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US 12,564,641 B2Granted
Eribulin antibody-drug conjugates and methods of use
AssigneeEisai R&D Management Co., Ltd.
InventorsEarl F. Albone, Jared Spidel
Life of this patent
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Abstract
Antibodies, antigen-binding fragments, and conjugates (e.g., antibody-drug conjugates such as those comprising eribulin) thereof that bind to mesothelin are disclosed. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering the compositions provided herein.
Claims32
An antibody-drug conjugate of Formula (I):
- Ab-(L-D)p (I)
- wherein
- Ab is an antibody or antigen-binding fragment, wherein the antibody or antigen-binding fragment is capable of binding to mesothelin and comprises three heavy chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 1 (HCDR1), SEQ ID NO:
- 2 (HCDR2), and SEQ ID NO:
- 3 (HCDR3);
- and three light chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 4 (LCDR1), SEQ ID NO:
- 5 (LCDR2), and SEQ ID NO:
- 6 (LCDR3), as defined by the Kabat numbering system;
- or three heavy chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 7 (HCDR1), SEQ ID NO:
- 8 (HCDR2), and SEQ ID NO:
- 9 (HCDR3);
- and three light chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 10 (LCDR1), SEQ ID NO:
- 11 (LCDR2), and SEQ ID NO:
- 12 (LCDR3), as defined by the IMGT numbering system;
- D is a therapeutic agent;
- L is a cleavable linker that covalently attaches Ab to D;
- and
- p is an integer from 1 to 8.
19 more elements
An antibody-drug conjugate of Formula (I):
- Ab-(L-D)p (I)
- wherein
- Ab is an antibody or antigen-binding fragment, wherein the antibody or antigen-binding fragment is capable of binding to mesothelin and comprises three heavy chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 1 (HCDR1), SEQ ID NO:
- 2 (HCDR2), and SEQ ID NO:
- 3 (HCDR3);
- and three light chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 4 (LCDR1), SEQ ID NO:
- 5 (LCDR2), and SEQ ID NO:
- 6 (LCDR3), as defined by the Kabat numbering system;
- or three heavy chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 7 (HCDR1), SEQ ID NO:
- 8 (HCDR2), and SEQ ID NO:
- 9 (HCDR3);
- and three light chain complementarity determining regions comprising amino acid sequences of SEQ ID NO:
- 10 (LCDR1), SEQ ID NO:
- 11 (LCDR2), and SEQ ID NO:
- 12 (LCDR3), as defined by the IMGT numbering system;
- D is eribulin;
- L is a cleavable linker comprising Mal-(PEG)2-Val-Cit-pAB;
- and
- p is an integer from 1 to 8.
19 more elements
Dependencies are inferred from the claim text.