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US 12,728,168 B2Granted
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
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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.
Claims28
An antibody drug conjugate, comprising:
- an anti-CEA antibody or an antigen-binding fragment thereof conjugated to a toxin drug 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, wherein:
- (i) the heavy chain variable region comprises a HCDR1, a HCDR2 and a HCDR3 set forth in SEQ ID NO:
- 21, SEQ ID NO:
- 22 and SEQ ID NO:
- 23, respectively, and the light chain variable region comprises a LCDR1, a LCDR2 and a LCDR3 set forth in SEQ ID NO:
- 24, SEQ ID NO:
- 25 and SEQ ID NO:
- 26, respectively;
- or the heavy chain variable region comprises a HCDR1, a HCDR2 and a HCDR3 set forth in SEQ ID NO:
- 21, SEQ ID NO:
- 47 and SEQ ID NO:
- 23, respectively, and the light chain variable region comprises a LCDR1, a LCDR2 and a LCDR3 set forth in SEQ ID NO:
- 24, SEQ ID NO:
- 25 and SEQ ID NO:
- 26, respectively;
- (ii) the heavy chain variable region comprises a HCDR1, a HCDR2 and a HCDR3 set forth in SEQ ID NO:
- 15, SEQ ID NO:
- 16 and SEQ ID NO:
- 17, respectively, and the light chain variable region comprises a LCDR1, a LCDR2 and a LCDR3 set forth in SEQ ID NO:
- 18, SEQ ID NO:
- 19 and SEQ ID NO:
- 20, respectively;
- or the heavy chain variable region comprises an HCDR1, a HCDR2 and a HCDR3 set forth in SEQ ID NO:
- 15, SEQ ID NO:
- 38 and SEQ ID NO:
- 17, respectively, and the light chain variable region comprises a LCDR1, a LCDR2 and a LCDR3 set forth in SEQ ID NO:
- 18, SEQ ID NO:
- 19 and SEQ ID NO:
- 20, respectively;
- (iii) the heavy chain variable region comprises a HCDR1, a HCDR2 and a HCDR3 set forth in SEQ ID NO:
- 27, SEQ ID NO:
- 28 and SEQ ID NO:
- 29, respectively, and the light chain variable region comprises a LCDR1, a LCDR2 and a LCDR3 set forth in SEQ ID NO:
- 30, SEQ ID NO:
- 31 and SEQ ID NO:
- 32, respectively;
- or
- (iv) the heavy chain variable region comprises a HCDR1 and a HCDR3 set forth in SEQ ID NO:
- 33 and SEQ ID NO:
- 34, respectively, and a HCDR2 set forth in SEQ ID NO:
- 16 or SEQ ID NO:
- 38;
- the light chain variable region comprises a LCDR1 and a LCDR3 set forth in SEQ ID NO:
- 35 and SEQ ID NO:
- 37, respectively, and a LCDR2 set forth in SEQ ID NO:
- 36 or SEQ ID NO:
- 64.
44 more elements
Dependencies are inferred from the claim text.