US2013045202A1PendingUtilityA1

Anti-pd-l1 antibodies and articles of manufacture

Assignee: GENENTECH INCPriority: Dec 9, 2008Filed: May 24, 2012Published: Feb 21, 2013
Est. expiryDec 9, 2028(~2.4 yrs left)· nominal 20-yr term from priority
A61P 43/00A61P 37/00A61P 33/02A61P 35/00A61P 31/12A61P 33/00A61P 31/04A61P 37/04A61P 37/02A61P 31/00A61P 31/10C07K 16/1145C07K 2317/52C07K 2317/73C07K 2317/71C07K 2317/56C07K 2317/74A61K 31/7068A61K 39/39558A61K 45/06C07K 2317/567C07K 16/30C07K 16/2827A61K 39/3955C07K 2317/92A61K 2039/507A61K 2039/505C07K 2317/565C07K 2317/76C07K 16/28C07K 16/22C07K 16/3046C07K 2317/14C07K 2317/24A61K 39/00Y02A50/30A61K 2300/00
62
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

The present application relates to anti-PD-L1 antibodies, which have therapeutic use 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 . An isolated anti-PD-L1 antibody or antigen binding fragment comprising a light chain or a heavy chain variable region sequence, wherein:
 (a) the heavy chain or antigen binding fragment thereof further comprises and HVR-H1, HVR-H2 and an HVR-H3 sequence having at least 85% sequence identity to GFTFSDSWIH (SEQ ID NO:15), AWISPYGGSTYYADSVKG (SEQ ID NO:16) and RHWPGGFDY (SEQ ID NO:3), respectively, or   (b) the light chain or antigen binding fragment thereof further comprises an HVR-L1, HVR-L2 and an HVR-L3 sequence having at least 85% sequence identity to RASQDVSTAVA (SEQ ID NO:17), SASFLYS (SEQ ID NO:18) and QQYLYHPAT (SEQ ID NO:19), respectively.   
     
     
         2 . The antibody of  claim 1 , wherein sequence identity is 90%. 
     
     
         3 . The antibody of  claim 2 , wherein the sequence identity is 95%. 
     
     
         4 . The antibody of  claim 1 , wherein the anti-PD-L1 antibody further comprises a VL and a VH framework region derived from a human consensus sequence. 
     
     
         5 . The antibody of  claim 4 , wherein the VH sequence is derived from a Kabat subgroup I, II, or III sequence. 
     
     
         6 . The antibody of  claim 5 , wherein the VH sequence is derived from Kabat subgroup III. 
     
     
         7 . The antibody of  claim 6 , further wherein the 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). 
     
     
         8 . The antibody 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. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         9 . The antibody of  claim 4 , wherein the VL sequence is derived from a Kabat kappa I, II, III or IV subgroup sequence. 
     
     
         10 . The antibody of  claim 9 , wherein the VL sequence is derived from Kabat kappa I. 
     
     
         11 . The antibody of  claim 9 , further wherein the variable light chain framework sequences are juxtaposed between the HVRs according to the formula: (LC-FR1)—(HVR-L1)-(LC-FR2)—(HVR-L2)-(LC-FR3)—(HVR-L3)-(LC-FR4). 
     
     
         12 . The antibody of  claim 11 , 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. 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         13 . The antibody of  claim 1 , wherein the anti-PD-L1 antibody comprises a constant region derived from a human antibody. 
     
     
         14 . The antibody of  claim 13 , wherein the constant region is IgG1. 
     
     
         15 . The antibody of  claim 14 , wherein the encoded antibody has reduced or minimal effector function. 
     
     
         16 . The antibody of  claim 15 , wherein the minimal effector function results from an effector-less Fc mutation. 
     
     
         17 . The antibody of  claim 16 , wherein the effector-less Fc mutation is N297A. 
     
     
         18 . The antibody of  claim 16 , wherein the effector-less Fc mutation is D265A/N297A. 
     
     
         19 . An isolated 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 sequence has at least 85% sequence identity to the heavy chain sequence:   
       
         
           
                 
               
                   (SEQ ID NO: 20) 
                 
                   EVQLVESGGGLVQPGGSLRLSCAASGFTFSDSWIHWVRQAPGKGLEWV 
                 
                     
                 
                   AWISPYGGSTYYADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYC 
                 
                     
                 
                   ARRHWPGGFDYWGQGTLVTVSA, 
                 
             
                
                
                
                
                
                
               
            
           
         
         further wherein, the heavy chain comprises an HVR-H1, HVR-H2 and HVR-H3, in which:
 (A) the HVR-H1 sequence is GFTFSX 1 SWIH (SEQ ID NO:1); 
 (B) the HVR-H2 sequence is AWIX 2 PYGGSX 3 YYADSVKG (SEQ ID NO:2); 
 (C) the HVR-H3 sequence is RHWPGGFDY, and (SEQ ID NO:3); and 
 
         (b) the light chain sequence has at least 85% sequence identity to the light chain sequence: 
       
       
         
           
                 
                 
               
                     
                   (SEQ ID NO: 21) 
                 
                     
                   DIQMTQSPSSLSASVGDRVTITCRASQDVSTAVAWYQQKP 
                 
                     
                     
                 
                     
                   GKYSASSFLYSGVPSRFSGSGSGTDFTLTISSLQPEDFAT 
                 
                     
                     
                 
                     
                   YYCQQYLYH PATFGQGTKVEIKR; 
                 
             
                
                
                
                
                
                
               
            
           
         
         further wherein, the light chain comprises an HVR-L1, HVR-L2 and HVR-L3, in which:
 (A) the HVR-L1 sequence is RASQX 4 X 5 X 6 TX 7 X 8 A (SEQ ID NOs:8); 
 (B) the HVR-L2 sequence is SASX 9 LX 10 S (SEQ ID NOs:9); 
 (C) the HVR-L3 sequence is QQX 11 X 12 X 13 X 14 PX 15 T (SEQ ID NOs:10); 
 
         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. 
       
     
     
         20 . The antibody of  claim 19  wherein X 1  is D; X 2  is S and X 3  is T. 
     
     
         21 . The antibody of  claim 19 , 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. 
     
     
         22 . The antibody of  claim 19 , 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. 
     
     
         23 . The antibody of  claim 22 , wherein the sequence identity is 90%. 
     
     
         24 . The antibody of  claim 23 , wherein the sequence identity is 95%. 
     
     
         25 . The antibody of  claim 24 , wherein the sequence identity is 96%. 
     
     
         26 . The antibody of  claim 25 , wherein the sequence identity is 97%. 
     
     
         27 . The antibody of  claim 26 , wherein the sequence identity is 98%. 
     
     
         28 . The antibody of  claim 27 , wherein the sequence identity is 99%. 
     
     
         29 . The antibody of  claim 19  wherein the antibody or antibody fragment comprises:
 (a) variable region heavy chain framework sequences juxtaposed between the HVRs according to the formula: (HC—FR1)—(HVR-H1)—(HC—FR2)—(HVR-H2)—(HC—FR3)—(HVR-H3)—(HC—FR4), and/or 
 (b) 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). 
 
       wherein the variable heavy chain framework sequences are the following: 
       
         
           
                 
               
                   (SEQ ID NO: 4) 
                 
                 
                 
               
                   (i) 
                   HC-FR1 is EVQLVESGGGLVQPGGSLRLSCAAS; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 5) 
                 
                 
                 
               
                   (ii) 
                   HC-FR2 is WVRQAPGKGLEWV; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 6) 
                 
                 
                 
               
                   (iii) 
                   HC-FR3 is RFTISADTSKNTAYLQMNSLRAEDTAVYYCAR; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 7) 
                 
                 
                 
               
                   (iv) 
                   HC-FR4 is WGQGTLVTVSA; 
                 
                     
                   and; 
                 
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
           
         
       
       and/or 
       further wherein the variable light chain framework sequences are the following: 
       
         
           
                 
               
                   (SEQ ID NO: 11) 
                 
                 
                 
               
                   (v) 
                   LC-FR1 is DIQMTQSPSSLSASVGDRVTITC; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 12) 
                 
                 
                 
               
                   (vi) 
                   LC-FR2 is WYQQKPGKAPKLLIY; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 13) 
                 
                 
                 
               
                   (vii) 
                   LC-FR3 is GVPSRFSGSGSGTDFTLTISSLQPEDFATYYC; 
                 
                     
                 
                 
               
                   (SEQ ID NO: 14) 
                 
                 
                 
               
                   (iv) 
                   LC-FR4 is FGQGTKVEIKR. 
                 
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
                
               
            
             
                
               
            
             
                
               
            
           
         
       
     
     
         30 . The antibody of  claim 29  further comprising a human constant region. 
     
     
         31 . The antibody of  claim 30 , wherein the constant region is selected from the group consisting of IgG1, IgG2, IgG3 and IgG4. 
     
     
         32 . The antibody of  claim 31 , wherein the constant region is IgG1. 
     
     
         33 . The antibody of  claim 32  having reduced or minimal effector function. 
     
     
         34 . The antibody of  claim 33 , wherein the minimal effector function results from an effector-less Fc mutation. 
     
     
         35 . The antibody of  claim 34 , wherein the effector-less Fc mutation is N297A. 
     
     
         36 . The antibody of  claim 34 , wherein the effector-less Fc mutation is D265A/N297A. 
     
     
         37 . The antibody of  claim 33 , wherein the minimal effector function results from aglycosylation. 
     
     
         38 . A composition comprising the antibody of  claims 1 - 18  and a pharmaceutically acceptable carrier. 
     
     
         39 . A composition comprising the antibody of  claims 19 - 37  and a pharmaceutically acceptable carrier. 
     
     
         40 . An article of manufacture comprising the composition of  claim 39  and at least one vaccine. 
     
     
         41 . An article of manufacture comprising the composition of  claim 39  and at least one anti-viral agent. 
     
     
         42 . An article of manufacture comprising the composition of  claim 39  and at least one chemotherapeutic agent. 
     
     
         43 . The article of  claim 42 , wherein the chemotherapeutic agent is an anti-VEGF antibody. 
     
     
         44 . The article of  claim 43 , wherein the chemotherapeutic agent is oxaliplatin. 
     
     
         45 . The article of  claim 43 , wherein the chemotherapeutic agent is a RAF inhibitor.

Join the waitlist — get patent alerts

Track US2013045202A1 — get alerts on status changes and closely related new filings.

We store only your email — no account needed. See our privacy policy.