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US 2023/0055408 A1Published application
Anti-cea antibody-exatecan analog conjugate and pharmaceutical use thereof
AssigneesJiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
InventorsHua YING, Langyong MAO, Sijia WANG
Life of this patent
Estimating the term…
Abstract
An anti-CEA antibody-exatecan analog conjugate and a pharmaceutical use thereof. Specifically, the anti-CEA antibody-exatecan analog conjugate is as shown in general formula (Pc-L-Y-D), wherein Pc is an anti-CEA antibody or an antigen-binding fragment thereof; L is a linker unit; Y is selected from —O—(CRaRb)m—CR1R2—C(O)—, —O—CR1R2—(CRaRb)m—, —O—CR1R2—, —NH—(CRaRb)m—CR1R2—C(O)—, and —S—(CRaRb)m—CR1R2—C(O); and n is a decimal or integer from 1 to 10.
Claims24
An antibody drug conjugate, comprising:
- an anti-CEA antibody or an antigen-binding fragment thereof conjugated to a toxin drug optionally by a linker, wherein the anti-CEA antibody or the antigen-binding fragment thereof comprises a heavy chain variable region and a light chain variable region of the antibody, wherein:
- i) the HCDR1 and the HCDR3 of the heavy chain variable region are identical to a HCDR1 and a HCDR3 of a heavy chain variable region set forth in SEQ ID NO:
- 9, and the HCDR2 of the heavy chain variable region is identical to a HCDR2 of the heavy chain variable region set forth in SEQ ID NO:
- 9 or differs therefrom by one amino acid;
- the LCDR1, the LCDR2 and the LCDR3 of the light chain variable region are identical to a LCDR1, a LCDR2 and a LCDR3 of a light chain variable region set forth in SEQ ID NO:
- 10:
- ii) a HCDR1 and a HCDR3 of the heavy chain variable region are identical to a HCDR1 and a HCDR3 of a heavy chain variable region set forth in SEQ ID NO:
- 7, and a HCDR2 of the heavy chain variable region is identical to a HCDR2 of the heavy chain variable region set forth in SEQ ID NO:
- 7 or differs therefrom by one amino acid;
- a LCDR1, a LCDR2 and a LCDR3 of the light chain variable region are identical to a LCDR1, a LCDR2 and a LCDR3 of a light chain variable region set forth in SEQ ID NO:
- 8;
- iii) the HCDR1, the HCDR2 and the HCDR3 of the heavy chain variable region are identical to an HCDR1, an HCDR2 and an HCDR3 of a heavy chain variable region set forth in SEQ ID NO:
- 11;
- the LCDR1, the LCDR2 and the LCDR3 of the light chain variable region are identical to a LCDR1, a LCDR2 and a LCDR3 of a light chain variable region set forth in SEQ ID NO:
- 12;
- or
- iv) the HCDR1 and the HCDR3 of the heavy chain variable region are identical to a HCDR1 and a HCDR3 of a heavy chain variable region set forth in SEQ ID NO:
- 13, and the HCDR2 of the heavy chain variable region is identical to a HCDR2 of the heavy chain variable region set forth in SEQ ID NO:
- 13 or differs therefrom by one amino acid;
- the LCDR1 and the LCDR3 of the light chain variable region are identical to a LCDR1 and a LCDR3 of a light chain variable region set forth in SEQ ID NO:
- 14, and the LCDR2 of the light chain variable region is identical to a LCDR2 of the light chain variable region set forth in SEQ ID NO:
- 14 or differs therefrom by one amino acid.
19 more elements
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Dependencies are inferred from the claim text.