IP Library › Granted Patent US 9,951,136
Granted Patent B2
US 9,951,136 · App. 14/268,932 · Granted Apr 24, 2018

Anti-IL-6 receptor antibodies and methods of use

Inventors: Sum Wai Pierre Lee (San Francisco, CA); Yaohuang Ke (San Francisco, CA); Yongke Zhang (Palo Alto, CA)
Assignee: APEXIGEN, INC.
C07K16/2866C07K2317/24C07K2317/33C07K2317/522C07K2317/54C07K2317/55C07K2317/76C07K2317/92
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Quick Facts
Patent No.
US 9,951,136
App. No.
14/268,932
Granted
Apr 24, 2018
Kind
B2
Abstract

The present invention provides anti-IL-6R monoclonal antibodies and related compositions, which may be used in any of a variety of therapeutic methods for the treatment of rheumatoid arthritis and other diseases.

Claims (21)

1. An isolated antibody or antigen-binding fragment thereof that binds to human interleukin-6 receptor (IL-6R), comprising:

(a) a heavy chain variable region comprising a VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:13, a VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:14, and a VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:15, and a light chain variable region comprising a VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:16, a VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO: 17, and a VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:18;

(b) a heavy chain variable region comprising a VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:45, a VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:55, and a VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:65, and a light chain variable region comprising a VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:75, a VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:85, and a VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:95;

(c) a heavy chain variable region comprising a VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:50, a VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:60, and a VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:70, and a light chain variable region comprising a VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:80, a VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:90, and a VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:100; or

(d) a heavy chain variable region comprising a VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:51, a VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:61, and a VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:71, and a light chain variable region comprising a VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:81, a VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:91, and a VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO: 101.

2. The isolated antibody or antigen-binding fragment thereof of claim 1 wherein the heavy chain variable region comprises the amino acid sequence set forth in SEQ ID NO:19.

3. The isolated antibody or antigen-binding fragment thereof of claim 1 wherein the light chain variable region comprises the amino acid sequence set forth in SEQ ID NO:20.

4. The isolated antibody or antigen-binding fragment thereof of claim 1 , wherein the antibody is humanized.

5. The isolated antibody or antigen-binding fragment thereof of claim 1 , wherein the antibody is selected from the group consisting of a single chain antibody, an scFv, a univalent antibody lacking a hinge region, and a minibody.

6. The isolated antigen-binding fragment of claim 1 , wherein the antigen-binding fragment is a Fab or a Fab′ fragment.

7. The isolated antigen-binding fragment of claim 1 , wherein the antigen-binding fragment is a F(ab′)2 fragment.

8. The isolated antibody of claim 1 , wherein the antibody is a whole antibody.

9. The isolated antibody or antigen-binding fragment thereof of claim 1 , comprising a human IgG constant domain.

10. The isolated antibody or antigen-binding fragment thereof of claim 9 , wherein the IgG constant domain comprises an IgG1 CH1 domain.

11. The isolated antibody or antigen-binding fragment thereof of claim 9 wherein the IgG constant domain comprises an IgG1 Fc region.

12. A composition comprising a physiologically acceptable carrier and a therapeutically effective amount of the isolated antibody or antigen-binding fragment thereof according to claim 1 .

13. The isolated antibody or antigen-binding fragment thereof of claim 1 , wherein the heavy chain variable region comprises the VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:13, the VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO: 14, and the VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:15, and wherein the light chain variable region comprises the VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:16, the VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:17, and the VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO: 18.

14. The isolated antibody or antigen-binding fragment thereof of claim 1 , wherein the heavy chain variable region comprises the amino acid sequence set forth in SEQ ID NO:19 and the light chain variable region comprises the amino acid sequence set forth in SEQ ID NO:20.

15. The isolated antibody or antigen-binding fragment thereof of claim 1 , wherein the heavy chain variable region comprises the VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:45, the VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:55, and the VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:65, and wherein the light chain variable region comprises the VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:75, the VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:85, and the VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:95.

16. The isolated antibody or antigen-binding fragment thereof of claim 1 , wherein the heavy chain variable region comprises the VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:50, the VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:60, and the VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:70, and wherein the light chain variable region comprises the VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:80, the VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:90, and the VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO: 100.

17. The isolated antibody or antigen-binding fragment thereof of claim 1 , wherein the heavy chain variable region comprises the VHCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:51, the VHCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:61, and the VHCDR3 region comprising the amino acid sequence set forth in SEQ ID NO:71, and wherein the light chain variable region comprises the VLCDR1 region comprising the amino acid sequence set forth in SEQ ID NO:81, the VLCDR2 region comprising the amino acid sequence set forth in SEQ ID NO:91, and the VLCDR3 region comprising the amino acid sequence set forth in SEQ ID NO: 101.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 18, 2016
From: LEE, SUM WAI PIERRE; KE, YAOHUANG; ZHANG, YONGKE
To: APEXIGEN, INC.
Reel/Frame 040414/0487 →
Continuity (3)
Continuation 13407293 · Feb 28, 2012
Provisional Application 61449005 · Mar 3, 2011
Related Publication 20140322239A1 · Oct 30, 2014