Use of antibody drug conjugate

Abstract

The present invention provides an antitumor drug with excellent antitumor efficacy and safety profile, and superior therapeutic effect. An anti-TROP2 antibody is provided, comprising: CDRH1 composed of an amino acid sequence of sequence identification number 23, CDRH2 composed of an amino acid sequence of sequence identification number 24, and CDRH3 composed of an amino acid sequence of sequence identification number 25 in the variable region of its heavy chain; and CDRL1 composed of an amino acid sequence of sequence identification number 26, CDRL2 composed of an amino acid sequence of sequence identification number 27, and CDRL3 composed of an amino acid sequence of sequence identification number 28 in the variable region of its light chain.

Claims

1. Use of an antibody-drug conjugate in the manufacture of a medicament for treating lung cancer, wherein the antibody-drug conjugate comprises a linker and a drug linked to an anti-TROP2 antibody as shown in the following formula: -(succinimine-3-yl-N)-CH2CH2CH2CH2CH2-C(=O)-GGFG-NH-CH2-O-CH2-C(=O)-(NH-DX) wherein -(succinimine-3-yl-N)- has the structure shown in the following formula: , which binds to the anti-TROP2 antibody via a thioether bond at its 3rd position, and binds to a methylene group within the linker structure containing it at the nitrogen atom at the 1st position; -(NH-DX) represents the following group: , wherein the nitrogen atom of the amino group at the 1st position is the binding site; -GGFG- represents a tetrapeptide residue of -Gly-Gly-Phe-Gly-; wherein the anti-TROP2 antibody comprises SEQ ID The antibody is a humanized monoclonal antibody consisting of the heavy chain variable region composed of amino acid sequences at positions 20 to 140 of SEQ ID NO: 12 and the light chain variable region composed of amino acid sequences at positions 21 to 129 of SEQ ID NO:

18.

2. As requested in claim 1, wherein the average number of units in the drug-linker structure bound to each antibody is in the range of 2 to 8.

3. As requested in claim 1, wherein the average number of units in the drug-linker structure bound to each antibody is in the range of 3 to 8.

4. The use as claimed in any of claims 1 to 3, wherein the antibody-drug conjugate is administered in combination with other cancer treatment agents.

Images