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. The 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 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-; The anti-TROP2 antibody comprises the following heavy and light chains: the heavy chain comprises CDRH1 composed of the amino acid sequence of sequence identification number 23, CDRH2 composed of the amino acid sequence of sequence identification number 24, and CDRH3 composed of the amino acid sequence of sequence identification number 25; the light chain comprises CDRL1 composed of the amino acid sequence of sequence identification number 26, CDRL2 composed of the amino acid sequence of sequence identification number 27, and CDRL3 composed of the amino acid sequence of sequence identification number 28; and the isotype of the anti-TROP2 antibody is IgG1.

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. As claimed in any of claims 1 to 3, wherein the antibody-drug conjugate is administered in combination with another cancer treatment agent.

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