IP Library Granted Patent US 10,501,542
Granted Patent B2
US 10,501,542 · App. 15/353,886 · Granted Dec 10, 2019

CTLA4 binders

Inventors: Juha Punnonen (Belmont, CA); Maribel Beaumont (San Mateo, CA); Marie-Ange Buyse (Merelbeke, BE); Carlo Boutton (Wielsbeke, BE); Bruno Dombrecht (Heusden, BE); Bjorn Victor (Zwijndrecht, BE); Robert A. Kastelein (Portola Valley, CA)
Assignee: Merck Sharp & Dohme Corp.
C07K16/2818A61K39/3955A61K39/39558C07K14/765C07K16/18A61K2039/505A61K2039/54A61K2039/545C07K2317/22C07K2317/24C07K2317/31C07K2317/32C07K2317/33C07K2317/34C07K2317/35C07K2317/565C07K2317/569C07K2317/62C07K2317/76C07K2317/92C07K2319/31
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Quick Facts
Patent No.
US 10,501,542
App. No.
15/353,886
Granted
Dec 10, 2019
Kind
B2
Abstract

The present invention provides molecules, such as ISVDs and Nanobodies, that bind to CTLA4 or human serum albumin. These molecules have been engineered so as to reduce the incidence of binding by pre-existing antibodies in the bodies of a subject administered such a molecule. Methods for increasing immune response, treating cancer and/or treating an infectious disease with such molecules are provided.

Claims (39)

1. A CTLA4 binder comprising one or more immunoglobulin single variable domains (ISVDs) that bind to human CTLA4

wherein the one or more ISVDs independently comprises the amino acid sequence: XVQLVESGGGVVQPGGSLRLSCAASGGTFSFYGMG WFRQAPGKEREFVADIRTSAGRTYYADSVKGRFTISRDNSKNTVYLQMNSLRPEDTALYYCAAEPSGISGWDYWGQG TLVTVSS (SEQ ID NO: 60); and

optionally comprising a half-life extender and/or a C-terminal extender.

2. A CTLA4 binder comprising one or more immunoglobulin single variable domains (ISVDs) that bind to human CTLA4

wherein the one or more ISVDs independently comprises the amino acid sequence selected from SEQ ID NOs: 93-109; and

optionally lacking the signal sequence amino acids AAADYKDHDGDYKDHDIDYKDDDDKGAAHHHHHH (amino acids 120-153 of each of SEQ ID Nos: 93-109) thereof.

3. The CTLA4 binder of claim 1 , wherein the CTLA4 binder comprises a half-life extender.

4. The CTLA4 binder of claim 3 , wherein the half-life extender is an ISVD that binds to human serum albumin.

5. The CTLA4 binder of claim 4 wherein the ISVD that binds to human serum albumin is ALB11002, which has the amino acid sequence set forth in SEQ ID NO: 66.

6. The CTLA4 binder of claim 1 comprising:

an ISVD that binds to human CTLA4 comprising the amino acid sequence set forth in SEQ ID NO: 60; a peptide linker; an ISVD that binds to human CTLA4 comprising the amino acid sequence set forth in SEQ ID NO: 60; a peptide linker; a half-life extender; and, optionally, a C-terminal extension alanine.

7. A CTLA4 binder of claim 1 comprising:

an ISVD that binds to human CTLA4 comprising the amino acid sequence set forth in SEQ ID NO: 60; a peptide linker; a half-life extender; and, optionally, a C-terminal extension alanine.

8. The CTLA4 binder of claim 6 wherein each peptide linker comprises the amino acid sequence GGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGS (SEQ ID NO: 65).

9. An injection device or vessel that comprises the CTLA4 binder of claim 1 and further comprising a therapeutic agent.

10. The CTLA4 binder of claim 1 , wherein the CTLA4 binder comprises at least two ISVDs that bind human CTLA4.

11. A CTLA4 binder comprising one or more immunoglobulin single variable domains (ISVDs) that bind to human CTLA4 which comprises the amino acid sequence:

(SEQ ID NO: 62)

DVQLVESGGGVVQPGGSLRLSCAASGGTFSFYGMG

WFRQAPGKEREFVADIRTSAGRTYYADSVKGRFTISRDNSKNTVYLQMN

SLRPEDTALYYCAAEPSGISGWDYWGQGTLVTVSSGGGGSGGGGSGGGG

SGGGGSGGGGSGGGGSGGGGSEVQLVESGGGVVQPGGSLRLSCAASGGT

FSFYGMGWFRQAPGKEREFVADIRTSAGRTYYADSVKGRFTISRDNSKN

TVYLQMNSLRPEDTALYYCAAEPSGISGWDYWGQGTLVTVSSGGGGSGG

GGSGGGGSGGGGSGGGGSGGGGSGGGGSEVQLVESGGGVVQPGNSLRLS

CAASGFTFSSFGMSWVRQAPGKGLEWVSSISGSGSDTLYADSVKGRFTI

SRDNAKTTLYLQMNSLRPEDTALYYCTIGGSLSRSSQGTLVTVSSA.

12. A pharmaceutical composition comprising the CTLA4 binder of claim 11 and a pharmaceutically acceptable carrier.

13. A pharmaceutical composition comprising the CTLA4 binder of claim 12 and a pharmaceutically acceptable carrier.

14. A CTLA4 binder consisting of SEQ ID NO: 62.

15. A CTLA4 binder comprising one or more immunoglobulin single variable domains (ISVDs) that bind to human which comprises

the amino acid sequence:

(SEQ ID NO: 64)

DVQLVESGGGVVQPGGSLRLSCAASGGTFSFYGMG

WERQAPGKEREEVADIRTSAGRTYYADSVKGRFTISRDNSKNTVYLQMN

SLRPEDTALYYCAAEPSGISGWDYWGQGTLVTVSSGGGGSGGGGSGGGG

SGGGGSGGGGSGGGGSGGGGSEVQLVESGGGVVQPGNSLRLSCAASGET

FSSFGMSWVRQAPGKGLEWVSSISGSGSDTLYADSVKGRFTISRDNAKT

TLYLQMNSLRPEDTALYYCTIGGSLSRSSQGTLVTVSSA.

Assignments (7)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2017
From: PUNNONEN, JUHA; BEAUMONT, MARIBEL; KASTELEIN, ROBERT A.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 042073/0444 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2017
From: BUYSE, MARIE-ANGE; BOUTTON, CARLO; DOMBRECHT, BRUNO; VICTOR, BJORN
To: ABLYNX N.V.
Reel/Frame 042075/0660 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2017
From: ABLYNX N.V.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 042075/0774 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 22, 2016
From: BUYSE, MARIE-ANGE; BOUTTON, CARLO; DOMBRECHT, BRUNO; VICTOR, BJORN
To: ABLYNX N.V.
Reel/Frame 040401/0895 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 22, 2016
From: ABLYNX N.V.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 040402/0301 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 22, 2016
From: PUNNONEN, JUHA; BEAUMONT, MARIBEL
To: MERCK SHARP & DOHME CORP.
Reel/Frame 040401/0448 →
Continuity (2)
Provisional Application 62257001 · Nov 18, 2015
Related Publication 20170137521A1 · May 18, 2017
Cited By (4)
US 50,682 US 12,516,105 US 12,630,609 US 12,662,525