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US 2026/0232830 A1Published application
Antigen binding molecule specifically binding to egfr and muc1, drug conjugate thereof, and medical use thereof
AssigneesJiangsu Hengrui Pharmaceuticals Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
InventorsZiheng Liu, Bing Hu, Le Sun, Shimeng Liu, Xinyu Gao, Xun Li, Liqun Cao, Xin Ye, Feng He
Life of this patent
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Abstract
The present invention relates to an antigen binding molecule specifically binding to EGFR and MUC1, a drug conjugate thereof, and a medical use thereof. Specifically, the present invention relates to an anti-MUC1 antibody or an antigen binding fragment thereof, an anti-EGFR antibody or an antigen binding fragment thereof, an antigen binding molecule specifically binding to EGFR and MUC1, a drug conjugate thereof, and a medical use thereof.
Claims31
An anti-MUC1 antibody or an antigen-binding fragment thereof, comprising a heavy chain variable region and a light chain variable region, wherein the heavy chain variable region comprises a HCDR1, a HCDR2, and a HCDR3, and the light chain variable region comprises a LCDR1, a LCDR2, and a LCDR3, wherein:
- a. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 in SEQ ID NO:
- 4, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 5, respectively;
- or
- b. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 of any one of SEQ ID NO:
- 6 or 47, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 7, respectively;
- or
- c. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 in SEQ ID NO:
- 8, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 9, respectively;
- or
- d. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 of any one of SEQ ID NO:
- 63, 10, or 64, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 11, respectively.
12 more elements
An any-EGFR antibody or an antigen-binding fragment thereof, comprising a heavy chain variable region and a light chain variable region, wherein the heavy chain variable region comprises a HCDR1, a HCDR2, and a HCDR3, and the light chain variable region comprises a LCDR1, a LCDR2, and a LCDR3, wherein:
- a. in the heavy chain variable region, the HCDR1 comprises the amino acid sequence of SEQ ID NO:
- 116, the HCDR2 comprises the amino acid sequence of SEQ ID NO:
- 117, and the HCDR3 comprises the amino acid sequence of SEQ ID NO:
- 129, 128, 130, or 131;
- and in the light chain variable region, the LCDR1 comprises the amino acid sequence of SEQ ID NO:
- 119, the LCDR2 comprises the amino acid sequence of SEQ ID NO:
- 120, and the LCDR3 comprises the amino acid sequence of SEQ ID NO:
- 121;
- or
- b. in the heavy chain variable region, the HCDR1 comprises the amino acid sequence of SEQ ID NO:
- 126 or 133, the HCDR2 comprises the amino acid sequence of SEQ ID NO:
- 117, and the HCDR3 comprises the amino acid sequence of SEQ ID NO:
- 118;
- and in the light chain variable region, the LCDR1 comprises the amino acid sequence of SEQ ID NO:
- 119, the LCDR2 comprises the amino acid sequence of SEQ ID NO:
- 120, and the LCDR3 comprises the amino acid sequence of SEQ ID NO:
- 121;
- or
- c. in the heavy chain variable region, the HCDR1 comprises the amino acid sequence of SEQ ID NO:
- 116, the HCDR2 comprises the amino acid sequence of SEQ ID NO:
- 127, 132, or 134, and the HCDR3 comprises the amino acid sequence of SEQ ID NO:
- 118;
- and in the light chain variable region, the LCDR1 comprises the amino acid sequence of SEQ ID NO:
- 119, the LCDR2 comprises the amino acid sequence of SEQ ID NO:
- 120, and the LCDR3 comprises the amino acid sequence of SEQ ID NO:
- 121;
- or
- d. in the heavy chain variable region, the HCDR1 comprises the amino acid sequence of SEQ ID NO:
- 126, the HCDR2 comprises the amino acid sequence of SEQ ID NO:
- 127, and the HCDR3 comprises the amino acid sequence of SEQ ID NO:
- 118;
- and in the light chain variable region, the LCDR1 comprises the amino acid sequence of SEQ ID NO:
- 119, the LCDR2 comprises the amino acid sequence of SEQ ID NO:
- 120, and the LCDR3 comprises the amino acid sequence of SEQ ID NO:
- 121;
- e. in the heavy chain variable region, the HCDR1 comprises the amino acid sequence of SEQ ID NO:
- 126, the HCDR2 comprises the amino acid sequence of SEQ ID NO:
- 117, and the HCDR3 comprises the amino acid sequence of SEQ ID NO:
- 128, 129, 130, or 131;
- and in the light chain variable region, the LCDR1 comprises the amino acid sequence of SEQ ID NO:
- 119, the LCDR2 comprises the amino acid sequence of SEQ ID NO:
- 120, and the LCDR3 comprises the amino acid sequence of SEQ ID NO:
- 121.
40 more elements
An antigen-binding molecule that specifically binds to EGFR and MUC1, comprising:
- at least one antigen-binding moiety that specifically binds to EGFR, and
- at least one antigen-binding moiety that specifically binds to MUC1, wherein:
- the antigen-binding moiety that specifically binds to EGFR comprises a heavy chain variable region EGFR-VH and a light chain variable region EGFR-VL, and
- the antigen-binding moiety that specifically binds to MUC1 comprises a heavy chain variable region MUC1-VH and a light chain variable region MUC1-VL, wherein:
- a. the EGFR-VH comprises a HCDR1 comprising the amino acid sequence of SEQ ID NO:
- 116, a HCDR2 comprising the amino acid sequence of SEQ ID NO:
- 117, and a HCDR3 comprising the amino acid sequence of SEQ ID NO:
- 129, 128, 130, or 131, and the EGFR-VL comprises a LCDR1 comprising the amino acid sequence of SEQ ID NO:
- 119, a LCDR2 comprising the amino acid sequence of SEQ ID NO:
- 120, and a LCDR3 comprising the amino acid sequence of SEQ ID NO:
- 121;
- or
- b. the EGFR-VH comprises a HCDR1 comprising the amino acid sequence of SEQ ID NO:
- 126 or 133, a HCDR2 comprising the amino acid sequence of SEQ ID NO:
- 117, and a HCDR3 comprising the amino acid sequence of SEQ ID NO:
- 118, and the EGFR-VL comprises a LCDR1 comprising the amino acid sequence of SEQ ID NO:
- 119, a LCDR2 comprising the amino acid sequence of SEQ ID NO:
- 120, and a LCDR3 comprising the amino acid sequence of SEQ ID NO:
- 121;
- or
- c. the EGFR-VH comprises a HCDR1 comprising the amino acid sequence of SEQ ID NO:
- 116, a HCDR2 comprising the amino acid sequence of SEQ ID NO:
- 127, 132, or 134, and a HCDR3 comprising the amino acid sequence of SEQ ID NO:
- 118, and the EGFR-VL comprises a LCDR1 comprising the amino acid sequence of SEQ ID NO:
- 119, a LCDR2 comprising the amino acid sequence of SEQ ID NO:
- 120, and a LCDR3 comprising the amino acid sequence of SEQ ID NO:
- 121;
- or
- d. the EGFR-VH comprises a HCDR1 comprising the amino acid sequence of SEQ ID NO:
- 126, a HCDR2 comprising the amino acid sequence of SEQ ID NO:
- 127, and a HCDR3 comprising the amino acid sequence of SEQ ID NO:
- 118, and the EGFR-VL comprises a LCDR1 comprising the amino acid sequence of SEQ ID NO:
- 119, a LCDR2 comprising the amino acid sequence of SEQ ID NO:
- 120, and a LCDR3 comprising the amino acid sequence of SEQ ID NO:
- 121;
- e. the EGFR-VH comprises a HCDR1 comprising the amino acid sequence of SEQ ID NO:
- 126, a HCDR2 comprising the amino acid sequence of SEQ ID NO:
- 117, and a HCDR3 comprising the amino acid sequence of SEQ ID NO:
- 128, 129, 130, or 131, and the EGFR-VL comprises a LCDR1 comprising the amino acid sequence of SEQ ID NO:
- 119, a LCDR2 comprising the amino acid sequence of SEQ ID NO:
- 120, and a LCDR3 comprising the amino acid sequence of SEQ ID NO:
- 121;
- and
- the heavy chain variable region MUC1-VH comprises a HCDR1, a HCDR2, and a HCDR3, and the light chain variable region MUC1-VL comprises a LCDR1, a LCDR2, and a LCDR3, wherein:
- a. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 in SEQ ID NO:
- 4, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 5, respectively;
- or
- b. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 of any one of SEQ ID NO:
- 6 or 47, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 7, respectively;
- or
- c. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 in SEQ ID NO:
- 8, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 9, respectively;
- or
- d. the HCDR1, HCDR2, and HCDR3 of the heavy chain variable region comprise the amino acid sequences of a HCDR1, a HCDR2, and a HCDR3 of any one of SEQ ID NO:
- 63, 10, or 64, respectively, and the LCDR1, LCDR2, and LCDR3 of the light chain variable region comprise the amino acid sequences of a LCDR1, a LCDR2, and a LCDR3 in SEQ ID NO:
- 11, respectively.
56 more elements
Dependencies are inferred from the claim text.