US2013045200A1PendingUtilityA1

Methods of using anti-pd-l1 antibodies and their use to treat infection resulting from t-cell dysfunction

Assignee: GENENTECH INCPriority: Dec 9, 2008Filed: May 23, 2012Published: Feb 21, 2013
Est. expiryDec 9, 2028(~2.4 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 33/02A61P 37/04A61P 37/02A61P 37/00A61P 35/00A61P 31/04A61P 31/00A61P 31/10A61P 33/00A61P 31/12C07K 16/1145C07K 2317/71A61K 39/39558C07K 2317/74C07K 16/22A61K 31/7068C07K 16/2827C07K 2317/24C07K 16/30C07K 2317/56C07K 2317/52C07K 2317/73C07K 2317/14A61K 45/06C07K 2317/565A61K 2039/507A61K 39/3955C07K 16/3046A61K 2039/505C07K 2317/92C07K 16/28C07K 2317/567C07K 2317/76A61K 39/00Y02A50/30A61K 2300/00
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Claims

Abstract

The present application relates to methods of using anti-PD-L1 antibodies to enhance T-cell function to upregulate cell-mediated immune responses and for the treatment of T cell dysfunctional disorders, including infection (e.g., acute and chronic) and tumor immunity.

Claims

exact text as granted — not AI-modified
1 . A method of enhancing T-cell function comprising administering an effective amount of an anti-PD-L1 antibody or antigen binding fragment thereof, wherein the antibody or antibody fragment comprises a heavy chain and a light chain variable region sequence, wherein:
 (a) the heavy chain comprises an HVR-H1, HVR-H2 and HVR-H3, wherein further:   
       
         
           
                 
               
                   (SEQ ID NO: 1) 
                 
                 
                 
               
                   (i) 
                   the HVR-H1 sequence is GFTFSX 1 SWIH; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 2) 
                 
                 
                 
               
                   (ii) 
                   the HVR-H2 sequence is AWIX 2 PYGGSX 3 YYADSVKG; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 3) 
                 
                 
                 
               
                   (iii) 
                   the HVR-H3 sequence is RHWPGGFDY,; 
                 
                   and 
                     
                 
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
           
         
         (b) the light chain comprises an HVR-L1, HVR-L2 and HVR-L3, wherein further: 
       
       
         
           
                 
               
                   (SEQ ID NOs: 8) 
                 
                 
                 
               
                   (iv) 
                   the HVR-L1 sequence is RASQX 4 X 5 X 6 TX 7 X 8 A; 
                 
                     
                 
                 
               
                   (SEQ ID NOs: 9) 
                 
                 
                 
               
                   (v) 
                   the HVR-L2 sequence is SASX 9 LX 10 S; 
                 
                     
                 
                 
               
                   (SEQ ID NOs: 10) 
                 
                 
                 
               
                   (vi) 
                   the HVR-L3 sequence is QQX 11 X 12 X 13 X 14 PX 15 T; 
                 
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
               
            
           
         
         wherein: X 1  is D or G; X 2  is S or L; X 3  is T or S; X 4  may be D or V; X 5  may be V or I; X 6  may be S or N; X 7  may be A or F; X 8  may be V or L; X 9  may be F or T; X 10  may be Y or A; X 11  may be Y, G, F, or S; X 12  may be L, Y, F or W; X 13  may be Y, N, A, T, G, F or I; X 14  may be H, V, P, T or I; X 15  may be A, W, R, P or T. 
       
     
     
         2 . The method of  claim 1  wherein X 1  is D; X 2  is S and X 3  is T. 
     
     
         3 . The method of  claim 1 , wherein X 4 =D, X 5 =V, X 6 =S, X 7 =A and X 8 =V, X 9 =F, and X 10 =Y, X 11 =Y, X 12 =L, X 13 =Y, X 14 =H and X 15 =A. 
     
     
         4 . The method of  claim 1 , wherein X 1 =D, X 2 =S and X 3 =T, X 4 =D, X 5 =V, X 6 =S, X 7 =A and X 8 =V, X 9 =F, and X 10 =Y, X 11 =Y, X 12 =L, X 13 =Y, X 14 =H and X 15 =A. 
     
     
         5 . The method of  claim 4 , wherein the encoded variable region heavy chain framework sequences are juxtaposed between the HVRs according to the formula: (HC-FR1)-(HVR-H1)-(HC-FR2)-(HVR-H2)-(HC-FR3)-(HVR-H3)-(HC-FR4) and/or the encoded variable region light chain framework sequences juxtaposed between the HVRs according to the formula: (LC-FR1)-(HVR-L1)-(LC-FR2)-(HVR-L2)-(LC-FR3)-(HVR-L3)-(LC-FR4). 
     
     
         6 . The method of  claim 5 , wherein the framework sequences are human. 
     
     
         7 . The method of  claim 6  wherein the variable heavy chain framework sequences are VH subgroup III consensus framework. 
     
     
         8 . The method of  claim 6  wherein the variable region light chain framework sequences are VL kappa I consensus framework. 
     
     
         9 . The method of  claim 7  wherein one or more of the heavy chain framework sequences is the following: 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 4) 
                 
                     
                   HC-FR1 is EVQLVESGGGLVQPGGSLRLSCAAS; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 5) 
                 
                     
                   HC-FR2 is WVRQAPGKGLEWV; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 6) 
                 
                     
                   HC-FR3 is RFTISADTSKNTAYLQMNSLRAEDTAVYYCAR; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 7) 
                 
                     
                   HC-FR4 is WGQGTLVTVSA. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         10 . The method of  claim 8  wherein one or more of the light chain framework sequences is the following: 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 11) 
                 
                     
                   LC-FR1 is DIQMTQSPSSLSASVGDRVTITC; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 12) 
                 
                     
                   LC-FR2 is WYQQKPGKAPKLLIY; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 13) 
                 
                     
                   LC-FR3 is GVPSRFSGSGSGTDFTLTISSLQPEDFATYYC,; 
                 
                     
                   and 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 14) 
                 
                     
                   LC-FR4 is FGQGTKVEIKR. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         11 . The method of  claim 6  wherein:
 (a) one or more of the heavy chain framework sequences is the following: 
 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 4) 
                 
                     
                   HC-FR1 is EVQLVESGGGLVQPGGSLRLSCAAS; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 5) 
                 
                     
                   HC-FR2 is WVRQAPGKGLEWV; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 6) 
                 
                     
                   HC-FR3 is RFTISADTSKNTAYLQMNSLRAEDTAVYYCAR; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 7) 
                 
                     
                   HC-FR4 is WGQGTLVTVSA; 
                 
                     
                   and 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
         (b) one or more of the light chain framework sequences is the following: 
       
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 11) 
                 
                     
                   LC-FR1 is DIQMTQSPSSLSASVGDRVTITC; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 12) 
                 
                     
                   LC-FR2 is WYQQKPGKAPKLLIY; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 13) 
                 
                     
                   LC-FR3 is GVPSRFSGSGSGTDFTLTISSLQPEDFATYYC,; 
                 
                     
                   and 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 14) 
                 
                     
                   LC-FR4 is FGQGTKVEIKR. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         12 . The method of  claim 11  further comprising a human constant region. 
     
     
         13 . The method of  claim 12 , wherein the constant region is selected from the group consisting of IgG1, IgG2, IgG3 and IgG4. 
     
     
         14 . The method of  claim 13  wherein the constant region is IgG1. 
     
     
         15 . The method of  claim 14  having reduced or minimal effector function. 
     
     
         16 . The method of  claim 15 , wherein the minimal effector function results from an effector-less Fc mutation. 
     
     
         17 . The method of  claim 16 , wherein the effector-less Fc mutation is N297A. 
     
     
         18 . The method of  claim 16 , wherein the effector-less Fc mutation is D265A/N297A. 
     
     
         19 . The method of  claim 15 , wherein the minimal effector function results from aglycosylation. 
     
     
         20 . A method of treating a T-cell dysfunctional disorder resulting from an infection comprising administering an effective amount of an anti-PD-L1 antibody or antigen binding fragment thereof, wherein the antibody or antibody fragment comprises a heavy chain and a light chain variable region sequence, wherein:
 (a) the heavy chain comprises an HVR-H1, HVR-H2 and HVR-H3, wherein further:   
       
         
           
                 
               
                   (SEQ ID NO: 1) 
                 
                 
                 
               
                   (i) 
                   the HVR-H1 sequence is GFTFSX 1 SWIH; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 2) 
                 
                 
                 
               
                   (ii) 
                   the HVR-H2 sequence is AWIX 2 PYGGSX 3 YYADSVKG; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 3) 
                 
                 
                 
               
                   (iii) 
                   the HVR-H3 sequence is RHWPGGFDY,; 
                 
                   and 
                     
                 
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
           
         
         (b) the light chain comprises an HVR-L1, HVR-L2 and HVR-L3, wherein further: 
       
       
         
           
                 
               
                   (SEQ ID NOs: 8) 
                 
                 
                 
               
                   (iv) 
                   the HVR-L1 sequence is RASQX 4 X 5 X 6 TX 7 X 8 A; 
                 
                     
                 
                 
               
                   (SEQ ID NOs: 9) 
                 
                 
                 
               
                   (v) 
                   the HVR-L2 sequence is SASX 9 LX 10 S; 
                 
                     
                 
                 
               
                   (SEQ ID NOs: 10) 
                 
                 
                 
               
                   (vi) 
                   the HVR-L3 sequence is QQX 11 X 12 X 13 X 14 PX 15 T; 
                 
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
               
            
           
         
         wherein: X 1  is D or G; X 2  is S or L; X 3  is T or S; X 4  may be D or V; X 5  may be V or I; X 6  may be S or N; X 7  may be A or F; X 8  may be V or L; X 9  may be F or T; X 10  may be Y or A; X 11  may be Y, G, F, or S; X 12  may be L, Y, F or W; X 13  may be Y, N, A, T, G, F or I; X 14  may be H, V, P, T or I; X 15  may be A, W, R, P or T. 
       
     
     
         21 . The method of  claim 20  wherein X 1  is D; X 2  is S and X 3  is T. 
     
     
         22 . The method of  claim 20 , wherein X 4 =D, X 5 =V, X 6 =S, X 7 =A and X 8 =V, X 9 =F, and X 10 =Y, X 11 =Y, X 12 =L, X 13 =Y, X 14 =H and X 15 =A. 
     
     
         23 . The method of  claim 20 , wherein X 1 =D, X 2 =S and X 3 =T, X 4 =D, X 5 =V, X 6 =S, X 7 =A and X 8 =V, X 9 =F, and X 10 =Y, X 11 =Y, X 12 =L, X 13 =Y, X 14 =H and X 15 =A. 
     
     
         24 . The method of  claim 23 , wherein the encoded variable region heavy chain framework sequences are juxtaposed between the HVRs according to the formula: (HC-FR1)-(HVR-H1)-(HC-FR2)-(HVR-H2)-(HC-FR3)-(HVR-H3)-(HC-FR4) and/or the encoded variable region light chain framework sequences juxtaposed between the HVRs according to the formula: (LC-FR1)-(HVR-L1)-(LC-FR2)-(HVR-L2)-(LC-FR3)-(HVR-L3)-(LC-FR4). 
     
     
         25 . The method of  claim 24 , wherein the framework sequences are human. 
     
     
         26 . The method of  claim 25  wherein the variable heavy chain framework sequences are VH subgroup III consensus framework. 
     
     
         27 . The method of  claim 25  wherein the variable region light chain framework sequences are VL kappa I consensus framework. 
     
     
         28 . The method of  claim 26  wherein one or more of the heavy chain framework sequences is the following: 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 4) 
                 
                     
                   HC-FR1 is EVQLVESGGGLVQPGGSLRLSCAAS; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 5) 
                 
                     
                   HC-FR2 is WVRQAPGKGLEWV; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 6) 
                 
                     
                   HC-FR3 is RFTISADTSKNTAYLQMNSLRAEDTAVYYCAR; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 7) 
                 
                     
                   HC-FR4 is WGQGTLVTVSA. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         29 . The method of  claim 27  wherein one or more of the light chain framework sequences is the following: 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 11) 
                 
                     
                   LC-FR1 is DIQMTQSPSSLSASVGDRVTITC; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 12) 
                 
                     
                   LC-FR2 is WYQQKPGKAPKLLIY; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 13) 
                 
                     
                   LC-FR3 is GVPSRFSGSGSGTDFTLTISSLQPEDFATYYC,; 
                 
                     
                   and 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 14) 
                 
                     
                   LC-FR4 is FGQGTKVEIKR. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         30 . The method of  claim 27  wherein:
 (a) one or more of the heavy chain framework sequences is the following: 
 
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 4) 
                 
                     
                   HC-FR1 is EVQLVESGGGLVQPGGSLRLSCAAS; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 5) 
                 
                     
                   HC-FR2 is WVRQAPGKGLEWV; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 6) 
                 
                     
                   HC-FR3 is RFTISADTSKNTAYLQMNSLRAEDTAVYYCAR; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 7) 
                 
                     
                   HC-FR4 is WGQGTLVTVSA; 
                 
                     
                   and 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
         (b) one or more of the light chain framework sequences is the following: 
       
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 11) 
                 
                     
                   LC-FR1 is DIQMTQSPSSLSASVGDRVTITC; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 12) 
                 
                     
                   LC-FR2 is WYQQKPGKAPKLLIY; 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 13) 
                 
                     
                   LC-FR3 is GVPSRFSGSGSGTDFTLTISSLQPEDFATYYC,; 
                 
                     
                   and 
                 
                     
                     
                 
                     
                   (SEQ ID NO: 14) 
                 
                     
                   LC-FR4 is FGQGTKVEIKR. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         31 . The method of  claim 30  further comprising a human constant region. 
     
     
         32 . The method of  claim 31 , wherein the constant region is selected from the group consisting of IgG1, IgG2, IgG3 and IgG4. 
     
     
         33 . The method of  claim 32 , wherein the constant region is IgG1. 
     
     
         34 . The method of  claim 33  having reduced or minimal effector function. 
     
     
         35 . The method of  claim 34 , wherein the minimal effector function results from an effector-less Fc mutation. 
     
     
         36 . The method of  claim 35 , wherein the effector-less Fc mutation is N297A. 
     
     
         37 . The method of  claim 35 , wherein the effector-less Fc mutation is D265A/N297A. 
     
     
         38 . The method of  claim 34 , wherein the minimal effector function results from aglycosylation. 
     
     
         39 . A method of treating a T-cell dysfunctional disorder resulting from an infection comprising administering to a patient a composition comprising a pharmaceutically-acceptable carrier and therapeutically effective amount of an anti-PD-L1 antibody or antigen binding fragment thereof, wherein the antibody or antibody fragment comprises a heavy chain and light chain variable region sequence, wherein:
 (a) the heavy chain comprises the sequence: EVQLVESGGGLVQPGGSLRLS CAASGFTFSDSWIHWVRQAPGKGLEWVAWISPYGGSTYYADSVKGRFTI SADTSKNTAYLQMNSLRAEDTAVYYCARRHWPGGFDYWGQGTLVTVS A (SEQ ID NO:20), and   (b) the light chain comprises the sequence: DIQMTQSPSSLSASVGDRVTITC RASQDVSTAVAWYQQKPGKAPKLLIYSASFLYSGVPSRFSGSGSGTDFTL TISSLQPEDFATYYCQQYLYH PATFGQGTKVEIKR (SEQ ID NO:21).   
     
     
         40 . The method of  claim 39  wherein the antibody further comprises a human constant region. 
     
     
         41 . The method of  claim 40 , wherein the constant region is selected from the group consisting of IgG1, IgG2, IgG3 and IgG4. 
     
     
         42 . The method of  claim 41 , wherein the constant region is IgG1. 
     
     
         43 . The method of  claim 42  having reduced or minimal effector function. 
     
     
         44 . The nucleic acid of  claim 43 , wherein the minimal effector function results from an effector-less Fc mutation. 
     
     
         45 . The method of  claim 44 , wherein the effector-less Fc mutation is N297A. 
     
     
         46 . The method of  claim 44 , wherein the effector-less Fc mutation is D265A/N297A. 
     
     
         47 . The method of  claim 43 , wherein the minimal effector function results from aglycosylation. 
     
     
         48 . The method of any of  claims 39 - 47 , further comprising the administration of an antibiotic. 
     
     
         49 . The method of  claim 48 , wherein the antibiotic is an anti-viral agent. 
     
     
         50 . The method of  claim 49 , wherein the anti-viral agent is a reverse transcriptase inhibitor. 
     
     
         51 . The method of  claim 50 , wherein the reverse transcriptase inhibitor is a polymerase inhibitor. 
     
     
         52 . The method of  claim 49 , wherein the anti-viral agent is a protease inhibitor. 
     
     
         53 . The method of any of  claims 39 - 47 , further comprising the administration of at least one vaccine. 
     
     
         54 . The method of  claim 39 , wherein the infection is chronic. 
     
     
         55 . The method of  claim 54 , wherein the chronic infection is persistent. 
     
     
         56 . The method of  claim 54 , wherein the chronic infection is latent. 
     
     
         57 . The method of  claim 54 , where in the chronic infection is slow. 
     
     
         58 . The method of  claim 39 , wherein the infection results from a pathogen selected from the group consisting of bacteria, virus, fungi and protozoan. 
     
     
         59 . The method of  claim 58 , wherein the pathogen is a bacteria, and the method further comprises the administration of an anti-bacterial agent. 
     
     
         60 . The method of  claim 58 , wherein the pathogen is a virus, and the method further comprises the administration of an anti-viral agent. 
     
     
         61 . The method of  claim 58 , wherein the pathogen is a fungi, and the method further comprises the administration of an anti-fungal agent. 
     
     
         62 . The method of  claim 58 , wherein the pathogen is a protozoan, and the method further comprises the administration of an anti-protozoan agent.

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