US2021292410A1PendingUtilityA1

Treatment paradigm for an anti-cd19 antibody and venetoclax combination treatment

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Assignee: MORPHOSYS AGPriority: Dec 7, 2017Filed: May 30, 2018Published: Sep 23, 2021
Est. expiryDec 7, 2037(~11.4 yrs left)· nominal 20-yr term from priority
A61K 31/09C07D 249/04A61K 31/4192A61K 31/573A61K 2039/545A61P 35/00C07K 2317/565A61K 31/635C07K 16/2803
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Claims

Abstract

The instant invention describes pharmaceutical compositions and dosing regimens comprising seviteronel and/or dexamethasone, and methods of treating diseases, disorders or symptoms thereof.

Claims

exact text as granted — not AI-modified
1 : A combination comprising an anti-CD19 antibody and a BCL-2 inhibitor, for use in the treatment of a patient suffering from non-Hodgkin's lymphoma, chronic lymphocytic leukemia and/or small lymphocytic lymphoma, wherein said anti-CD19 antibody is administered at least 7 days prior to the first administration of said BCL-2 inhibitor. 
     
     
         2 : A combination according to  claim 1 , wherein the anti-CD19 antibody is administered weekly, bi-weekly or monthly after a first administration on Day 1 and wherein the BCL-2 inhibitor is administered for the first time on Day 8. 
     
     
         3 : A combination according to  claim 1 , wherein the anti-CD19 antibody after a first administration on Day 1 is administered weekly for the first 3 months. 
     
     
         4 : A combination according to  claim 3 , wherein the anti-CD19 antibody after a first administration on Day 1 is administered weekly for the first 3 months and bi-weekly for at least the next 3 months. 
     
     
         5 : A combination according to  claim 4 , wherein the anti-CD19 antibody after a first administration on Day 1 is administered weekly for the first 3 months, bi-weekly for the next 3 months and monthly thereafter. 
     
     
         6 : A combination according to  claim 2 , wherein there is an additional dosing of the anti-CD19 antibody on Day 4. 
     
     
         7 : A combination according to  claim 2 , wherein the BCL-2 inhibitor is administered for the first time on Day 8 with a starting dose of 20 mg followed by a weekly ramp-up dosing of 50 mg, 100 mg, 200 mg and 400 mg followed by a daily dosing of 400 mg. 
     
     
         8 . (canceled) 
     
     
         9 : A combination according to  claim 1 , wherein said BCL-2 inhibitor is venetoclax. 
     
     
         10 : A combination according to  claim 1 , wherein the anti-CD19 antibody comprises an HCDR1 region comprising sequence SYVMH (SEQ ID NO: 1), an HCDR2 region comprising sequence NPYNDG (SEQ ID NO: 2), an HCDR3 region comprising sequence GTYYYGTRVFDY (SEQ ID NO: 3), an LCDR1 region comprising sequence RSSKSLQNVNGNTYLY (SEQ ID NO: 4), an LCDR2 region comprising sequence RMSNLNS (SEQ ID NO: 5), and an LCDR3 region comprising sequence MQHLEYPIT (SEQ ID NO: 6) 
     
     
         11 : A combination according to  claim 9 , wherein the anti-CD19 antibody comprises a variable heavy chain comprising the sequence 
       
         
           
                 
               
                   (SEQ ID NO: 10) 
                 
                   EVQLVESGGGLVKPGGSLKLSCAASGYTFTSYVMHWVRQAPGKGLEWIGY 
                 
                     
                 
                   INPYNDGTKYNEKFQGRVTISSDKSISTAYMELSSLRSEDTAMYYCARGT 
                 
                     
                 
                   YYYGTRVFDYWGQGTLVTVSS 
                 
             
                
                
                
                
                
                
               
            
           
         
         and a variable light chain of the sequence 
       
       
         
           
                 
               
                   (SEQ ID NO: 11) 
                 
                   DIVMTQSPATLSLSPGERATLSCRSSKSLQNVNGNTYLYWFQQKPGQSPQ 
                 
                     
                 
                   LLIYRMSNLNSGVPDRFSGSGSGTEFTLTISSLEPEDFAVYYCMQHLEYP 
                 
                     
                 
                   ITFGAGTKLEIK. 
                 
             
                
                
                
                
                
                
               
            
           
         
       
     
     
         12 : A combination according to  claim 9 , wherein the anti-CD19 antibody comprises a heavy chain constant domain comprising the sequence 
       
         
           
                 
               
                   (SEQ ID NO: 12) 
                 
                   ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGV 
                 
                     
                 
                   HTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEP 
                 
                     
                 
                   KSCDKTHTCPPCPAPELLGGPDVFLFPPKPKDTLMISRTPEVTCVVVDVS 
                 
                     
                 
                   HEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGK 
                 
                     
                 
                   EYKCKVSNKALPAPEEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTC 
                 
                     
                 
                   LVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSKLTVDKSRW 
                 
                     
                 
                   QQGNVFSCSVMHEALHNHYTQKSLSLSPGK. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         13 : A combination according to  claim 10 , wherein the anti-CD19 antibody comprises a light chain constant domain comprising the sequence 
       
         
           
                 
               
                   (SEQ ID NO: 13) 
                 
                   RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSG 
                 
                     
                 
                   NSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTK 
                 
                     
                 
                   SFNRGEC. 
                 
             
                
                
                
                
                
                
               
            
           
         
       
     
     
         14 : A combination according to  claim 10 , wherein the anti-CD19 antibody is administered in a concentration of 12 mg/kg. 
     
     
         15 : A method for treatment of a subject with chronic lymphocytic leukemia, small lymphocytic lymphoma or non-Hodgkin's lymphoma, wherein the non-Hodgkin's lymphoma is selected from the group consisting of follicular lymphoma, small lymphocytic lymphoma, mucosa-associated lymphoid tissue, marginal zone, diffuse large B cell, Burkitt's, and mantle cell, said method comprising administering the subject the combination of  claim 1 . 
     
     
         16 : The method of  claim 15  wherein said anti-CD19 antibody and said BCL-2 inhibitor are administered separately. 
     
     
         17 : A combination according to  claim 10 , wherein the anti-CD19 antibody comprises a heavy chain constant domain comprising the sequence 
       
         
           
                 
               
                   (SEQ ID NO: 12) 
                 
                   ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGV 
                 
                     
                 
                   HTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEP 
                 
                     
                 
                   KSCDKTHTCPPCPAPELLGGPDVFLFPPKPKDTLMISRTPEVTCVVVDVS 
                 
                     
                 
                   HEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRVVSVLTVVHQDWLNGK 
                 
                     
                 
                   EYKCKVSNKALPAPEEKTISKTKGQPREPQVYTLPPSREEMTKNQVSLTC 
                 
                     
                 
                   LVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSKLTVDKSRW 
                 
                     
                 
                   QQGNVFSCSVMHEALHNHYTQKSLSLSPGK. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         18 : A combination according to  claim 11 , wherein the anti-CD19 antibody comprises a light chain constant domain comprising the sequence 
       
         
           
                 
               
                   (SEQ ID NO: 13) 
                 
                   RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSG 
                 
                     
                 
                   NSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTK 
                 
                     
                 
                   SFNRGEC. 
                 
             
                
                
                
                
                
                
               
            
           
         
       
     
     
         19 : A combination according to  claim 12 , wherein the anti-CD19 antibody comprises a light chain constant domain comprising the sequence 
       
         
           
                 
               
                   (SEQ ID NO: 13) 
                 
                   RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSG 
                 
                     
                 
                   NSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTK 
                 
                     
                 
                   SFNRGEC. 
                 
             
                
                
                
                
                
                
               
            
           
         
       
     
     
         20 : A combination according to  claim 11 , wherein the anti-CD19 antibody is administered in a concentration of 12 mg/kg. 
     
     
         21 : A combination according to  claim 12 , wherein the anti-CD19 antibody is administered in a concentration of 12 mg/kg.

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