IP Library › Granted Patent US 12662549
Granted Patent B2
US 12662549 · App. 18/620,397 · Granted Jun 23, 2026

Binding agents targeting TROP2-expressing tumor cells

Inventors: Wenyang Hou (Montréal, CA); Shugang Yao (Montréal, CA); Luis Da Cruz (Montréal, CA); David S. Young (Montréal, CA)
Assignee: KisoJi Biotechnology Inc.
C07K16/30A61P35/00A61K2039/505C07K2317/524C07K2317/526C07K2317/53C07K2317/565C07K2317/567C07K2317/569C07K2317/732C07K2317/77C07K2317/92
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Quick Facts
Patent No.
US 12662549
App. No.
18/620,397
Granted
Jun 23, 2026
Kind
B2
Abstract

The present disclosure generally relates to binding agents, such as antibodies and antigen binding fragments thereof, that are capable of binding to trophoblast cell surface antigen-2 (TROP2). Also disclosed herein are binding agents that are capable of targeting TROP2-expressing tumor cells and their use for the treatment of cancer. Single domain antibodies that specifically binds to amino acid residues of the extracellular domain of TROP2 are provided.

Claims (24)

1 . A VHH that specifically binds to TROP2 comprising:

a. a CDRH1 having the amino acid sequence set forth in SEQ ID NO:7, a CDRH2 having the amino acid sequence set forth in SEQ ID NO:8 and a CDRH3 having the amino acid sequence set forth in SEQ ID NO:9;

b. a CDRH1 having the amino acid sequence set forth in SEQ ID NO:19, a CDRH2 having the amino acid sequence set forth in SEQ ID NO:20 and a CDRH3 having the amino acid sequence set forth in SEQ ID NO:21;

c. a CDRH1 having the amino acid sequence set forth in SEQ ID NO:56, a CDRH2 having the amino acid sequence set forth in SEQ ID NO:57 and a CDRH3 having the amino acid sequence set forth in SEQ ID NO:58; or

d. a CDRH1 having the amino acid sequence set forth in SEQ ID NO:66, a CDRH2 having the amino acid sequence set forth in SEQ ID NO:67 and a CDRH3 having the amino acid sequence set forth in SEQ ID NO:68.

2 . The VHH of claim 1 , wherein the VHH comprises: an amino acid sequence at least 90%, 95%, or 99% identical to the amino acid sequence set forth in SEQ ID NOs: 24 or 28.

3 . The VHH of claim 2 , wherein the VHH comprises: the amino acid sequence set forth in SEQ ID NOs: 24 or 28.

4 . A single domain antibody (sdAb), wherein the sdAb comprises the VHH of claim 1 .

5 . A pharmaceutical composition comprising the sdAb of claim 4 and a pharmaceutically acceptable carrier.

6 . A nucleic acid encoding the sdAb of claim 4 .

7 . A cell expressing a single domain antibody comprising the VHH of claim 1 .

8 . A single domain antibody (sdAb) that binds to TROP2 comprising two identical polypeptide chains, each comprising a VHH, a hinge domain, a CH2 domain and a CH3 domain, wherein the VHH comprises the amino acid sequence set forth in SEQ ID NOs: 24 or 28.

9 . A multispecific antibody comprising the VHH of claim 1 .

10 . A bispecific antibody comprising the VHH of claim 1 .

11 . The sdAb of claim 4 further comprising a hinge domain, a CH2 domain and a CH3 domain.

12 . The sdAb of claim 11 , wherein the hinge domain, CH2 domain and CH3 domain are human IgG1.

13 . The sdAb of claim 12 , wherein the hinge domain comprises the sequence set forth in SEQ ID NO: 36.

14 . The sdAb of claim 12 , wherein the CH2 domain comprises the sequence set forth in SEQ ID NO: 37.

15 . The sdAb of claim 12 , wherein the CH3 domain comprises the sequence set forth in SEQ ID NO: 38.

16 . The sdAb of claim 4 , wherein the sdAb is a homodimer.

17 . The sdAb of claim 8 , wherein the hinge domain, CH2 domain and CH3 domain are human IgG1.

18 . The sdAb of claim 8 , wherein the hinge domain comprises the sequence set forth in SEQ ID NO: 36.

19 . The sdAb of claim 8 , wherein the CH2 domain comprises the sequence set forth in SEQ ID NO: 37.

20 . The sdAb of claim 8 , wherein the CH3 domain comprises the sequence set forth in SEQ ID NO: 38.