IP Library Granted Patent US 11,987,633
Granted Patent B2
US 11,987,633 · App. 17/204,166 · Granted May 21, 2024

Cross-species-specific single domain bispecific single chain antibody

Inventors: Peter Kufer (Munich, DE); Tobias Raum (Munich, DE); Roman Kischel (Munich, DE); Ralf Lutterbüse (Munich, DE); Patrick Hoffmann (Munich, DE); Matthias Klinger (Munich, DE); Doris Rau (Munich, DE); Susanne Mangold (Munich, DE)
Assignee: AMGEN RESEARCH (MUNICH) GMBH
C07K16/2863C07K16/2803C07K16/2878C07K16/2884C07K2317/31C07K2317/34
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Quick Facts
Patent No.
US 11,987,633
App. No.
17/204,166
Granted
May 21, 2024
Kind
B2
Abstract

The present invention relates to a bispecific single chain antibody molecule comprising a first binding domain consisting of one antibody variable domain capable of binding to an epitope of the human and non-chimpanzee primate CD3 epsilon chain, wherein the epitope is part of an amino acid sequence comprised in the group consisting of SEQ ID NOs. 2, 4, 6, and 8, and a second binding domain capable of binding to an epitope of a human and a non-chimpanzee primate tumor target antigen. The invention further relates to a bispecific single chain antibody molecule comprising a first binding domain capable of binding to an epitope of human and non-chimpanzee primate CD3ε (epsilon) chain, wherein the epitope is part of an amino acid sequence comprised in the group consisting of SEQ ID NOs. 2, 4, 6, and 8, and a second binding domain consisting of one antibody variable domain capable of binding to an epitope of a human and a non-chimpanzee primate tumor target antigen. The invention also provides nucleic acids encoding said bispecific single chain antibody molecule as well as vectors and host cells and a process for its production. The invention further relates to pharmaceutical compositions comprising said bispecific single chain antibody molecule and medical uses of said bispecific single chain antibody molecule.

Claims (45)

1. A nucleic acid comprising a polynucleotide encoding a bispecific single chain antibody molecule comprising a first binding domain which binds to an epitope of a human CD3 epsilon (CD3ε) chain, wherein the epitope is part of the amino acid sequence set forth in SEQ ID NO: 2, 4, 6, or 8, and comprises at least the amino acid sequence Gln-Asp-Gly-Asn-Glu (QDGNE; SEQ ID NO: 430), and a second binding domain comprising an antibody variable domain that is cross-species specific and binds to an epitope of a human and a non-chimpanzee primate tumor target antigen, wherein the first binding domain is a VHH domain and comprises CDR 1 of SEQ ID NO: 398, CDR 2 of SEQ ID NO: 399 and CDR 3 of SEQ ID. NO: 400.

2. The nucleic acid of claim 1 , wherein the first binding domain further binds a Callithrix jacchus, Sanguinis oedipus or Saimiri sciureus CD3ε chain.

3. The nucleic acid of claim 1 , wherein at least one of said first or second binding domain is CDR-grafted, humanized or human.

4. The nucleic acid of claim 1 , wherein the first binding domain comprises an antibody variable domain comprising:

(a) the amino acid sequence of SEQ ID NO. 397;

(b) an amino acid sequence encoded by the nucleotide sequence of SEQ ID NO: 401;

(c) an amino acid sequence at least 80% identical to the amino acid sequence of SEQ ID NO: 397 or the amino acid sequence encoded by the nucleotide sequence of SEQ ID NO: 401; or

(d) an amino acid sequence at least 90% identical to the amino acid sequence of SEQ ID NO: 397 or the amino acid sequence encoded by the nucleotide sequence of SEQ ID NO: 401.

5. The nucleic acid of claim 1 , wherein the antibody variable domain of the second binding domain comprises CDR1-3 selected from the group consisting of:

(a) CDR 1 of SEQ ID NO: 376, CDR 2 of SEQ ID NO. 377 and CDR 3 of SEQ ID NO. 378; and

(b) CDR 1 of SEQ ID NO: 387, CDR 2 of SEQ ID NO. 388 and CDR 3 of SEQ ID NO. 389.

6. The nucleic acid of claim 1 , wherein the second binding domain comprises an antibody variable domain as shown in SEQ ID NO: 375 or 386 or an amino acid sequence at least 80% identical to the amino acid sequence of SEQ ID NO: 375 or 386.

7. The nucleic acid of claim 1 , wherein the bispecific single chain antibody molecule comprises a sequence selected from:

(a) the amino acid sequence of SEQ ID NO: 380, 382, 384, 391, 393 or 395;

(b) an amino acid sequence encoded by the nucleic acid sequence of SEQ ID NO: 381, 383, 385, 392, 394 or 396; and

(c) an amino acid sequence at least 85% identical to the amino acid sequence of (a) or (b).

8. The nucleic acid of claim 1 , wherein the second binding domain comprises one antibody variable domain or two antibody variable domains.

9. The nucleic acid of claim 1 , wherein the second binding domain comprises a VHH domain.

10. The nucleic acid of claim 1 , wherein the tumor target antigen is EGFR, CD44v6 or CD30.

11. A nucleic acid comprising a polynucleotide encoding a bispecific single chain antibody molecule comprising a first binding domain, which binds to an epitope of a human CD3 epsilon (CD3ε) chain, wherein the epitope is part of the amino acid sequence set forth in SEQ ID NO: 2, 4, 6, or 8, and a second binding domain consisting of one antibody variable domain that is cross-species specific and binds to an epitope of a human and a non-chimpanzee primate tumor target antigen, wherein the first binding domain is a VHH domain and comprises CDR 1 of SEQ ID NO: 398, CDR 2 of SEQ ID NO: 399 and CDR 3 of SEQ ID. NO: 400.

12. The nucleic acid of claim 11 , wherein the first binding domain further binds a non-chimpanzee primate CD3ε chain.

13. The nucleic acid of claim 11 , wherein the first binding domain further binds a Callithrix jacchus, Sanguinis oedipus or Saimiri sciureus CD3ε chain.

14. The nucleic acid of claim 11 , wherein at least one of said first or second binding domain is CDR-grafted, humanized or human.

15. The nucleic acid of claim 11 , wherein the first binding domain comprises an antibody variable domain comprising:

(a) the amino acid sequence of SEQ ID NO. 397;

(b) an amino acid sequence encoded by the nucleotide sequence of SEQ ID NO: 401;

(c) an amino acid sequence at least 80% identical to the amino acid sequence of SEQ ID NO: 397 or the amino acid sequence encoded by the nucleotide sequence of SEQ ID NO: 401; or

(d) an amino acid sequence at least 90% identical to the amino acid sequence of SEQ ID NO: 397 or the amino acid sequence encoded by the nucleotide sequence of SEQ ID NO: 401.

16. The nucleic acid of claim 11 , wherein the antibody variable domain of the second binding domain comprises CDR1-3 selected from the group consisting of:

(a) CDR 1 of SEQ ID NO: 376, CDR 2 of SEQ ID NO. 377 and CDR 3 of SEQ ID NO. 378; and

(b) CDR 1 of SEQ ID NO: 387, CDR 2 of SEQ ID NO. 388 and CDR 3 of SEQ ID NO. 389.

17. The nucleic acid of claim 11 , wherein the second binding domain comprises an antibody variable domain as shown in SEQ ID NO: 375 or 386 or an amino acid sequence at least 80% identical to the amino acid sequence of SEQ ID NO: 375 or 386.

18. The nucleic acid of claim 11 , wherein the bispecific single chain antibody molecule comprises a sequence selected from:

(a) the amino acid sequence of SEQ ID NO: 380, 382, 384, 391, 393 or 395;

(b) an amino acid sequence encoded by the nucleic acid sequence of SEQ ID NO: 381, 383, 385, 392, 394 or 396; and

(c) an amino acid sequence at least 85% identical to the amino acid sequence of (a) or (b).

19. The nucleic acid of claim 11 , wherein the second binding domain comprises one antibody variable domain or two antibody variable domains.

20. The nucleic acid of claim 11 , wherein the second binding domain comprises a VHH domain.

21. The nucleic acid of claim 11 , wherein the tumor target antigen is EGFR, CD44v6 or CD30.

22. A vector comprising the nucleic acid of claim 1 .

23. A vector comprising the nucleic acid of claim 11 .

24. A host cell comprising the vector of claim 22 .

25. A host cell comprising the vector of claim 23 .

26. A process for producing a bispecific single chain antibody molecule comprising a first binding domain which binds to an epitope of a human CD3 epsilon (CD3ε) chain, wherein the epitope is part of the amino acid sequence set forth in SEQ ID NO: 2, 4, 6, or 8, and comprises at least the amino acid sequence Gln-Asp-Gly-Asn-Glu (QDGNE; SEQ ID NO: 430), and a second binding domain comprising an antibody variable domain that is cross-species specific and binds to an epitope of a human and a non-chimpanzee primate tumor target antigen, wherein the first binding domain is a VHH domain and comprises CDR 1 of SEQ ID NO: 398, CDR 2 of SEQ ID NO: 399 and CDR 3 of SEQ ID. NO: 400, the process comprising culturing the host cell of claim 24 under conditions allowing the expression of the bispecific single chain antibody molecule and recovering the molecule from the culture.

27. A process for producing a bispecific single chain antibody molecule comprising a first binding domain, which binds to an epitope of a human CD3 epsilon (CD3ε) chain, wherein the epitope is part of the amino acid sequence set forth in SEQ ID NO: 2, 4, 6, or 8, and a second binding domain consisting of one antibody variable domain that is cross-species specific and binds to an epitope of a human and a non-chimpanzee primate tumor target antigen, wherein the first binding domain is a VHH domain and comprises CDR 1 of SEQ ID NO: 398, CDR 2 of SEQ ID NO: 399 and CDR 3 of SEQ ID. NO: 400, the process comprising culturing the host cell of claim 25 under conditions allowing the expression of the bispecific single chain antibody molecule and recovering the molecule from the culture.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 4, 2021
From: KUFER, PETER; RAUM, TOBIAS
To: MICROMET AG
Reel/Frame 057078/0456 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 4, 2021
From: KISCHEL, ROMAN; LUTTERBÜSE, RALF; HOFFMANN, PATRICK; KLINGER, MATTHIAS; RAU, DORIS; MANGOLD, SUSANNE
To: AMGEN RESEARCH (MUNICH) GMBH
Reel/Frame 057582/0036 →
CHANGE OF NAME Recorded Aug 4, 2021
From: MICROMET AG
To: AMGEN RESEARCH (MUNICH) GMBH
Reel/Frame 057582/0086 →
Continuity (3)
Continuation 13122280
Provisional Application 61101935 · Oct 1, 2008
Related Publication 20220041736A1 · Feb 10, 2022
Cited By (1)
US 12,577,305