IP Library Granted Patent US 10,184,000
Granted Patent B2
US 10,184,000 · App. 15/167,832 · Granted Jan 22, 2019

Optimized Fc variants and methods for their generation

Inventors: Gregory Alan Lazar (Pacifica, CA); Arthur J. Chirino (Camarillo, CA); Wei Dang (Pasadena, CA); John Desjarlais (Pasadena, CA); Stephen K. Doberstein (San Francisco, CA); Robert J. Hayes (Thousand Oaks, CA); Sher Bahadur Karki (Santa Monica, CA); Omid Vafa (Monrovia, CA)
Assignee: Xencor, Inc.
C07K16/283A61K39/395A61K39/3955A61K39/39566C07K16/00C07K16/22C07K16/2863C07K16/2875C07K16/2887C07K16/2893C07K16/2896C07K16/32C07K16/4291C12P21/005C40B30/02G06F19/12G06F19/16G06F19/22A61K2039/505C07K2317/14C07K2317/21C07K2317/24C07K2317/33C07K2317/34C07K2317/41C07K2317/51C07K2317/52C07K2317/522C07K2317/524C07K2317/526C07K2317/56C07K2317/71C07K2317/72C07K2317/732C07K2317/734C07K2317/76C07K2317/77C07K2317/92C07K2319/30
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Quick Facts
Patent No.
US 10,184,000
App. No.
15/167,832
Granted
Jan 22, 2019
Kind
B2
Abstract

The present invention relates to optimized Fc variants, methods for their generation, and antibodies and Fc fusions comprising optimized Fc variants.

Claims (38)

1. A nucleic acid encoding a polypeptide comprising an Fc variant of a parent Fc polypeptide, said Fc variant comprising amino acid substitutions at positions 239 and 332 in the Fc region, wherein numbering is according to the EU index.

2. The nucleic acid according to claim 1 , wherein the substitution at position 239 is selected from the group consisting of D and E.

3. The nucleic acid according to claim 1 , wherein the substitution at position 332 is selected from the group consisting of D and E.

4. The nucleic acid according to claim 1 , wherein the substitution at positions 239 and 332 are selected from the group consisting of 239D/332E, 239D/332D, 239E/332D, and 239E/332E.

5. The nucleic acid according to claim 1 , wherein the substitutions at positions 239 and 332 are 239D and 332E.

6. The nucleic acid according to claim 1 , wherein the parent Fc polypeptide is a human IgG1 Fc polypeptide.

7. An expression vector comprising the nucleic acid according to claim 1 .

8. A host cell comprising a nucleic acid according to claim 1 .

9. A host cell comprising an expression vector according to claim 7 .

10. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 8 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

11. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 9 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

12. A nucleic acid encoding a heavy chain of an antibody comprising an Fc variant of a parent Fc polypeptide, said Fc variant comprising amino acid substitutions at positions 239 and 332 in the Fc region, wherein numbering is according to the EU index.

13. The nucleic acid according to claim 12 , wherein the substitution at position 239 is selected from the group consisting of D and E.

14. The nucleic acid according to claim 12 , wherein the substitution at position 332 is selected from the group consisting of D and E.

15. The nucleic acid according to claim 12 , wherein the substitution at positions 239 and 332 are selected from the group consisting of 239D/332E, 239D/332D, 239E/332D, and 239E/332E.

16. The nucleic acid according to claim 12 , wherein the substitutions at positions 239 and 332 are 239D and 332E.

17. The nucleic acid according to claim 12 , wherein the parent Fc polypeptide is a human IgG1 Fc polypeptide.

18. The nucleic acid according to claim 12 , wherein the antibody is a monoclonal antibody.

19. An expression vector comprising the nucleic acid according to claim 12 .

20. A host cell comprising a nucleic acid according to claim 12 .

21. A host cell comprising an expression vector according to claim 19 .

22. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 20 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

23. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 21 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

24. A nucleic acid encoding a polypeptide comprising an Fc variant of a parent Fc polypeptide, said Fc variant comprising amino acid substitutions 239D and 332E in the Fc region, wherein said Fc variant exhibits increased FcγRIIIa binding, and wherein numbering is according to the EU index.

25. The nucleic acid according to claim 24 , wherein the parent Fc polypeptide is a human IgG1 Fc polypeptide.

26. An expression vector comprising the nucleic acid according to claim 24 .

27. A host cell comprising a nucleic acid according to claim 24 .

28. A host cell comprising an expression vector according to claim 26 .

29. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 27 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

30. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 28 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

31. A nucleic acid encoding a heavy chain of an antibody comprising an Fc variant of a parent Fc polypeptide, said Fc variant comprising amino acid substitutions 239D and 332E in the Fc region, wherein said Fc variant exhibits increased FcγRIIIa binding, and wherein numbering is according to the EU index.

32. The nucleic acid according to claim 31 , wherein the parent Fc polypeptide is a human IgG1 Fc polypeptide.

33. The nucleic acid according to claim 31 , wherein the antibody is a monoclonal antibody.

34. An expression vector comprising the nucleic acid according to claim 31 .

35. A host cell comprising a nucleic acid according to claim 31 .

36. A host cell comprising an expression vector according to claim 34 .

37. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 35 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

38. A method of producing a polypeptide comprising: a) culturing a host cell according to claim 36 under conditions wherein said polypeptide is produced; and b) purifying said polypeptide.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 31, 2016
From: LAZAR, GREGORY ALAN; CHIRINO, ARTHUR J.; DANG, WEI; DESJARLAIS, JOHN RUDOLPH; DOBERSTEIN, STEPHEN KOHL; HAYES, ROBERT J.; KARKI, SHER BAHADUR; VAFA, OMID
To: XENCOR, INC.
Reel/Frame 038754/0395 →
Continuity (9)
Division 13773485 · Feb 21, 2013
Division 13346604 · Jan 9, 2012
Division 11981822 · Oct 31, 2007
Division 10672280 · Sep 26, 2003
Provisional Application 60477839 · Jun 12, 2003
Provisional Application 60467606 · May 2, 2003
Provisional Application 60442301 · Jan 23, 2003
Provisional Application 60414433 · Sep 27, 2002
Related Publication 20160347825A1 · Dec 1, 2016
Cited By (1)
US 12,338,278