US2023053631A1PendingUtilityA1

Antibodies to lilrb2

69
Assignee: JOUNCE THERAPEUTICS INCPriority: Dec 22, 2017Filed: Jun 13, 2022Published: Feb 23, 2023
Est. expiryDec 22, 2037(~11.4 yrs left)· nominal 20-yr term from priority
C07K 2317/76C12Q 1/6886C07K 16/2896C07K 16/46A61P 35/00C12Q 2600/158C07K 2317/24A61K 45/06C07K 2317/565C07K 16/2803C07K 2317/33C07K 2317/92C07K 2317/32C07K 2317/31C07K 16/2818C07K 2317/51A61K 38/00C07K 16/3061C07K 2317/515A61K 2039/505
69
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Claims

Abstract

Provided herein are various embodiments relating to antibodies that bind LILRB2. Anti-LILRB2 antibodies can be used in methods to treat disease, for example, cancer.

Claims

exact text as granted — not AI-modified
1 . An antibody that specifically binds to human LILRB2, wherein the antibody comprises the following complementarity determining regions (CDRs):
 (a) a CDR-H1 comprising the amino acid sequence of JY(J) 2 G(J) 2  (SEQ ID NO: 171);   (b) a CDR-H2 comprising the amino acid sequence of (J) 2 W(J) 11 KJ (SEQ ID NO: 172);   (c) a CDR-H3 comprising the amino acid sequence of (J) 2 I(J) 3 TDYV(J) 3  (SEQ ID NO: 173);   (d) a CDR-L1 comprising the amino acid sequence of (J) 8 DLJ (SEQ ID NO: 174);   (e) a CDR-L2 comprising the amino acid sequence of (J) 7  (SEQ ID NO: 175); and   (f) a CDR-L3 comprising the amino acid sequence of (J) 3 YJYPLJ (SEQ ID NO: 176),   wherein each J is independently a naturally occurring amino acid.   
     
     
         2 . The antibody of  claim 1 , wherein the CDR-H2 comprises the amino acid sequence of SJW(J) 11 KJ (SEQ ID NO: 177) and/or the CDR-L3 comprises the amino acid sequence of (J) 3 YDYPLJ (SEQ ID NO: 178). 
     
     
         3 . The antibody of  claim 1 , wherein the CDR-H1 comprises the amino acid sequence of: 
       
         
           
                 
                 
               
                     
                   (i) 
                 
                     
                   (SEQ ID NO: 15) 
                 
                     
                   TYAMGVS; 
                 
                     
                     
                 
                     
                   (ii) 
                 
                     
                   (SEQ ID NO: 179) 
                 
                     
                   JYAMGVS; 
                 
                     
                     
                 
                     
                   (iii) 
                 
                     
                   (SEQ ID NO: 180) 
                 
                     
                   TYJMGVS; 
                 
                     
                     
                 
                     
                   (iv) 
                 
                     
                   (SEQ ID NO: 181) 
                 
                     
                   TYAJGVS; 
                 
                     
                     
                 
                     
                   (v) 
                 
                     
                   (SEQ ID NO: 182) 
                 
                     
                   TYAMGJS; 
                 
                     
                     
                 
                     
                   (vi) 
                 
                     
                   (SEQ ID NO: 183) 
                 
                     
                   TYAMGVJ; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 (vii) a variant of any one of (ii) to (vi) comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 171. 
 
     
     
         4 . The antibody of  claim 1 , wherein the CDR-H2 comprises the amino acid sequence of: 
       
         
           
                 
                 
               
                     
                   (i) 
                 
                     
                   (SEQ ID NO: 16) 
                 
                     
                   SIWWNGNKYNNPSLKS; 
                 
                     
                     
                 
                     
                   (ii) 
                 
                     
                   (SEQ ID NO: 184) 
                 
                     
                   SJWWNGNKYNNPSLKS; 
                 
                     
                     
                 
                     
                   (iii) 
                 
                     
                   (SEQ ID NO: 185) 
                 
                     
                   SIWJNGNKYNNPSLKS; 
                 
                     
                     
                 
                     
                   (iv) 
                 
                     
                   (SEQ ID NO: 186) 
                 
                     
                   SIWWJGNKYNNPSLKS; 
                 
                     
                     
                 
                     
                   (v) 
                 
                     
                   (SEQ ID NO: 187) 
                 
                     
                   SIWWNJNKYNNPSLKS; 
                 
                     
                     
                 
                     
                   (vi) 
                 
                     
                   (SEQ ID NO: 188) 
                 
                     
                   SIWWNGJKYNNPSLKS; 
                 
                     
                     
                 
                     
                   (vii) 
                 
                     
                   (SEQ ID NO: 189) 
                 
                     
                   SIWWNGNJYNNPSLKS; 
                 
                     
                     
                 
                     
                   (viii) 
                 
                     
                   (SEQ ID NO: 190) 
                 
                     
                   SIWWNGNKJNNPSLKS; 
                 
                     
                     
                 
                     
                   (ix) 
                 
                     
                   (SEQ ID NO: 191) 
                 
                     
                   SIWWNGNKYJNPSLKS; 
                 
                     
                     
                 
                     
                   (x) 
                 
                     
                   (SEQ ID NO: 192) 
                 
                     
                   SIWWNGNKYNJPSLKS; 
                 
                     
                     
                 
                     
                   (xi) 
                 
                     
                   (SEQ ID NO: 193) 
                 
                     
                   SIWWNGNKYNNJSLKS; 
                 
                     
                     
                 
                     
                   (xii) 
                 
                     
                   (SEQ ID NO: 194) 
                 
                     
                   SIWWNGNKYNNPJLKS; 
                 
                     
                     
                 
                     
                   (xiii) 
                 
                     
                   (SEQ ID NO: 195) 
                 
                     
                   SIWWNGNKYNNPSJKS; 
                 
                     
                     
                 
                     
                   (xiv) 
                 
                     
                   (SEQ ID NO: 196) 
                 
                     
                   SIWWNGNKYNNPSLKJ; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 (xv) a variant of any one of (ii) to (xiv) comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 172. 
 
     
     
         5 . The antibody of  claim 1 , wherein the CDR-H3 comprises the amino acid sequence of: 
       
         
           
                 
                 
               
                     
                   (ix) 
                 
                     
                   (SEQ ID NO: 204) 
                 
                     
                   SRIIRFTDYVMDJ; 
                 
                     
                     
                 
                     
                   (i) 
                 
                     
                   (SEQ ID NO: 17) 
                 
                     
                   SRHRFTDYVMDA; 
                 
                     
                     
                 
                     
                   (ii) 
                 
                     
                   (SEQ ID NO: 197) 
                 
                     
                   JRIIRFTDYVMDA; 
                 
                     
                     
                 
                     
                   (iii) 
                 
                     
                   (SEQ ID NO: 198) 
                 
                     
                   SJIIRFTDYVMDA; 
                 
                     
                     
                 
                     
                   (iv) 
                 
                     
                   (SEQ ID NO: 199) 
                 
                     
                   SRIJRFTDYVMDA; 
                 
                     
                     
                 
                     
                   (v) 
                 
                     
                   (SEQ ID NO: 200) 
                 
                     
                   SRIIJFTDYVMDA; 
                 
                     
                     
                 
                     
                   (vi) 
                 
                     
                   (SEQ ID NO: 201) 
                 
                     
                   SRIIRJTDYVMDA; 
                 
                     
                     
                 
                     
                   (vii) 
                 
                     
                   (SEQ ID NO: 202) 
                 
                     
                   SRIIRFTDYVJDA; 
                 
                     
                     
                 
                     
                   (viii) 
                 
                     
                   (SEQ ID NO: 203) 
                 
                     
                   SRIIRFTDYVMJA; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 (x) a variant of any one of (ii) to (ix) comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 173. 
 
     
     
         6 . The antibody of  claim 1 , wherein the CDR-L1 comprises the amino acid sequence of: 
       
         
           
                 
                 
               
                     
                   (i) 
                 
                     
                   (SEQ ID NO: 18) 
                 
                     
                   RASEDIYNDLA; 
                 
                     
                     
                 
                     
                   (ii) 
                 
                     
                   (SEQ ID NO: 205) 
                 
                     
                   JASEDIYNDLA; 
                 
                     
                     
                 
                     
                   (iii) 
                 
                     
                   (SEQ ID NO: 206) 
                 
                     
                   RJSEDIYNDLA; 
                 
                     
                     
                 
                     
                   (iv) 
                 
                     
                   (SEQ ID NO: 207) 
                 
                     
                   RAJEDIYNDLA; 
                 
                     
                     
                 
                     
                   (v) 
                 
                     
                   (SEQ ID NO: 208) 
                 
                     
                   RASJDIYNDLA; 
                 
                     
                     
                 
                     
                   (vi) 
                 
                     
                   (SEQ ID NO: 209) 
                 
                     
                   RASEJIYNDLA; 
                 
                     
                     
                 
                     
                   (vii) 
                 
                     
                   (SEQ ID NO: 210) 
                 
                     
                   RASEDJYNDLA; 
                 
                     
                     
                 
                     
                   (viii) 
                 
                     
                   (SEQ ID NO: 211) 
                 
                     
                   RASEDIJNDLA; 
                 
                     
                     
                 
                     
                   (ix) 
                 
                     
                   (SEQ ID NO: 212) 
                 
                     
                   RASEDIYJDLA; 
                 
                     
                     
                 
                     
                   (x) 
                 
                     
                   (SEQ ID NO: 213) 
                 
                     
                   RASEDIYNDLJ; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 (xi) a variant of any one of (ii) to (x) comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 174. 
 
     
     
         7 . The antibody of  claim 1 , wherein the CDR-L2 comprises the amino acid sequence of: 
       
         
           
                 
                 
               
                     
                   (i) 
                 
                     
                   (SEQ ID NO: 19) 
                 
                     
                   NANSLHT; 
                 
                     
                     
                 
                     
                   (ii) 
                 
                     
                   (SEQ ID NO: 214) 
                 
                     
                   JANSLHT; 
                 
                     
                     
                 
                     
                   (iii) 
                 
                     
                   (SEQ ID NO: 215) 
                 
                     
                   NJNSLHT; 
                 
                     
                     
                 
                     
                   (iv) 
                 
                     
                   (SEQ ID NO: 216) 
                 
                     
                   NAJSLHT; 
                 
                     
                     
                 
                     
                   (v) 
                 
                     
                   (SEQ ID NO: 217) 
                 
                     
                   NANJLHT; 
                 
                     
                     
                 
                     
                   (vi) 
                 
                     
                   (SEQ ID NO: 218) 
                 
                     
                   NANSJHT; 
                 
                     
                     
                 
                     
                   (vii) 
                 
                     
                   (SEQ ID NO: 219) 
                 
                     
                   NANSLJT; 
                 
                     
                     
                 
                     
                   (viii) 
                 
                     
                   (SEQ ID NO: 220) 
                 
                     
                   NANSLHJ; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 (ix) a variant of any one of (ii) to (viii) comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 175. 
 
     
     
         8 . The antibody of  claim 1 , wherein the CDR-L3 comprises the amino acid sequence of: 
       
         
           
                 
                 
               
                     
                   (i) 
                 
                     
                   (SEQ ID NO: 20) 
                 
                     
                   QQYYDYPLT; 
                 
                     
                     
                 
                     
                   (ii) 
                 
                     
                   (SEQ ID NO: 221) 
                 
                     
                   JQYYDYPLT; 
                 
                     
                     
                 
                     
                   (iii) 
                 
                     
                   (SEQ ID NO: 222) 
                 
                     
                   QJYYDYPLT; 
                 
                     
                     
                 
                     
                   (iv) 
                 
                     
                   (SEQ ID NO: 223) 
                 
                     
                   QQJYDYPLT; 
                 
                     
                     
                 
                     
                   (v) 
                 
                     
                   (SEQ ID NO: 224) 
                 
                     
                   QQYYDYPLJ; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 (vi) a variant of any one of (ii) to (v) comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 176. 
 
     
     
         9 . The antibody of  claim 1 , wherein the CDR-H2 comprises the amino acid sequence of JIWWNGNKYNNPSLKS (SEQ ID NO: 225), or a variant thereof comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 172, and/or the CDR-L3 comprises the amino acid sequence of QQYYJYPLT (SEQ ID NO: 226), or a variant thereof comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 176. 
     
     
         10 . The antibody of  claim 3 , wherein one or more of the CDRs comprises said additional J amino acid. 
     
     
         11 . The antibody of  claim 1 , wherein the CDR-H3 comprises the amino acid sequence of (J) 2 IJXJTDYV(J) 3  (SEQ ID NO: 227), wherein X is not arginine. 
     
     
         12 . The antibody of  claim 11 , wherein X is selected from the group consisting of aspartate, glutamate, and alanine. 
     
     
         13 . The antibody of  claim 11 , wherein the CDR-H3 comprises the sequence of: 
       
         
           
                 
                 
               
                     
                   (i) 
                 
                     
                   (SEQ ID NO: 228) 
                 
                     
                   JRIIXFTDYVMDA; 
                 
                     
                     
                 
                     
                   (ii) 
                 
                     
                   (SEQ ID NO: 229) 
                 
                     
                   SJIIXFTDYVMDA; 
                 
                     
                     
                 
                     
                   (iii) 
                 
                     
                   (SEQ ID NO: 230) 
                 
                     
                   SRIJXFTDYVMDA; 
                 
                     
                     
                 
                     
                   (iv) 
                 
                     
                   (SEQ ID NO: 231) 
                 
                     
                   SRIIXFTDYVMDA; 
                 
                     
                     
                 
                     
                   (v) 
                 
                     
                   (SEQ ID NO: 232) 
                 
                     
                   SRIIXJTDYVMDA; 
                 
                     
                     
                 
                     
                   (vi) 
                 
                     
                   (SEQ ID NO: 233) 
                 
                     
                   SRIIXFTDYVJDA; 
                 
                     
                     
                 
                     
                   (vii) 
                 
                     
                   (SEQ ID NO: 234) 
                 
                     
                   SRIIXFTDYVMJA; 
                 
                     
                     
                 
                     
                   (viii) 
                 
                     
                   (SEQ ID NO: 235) 
                 
                     
                   SRIIXFTDYVMDJ; 
                 
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
       or
 (ix) a variant of any one of (ii) to (iii) or (v) to (viii) comprising an additional J amino acid in place of a recited amino acid that is represented by a J in SEQ ID NO: 173. 
 
     
     
         14 . The antibody of  claim 1 , wherein the antibody comprises a variable heavy chain (V H ) region comprising an amino acid sequence that is at least 90% identical to the amino acid sequence of SEQ ID NO: 3, 13, 23, 33, 43, 53, 63, 73, 83, 93, 103, or 113, and/or a variable light chain (V L ) region comprising an amino acid sequence that is at least 90% identical to the amino acid sequence of SEQ ID NO: 4, 14, 24, 34, 44, 54, 64, 74, 84, 94, 104, or 114. 
     
     
         15 . The antibody of  claim 1 , wherein the antibody comprises a variable heavy chain (V H ) region comprising the amino acid sequence of SEQ ID NO: 3, 13, 23, 33, 43, 53, 63, 73, 83, 93, 103, or 113, and/or a variable light chain (V L ) region comprising the amino acid sequence of SEQ ID NO: 4, 14, 24, 34, 44, 54, 64, 74, 84, 94, 104, or 114. 
     
     
         16 . The antibody of  claim 1 , wherein the antibody comprises a heavy chain comprising an amino acid sequence that is at least 90% identical to the amino acid sequence of SEQ ID NO: 1, 11, 21, 31, 41, 51, 61, 71, 81, 91, 101, or 111, and/or a light chain comprising an amino acid sequence that is at least 90% identical to the amino acid sequence of SEQ ID NO: 2, 22, 32, 42, 52, 62, 72, 82, 92, 102, or 112. 
     
     
         17 - 49 . (canceled) 
     
     
         50 . The antibody of  claim 1 , wherein the heavy chain additionally comprises a C-terminal lysine. 
     
     
         51 - 66 . (canceled) 
     
     
         67 . The antibody of  claim 1 , wherein the antibody binds to LILRB2 with a dissociation constant (K D ) of less than 3.0 nM. 
     
     
         68 . The antibody of  claim 67 , wherein the antibody binds to LILRB2 with a K D  of less than 1.5 nM. 
     
     
         69 . The antibody of  claim 68 , wherein the antibody binds to LILRB2 with a K D  of less than 1.0 nM. 
     
     
         70 . The antibody of  claim 69 , wherein the antibody binds to LILRB2 with a dissociation constant (K D ) less than 750 pM. 
     
     
         71 . The antibody of  claim 1 , wherein the antibody is a monoclonal antibody. 
     
     
         72 . The antibody of  claim 1 , wherein the antibody is a chimeric antibody, a humanized antibody, a CDR-grafted antibody, or a human antibody. 
     
     
         73 . The antibody of  claim 1 , wherein the antibody comprises an Fc region selected from the group consisting of a native Fc region, a variant Fc region, and a functional Fc region. 
     
     
         74 . The antibody of  claim 1 , wherein the antibody is a conjugate antibody or is detectably labeled. 
     
     
         75 . The antibody of  claim 1 , wherein the antibody is an IgG1 antibody, an IgG2 antibody, an IgG3 antibody, or an IgG4 antibody. 
     
     
         76 . The antibody of  claim 75 , which is an IgG4 antibody. 
     
     
         77 - 96 . (canceled)

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