  claim 18 , wherein said humanized antibody contains a humanized variable heavy sequence selected from the following group:  
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   (1) 
                   EVQLQESGPGLVKPSETLSLTCTVSGDSIT NGFWI 
                     
                 
                     
                     
                   WIRKPPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSKNQFSLKLSSVTAADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (2) 
                   EVQLQESGPGLVKPSQTLSLTCTVSGDSIT NGFWI 
                 
                     
                     
                   WIRKHPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSKNQFSLKLSSVTAADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTITLTVSS; 
                 
                     
                     
                 
                     
                   (3) 
                   EVQLQESGPGLVKPSQTLSLTCAVSGDSIT NGFWI 
                 
                     
                     
                   WIRKHPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSNNQFSLNLNSVTRADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (4) 
                   EVQLQESGPGLVKPSETLSLTCAVYGDSIT NGFWI 
                 
                     
                     
                   WIRKPPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSKNQFYLKLSSVTAADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTTLTVSS, 
                 
                     
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and variants and equivalents thereof which contain one or more conservative amino acid substitutions which do not substantially affect the ability of the resultant humanized antibody to bind the gp39 antigen.  
     
     
         20 . The pharmaceutical composition of  claim 17 , wherein said humanized antibody contains a humanized variable light sequence selected from the following group:  
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   (1) 
                   DIVMTQSPSFLSASVGDRVTITC KASQNVITAVA 
                     
                 
                     
                     
                   WYQQKPGKSPKLLIY SASNRYT 
                 
                     
                     
                   GVPDRFSGSGSGTDFTLTISSLQPEDFADYFC QQYNSYPYT 
                 
                     
                     
                   FGGGTKLEIK; 
                 
                     
                     
                 
                     
                   (2) 
                   DIVMTQSPDSLAVSLGERATINC KASQNVITAVA 
                 
                     
                     
                   WYQQKPGQSPKLLIY SASNRYT 
                 
                     
                     
                   GVPDRFSGSGSGTDFTLTISSLQAEDVADYFC QQYNSYPYT 
                 
                     
                     
                   FGGGTKLEIK; 
                 
                     
                     
                 
                     
                   (3) 
                   DIVMTQSPSFMSTSVGDRVTITC KASQNVITAVA 
                 
                     
                     
                   WYQQKPGKSPKLLIY SASNRYT 
                 
                     
                     
                   GVPDRFSGSGSGTDFTLTISSMQPEDFADYFC QQYNSYPYT 
                 
                     
                     
                   FGGGTKLEIK; 
                 
                     
                     
                 
                     
                   (4) 
                   DIVMTQSPDSMATSLGERVTINC KASQNVITAVA 
                 
                     
                     
                   WYQQKPGQSPKLLIY SASNRYT 
                 
                     
                     
                   GVPDRFSGSGSGTDFTLTISSMQAEDVADYFC QQYNSYPYT 
                 
                     
                     
                   FGGGTKLEIK 
                 
                     
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and a humanized variable heavy sequence selected from the following group:  
       
         
           
                 
                 
                 
                 
               
                     
                     
                 
                     
                   (1) 
                   EVQLQESGPGLVKPSETLSLTCTVSGDSIT NGFWI 
                     
                 
                     
                     
                   WIRKPPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSKNQFSLKLSSVTAADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (2) 
                   EVQLQESGPGLVKPSQTLSLTCTVSGDSIT NGFWI 
                 
                     
                     
                   WIRKHPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSKNQFSLKLSSVTAADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (3) 
                   EVQLQESGPGLVKPSQTLSLTCAVSGDSIT NGFWI 
                 
                     
                     
                   WIRKHPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSNNQFSLNLNSVTRADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTTLTVSS; 
                 
                     
                     
                 
                     
                   (4) 
                   EVQLQESGPGLVKPSETLSLTCAVYGDSIT NGFWI 
                 
                     
                     
                   WLRKPPGNKLEYMG YISYSGSTYYNPSLKS 
                 
                     
                     
                   RISISRDTSKNQFYLKLSSVTAADTGVYYCAC 
                 
                     
                     
                   RSYGRTPYYFDF WGQGTTLTVSS, 
                 
                     
                     
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       and variants and equivalents thereof which contain one or more conservative amino acid substitutions which do not substantially affect the ability of the resultant humanized antibody to bind the gp39 antigen.  
     
     
         21 . The pharmaceutical composition of  claim 20 , wherein the humanized antibody contains humanized variable light sequence (1) and humanized variable heavy sequence (1).  
     
     
         22 . The pharmaceutical composition of  claim 20 , wherein the antibody contains humanized variable light sequence (2) and humanized variable heavy sequence (1).  
     
     
         23 - 24 . (canceled)  
     
     
         25 . A method of treatment of a disease treatable by modulating gp39 expression or inhibiting the gp39/CD40 interaction which comprises administering a therapeutically effective amount of a humanized antibody according to  claim 1 .  
     
     
         26 . The method of  claim 25 , wherein said disease is an autoimmune disorder.  
     
     
         27 . The method of  claim 26 , wherein said autoimmune disorder is selected from the group consisting of rheumatoid arthritis, psoriasis, multiple sclerosis, diabetes, systemic lupus erythematosus and ITP.  
     
     
         28 . The method of  claim 25 , wherein the disease is a non-autoimmune disorder.  
     
     
         29 . The method of  claim 26 , wherein the disease is graft-versus-host disease or graft rejection.

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