IP Library › Granted Patent US 12667557
Granted Patent B2
US 12667557 · App. 16/485,777 · Granted Jun 30, 2026

Method for treating EGFR-TKI-resistant non-small cell lung cancer by administration of anti-HER3 antibody-drug conjugate

Inventors: Kimio Yonesaka (Osaka-Sayama, JP); Kazuhiko Nakagawa (Osaka-Sayama, JP); Kenji Hirotani (Tokyo, JP)
Assignee: DAIICHI SANKYO COMPANY, LIMITED
A61K31/436A61K31/506A61K31/517A61K31/535C07K16/32A61K45/00A61K47/68A61P11/00A61P35/00
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Quick Facts
Patent No.
US 12667557
App. No.
16/485,777
Granted
Jun 30, 2026
Kind
B2
Abstract

[Problem] To provide a therapeutic agent and a therapeutic method for EGFR-TKI-resistant non-small cell lung cancer. [Solution] Provided are: a therapeutic agent that contains an anti-HER3 antibody-drug conjugate as an active ingredient, or a therapeutic method characterized by administering an anti-HER3 antibody-drug conjugate.

Claims (23)

1 . A therapeutic method for osimertinib-resistant non-small cell lung cancer, comprising administering an anti-HER3 antibody-drug conjugate to a human subject in need thereof.

2 . The therapeutic method according to claim 1 , wherein the non-small cell lung cancer is EGFR T790M mutation-negative non-small cell lung cancer.

3 . The therapeutic method according to claim 2 , wherein the osimertinib-resistant non-small cell lung cancer is further resistant to gefitinib, erlotinib or afatinib.

4 . The therapeutic method according to claim 2 , wherein the osimertinib-resistant non-small cell lung cancer is further resistant to gefitinib or erlotinib.

5 . The therapeutic method according to claim 1 , wherein the osimertinib-resistant non-small cell lung cancer is further resistant to gefitinib, erlotinib, afatinib, or a combination thereof.

6 . The therapeutic method according to claim 1 , wherein the non-small cell lung cancer expresses HER3.

7 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody-drug conjugate is an anti-HER3 antibody-drug conjugate in which a drug-linker represented by the following formula:

wherein A represents the connecting position to an anti-HER3 antibody,

is conjugated to the anti-HER3 antibody via a thioether bond.

8 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody is an antibody comprising a heavy chain comprising CDRH1 consisting of the amino acid sequence represented by SEQ ID NO:1, CDRH2 consisting of the amino acid sequence represented by SEQ ID NO:2, and CDRH3 consisting of the amino acid sequence represented by SEQ ID NO:3, and a light chain comprising CDRL1 consisting of the amino acid sequence represented by SEQ ID NO:4, CDRL2 consisting of the amino acid sequence represented by SEQ ID NO:5, and CDRL3 consisting of the amino acid sequence represented by SEQ ID NO:6.

9 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody is an antibody comprising a heavy chain comprising a heavy chain variable region consisting of the amino acid sequence represented by SEQ ID NO:7, and a light chain comprising a light chain variable region consisting of the amino acid sequence represented by SEQ ID NO:8.

10 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody is an antibody comprising a heavy chain consisting of the amino acid sequence represented by SEQ ID NO:9, and a light chain consisting of the amino acid sequence represented by SEQ ID NO:10.

11 . The therapeutic method according to claim 10 , wherein the anti-HER3 antibody lacks a lysine residue at the carboxyl terminus of the heavy chain.

12 . The therapeutic method according to claim 1 , wherein the average number of units of the drug-linker conjugated per antibody molecule in the anti-HER3 antibody-drug conjugate is in the range of 7 to 8.

13 . The therapeutic method according to claim 1 , wherein the average number of units of the drug-linker conjugated per antibody molecule in the anti-HER3 antibody-drug conjugate is in the range of 7.5 to 8.

14 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody-drug conjugate is administered in combination with a second drug.

15 . The therapeutic method according to claim 14 , wherein the second drug is gefitinib, erlotinib, afatinib, or osimertinib.

16 . The therapeutic method according to claim 15 , wherein the second drug is erlotinib.

17 . The therapeutic method according to claim 15 , wherein the second drug is osimertinib.

18 . The therapeutic method according to claim 1 , wherein the anti-HER3 antibody-drug conjugate comprises a drug-linker conjugated to an antibody via a thioether bond, wherein the antibody-drug conjugate releases a drug having a structure of:

19 . The therapeutic method according to claim 18 , wherein the anti-HER3 antibody-drug conjugate is administered in combination with a second drug.

20 . The therapeutic method according to claim 19 , wherein the second drug is gefitinib, erlotinib, afatinib, or osimertinib.

21 . The therapeutic method according to claim 20 , wherein the second drug is osimertinib.