IP Library Granted Patent US 10,189,888
Granted Patent B2
US 10,189,888 · App. 15/349,930 · Granted Jan 29, 2019

Viral vectors encoding recombinant FVIII variants with increased expression for gene therapy of hemophilia A

Inventors: Falko-Günter Falkner (Orth/Donau, AT); Franziska Horling (Gaenserndorf, AT); Johannes Lengler (Vienna, AT); Hanspeter Rottensteiner (Vienna, AT); Friedrich Scheiflinger (Vienna, AT)
Assignees: Baxalta Incorporated; Baxalta GmbH
C07K14/755A61K48/0008A61K48/0058A61K48/0066C12N15/86C12N2750/14143C12N2800/22C12N2840/007
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Quick Facts
Patent No.
US 10,189,888
App. No.
15/349,930
Granted
Jan 29, 2019
Kind
B2
Abstract

The present disclosure provides, among other aspects, codon-altered polynucleotides encoding Factor VIII variants for expression in mammalian cells. In some embodiments, the disclosure also provides mammalian gene therapy vectors and methods for treating hemophilia A.

Claims (48)

1. A polynucleotide comprising a nucleotide sequence encoding a Factor VIII polypeptide, the Factor VIII polypeptide comprising a light chain, a heavy chain, and a polypeptide linker joining the C-terminus of the heavy chain to the N-terminus of the light chain,

wherein the heavy chain of the Factor VIII polypeptide is encoded by a first nucleotide sequence having at least 99% identity over the entire length of SEQ ID NO: 3;

wherein the light chain of the Factor FVIII polypeptide is encoded by a second nucleotide sequence having at least 99% identity over the entire length of SEQ ID NO: 4; and

wherein the polypeptide linker comprises a furin cleavage site and a glycosylation peptide having an amino acid sequence of SEQ ID NO:55.

2. The polynucleotide of claim 1 , wherein the polypeptide linker is encoded by a third nucleotide sequence having at least 95% identity over the entire length of SEQ ID NO:38.

3. The polynucleotide of claim 1 , wherein the polypeptide linker is encoded by a third nucleotide sequence of SEQ ID NO:38.

4. The polynucleotide of claim 1 , wherein:

the first nucleotide sequence is SEQ ID NO: 3; and

the second nucleotide sequence is SEQ ID NO: 4.

5. The polynucleotide of claim 4 , wherein the polypeptide linker is encoded by a third nucleotide sequence of SEQ ID NO:38.

6. The polynucleotide of claim 1 , further comprising a promoter element operably linked to the polynucleotide encoding the Factor VIII polypeptide.

7. The polynucleotide of claim 6 , wherein the promoter element is a liver-specific promoter sequence upstream of the nucleotide sequence encoding the Factor VIII polypeptide.

8. The polynucleotide of claim 7 , further comprising an intron sequence positioned between the liver-specific promoter sequence and the nucleotide sequence encoding the Factor VIII polypeptide.

9. An adeno-associated virus (AAV) vector comprising a polynucleotide according to claim 1 .

10. An adeno-associated virus (AAV) particle comprising a polynucleotide according to claim 1 .

11. A host cell infected with an adeno-associated virus (AAV) particle comprising a polynucleotide according to claim 1 .

12. A method for producing an adeno-associated virus (AAV) particle comprising introducing a polynucleotide according to claim 1 into a mammalian host cell, wherein the polynucleotide is competent for replication in the mammalian host cell.

13. A method for treating hemophilia A comprising administering, to a patient in need thereof, an adeno-associated virus (AAV) particle according to claim 10 .

14. A method for transducing a host cell comprising contacting the host cell with an adeno-associated virus (AAV) particle according to claim 10 .

15. A polynucleotide comprising a nucleotide sequence having at least 99% identity over the entire length of SEQ ID NO:1, wherein the polynucleotide encodes a Factor VIII polypeptide having I105V, A127S, G151K, M166T, and L171P amino acid substitutions, relative to SEQ ID NO: 19.

16. The polynucleotide of claim 15 , wherein:

the Factor VIII polypeptide comprises a light chain, a heavy chain, and a polypeptide linker joining the C-terminus of the heavy chain to the N-terminus of the light chain; and

the polypeptide linker includes a glycosylation peptide having an amino acid sequence of SEQ ID NO:55 inserted between the heavy chain and the light chain.

17. The polynucleotide of claim 15 , comprising the sequence of SEQ ID NO:94.

18. The polynucleotide of claim 15 , further comprising a promoter element operably linked to the polynucleotide encoding the Factor VIII polypeptide.

19. The polynucleotide of claim 18 , wherein the promoter element is a liver-specific promoter sequence upstream of the nucleotide sequence encoding the Factor VIII polypeptide.

20. The polynucleotide of claim 19 , further comprising an intron sequence positioned between the liver-specific promoter sequence and the nucleotide sequence encoding the Factor VIII polypeptide.

21. An adeno-associated virus (AAV) vector comprising a polynucleotide according to claim 15 .

22. An adeno-associated virus (AAV) particle comprising a polynucleotide according to claim 15 .

23. A host cell infected with an adeno-associated virus (AAV) particle comprising a polynucleotide according to claim 15 .

24. A method for producing an adeno-associated virus (AAV) particle comprising introducing a polynucleotide according to claim 15 into a mammalian host cell, wherein the polynucleotide is competent for replication in the mammalian host cell.

25. A method for treating hemophilia A comprising administering, to a patient in need thereof, an adeno-associated virus (AAV) particle according to claim 22 .

26. A method for transducing a host cell comprising contacting the host cell with an adeno-associated virus (AAV) particle according to claim 22 .

27. A polynucleotide comprising a nucleotide sequence encoding a Factor VIII polypeptide, the Factor VIII polypeptide comprising a light chain, a heavy chain, and a polypeptide linker joining the C-terminus of the heavy chain to the N-terminus of the light chain, the Factor VIII polypeptide having I105V, A127S, G151K, M166T, and L171P amino acid substitutions, relative to SEQ ID NO: 19,

wherein the heavy chain of the Factor VIII polypeptide is encoded by a first nucleotide sequence having at least 99% identity over the entire length of SEQ ID NO: 3;

wherein the light chain of the Factor FVIII polypeptide is encoded by a second nucleotide sequence having at least 99% identity over the entire length of SEQ ID NO: 4; and

wherein the polypeptide linker comprises a furin cleavage site and a glycosylation peptide having an amino acid sequence of SEQ ID NO:55.

28. The polynucleotide of claim 27 , wherein the polypeptide linker is encoded by a third nucleotide sequence having at least 95% identity over the entire length of SEQ ID NO:38.

29. The polynucleotide of claim 27 , wherein the polypeptide linker is encoded by a third nucleotide sequence of SEQ ID NO:38.

30. The polynucleotide of claim 27 , further comprising a promoter element operably linked to the polynucleotide encoding the Factor VIII polypeptide.

31. The polynucleotide of claim 30 , wherein the promoter element is a liver-specific promoter sequence upstream of the nucleotide sequence encoding the Factor VIII polypeptide.

32. The polynucleotide of claim 31 , further comprising an intron sequence positioned between the liver-specific promoter sequence and the nucleotide sequence encoding the Factor VIII polypeptide.

33. An adeno-associated virus (AAV) vector comprising a polynucleotide according to claim 27 .

34. An adeno-associated virus (AAV) particle comprising a polynucleotide according to claim 27 .

35. A host cell infected with an adeno-associated virus (AAV) particle comprising a polynucleotide according to claim 27 .

36. A method for producing an adeno-associated virus (AAV) particle comprising introducing a polynucleotide according to claim 27 into a mammalian host cell, wherein the polynucleotide is competent for replication in the mammalian host cell.

37. A method for treating hemophilia A comprising administering, to a patient in need thereof, an adeno-associated virus (AAV) particle according to claim 34 .

38. A method for transducing a host cell comprising contacting the host cell with an adeno-associated virus (AAV) particle according to claim 34 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 31, 2021
From: BAXALTA GMBH; BAXALTA INCORPORATED
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 055189/0177 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 5, 2018
From: FALKNER, FALKO-GUENTER; HORLING, FRANZISKA; LENGLER, JOHANNES; ROTTENSTEINER, HANSPETER; SCHEIFLINGER, FRIEDRICH
To: BAXALTA INCORPORATED; BAXALTA GMBH
Reel/Frame 047678/0939 →
Continuity (2)
Provisional Application 62255317 · Nov 13, 2015
Related Publication 20170233455A1 · Aug 17, 2017
Cited By (1)
US 12,618,065