Modified antibody in which motif comprising cysteine residue is bound, modified antibody-drug conjugate comprising the modified antibody, and production method for same

A method of producing a modified antibody-drug conjugate comprising:

• (a) reacting the modified antibody, wherein the motif of a structure represented by the following formula 1 thereto, with a linker reagent to form an antibody-linker intermediate;
• and
• (b) reacting the intermediate with an active drug moiety to produce modified antibody-drug conjugate:
• Xa-[(MCys)n-Xbn]n Formula (1)
• wherein (MCys)n represents a simple cysteine residue or a peptide motif that contains a cysteine residue and has a specific functionality or a secondary or tertiary structure;
• Xa and Xbn each independently represents a peptide comprising 0 to 20 amino acid residues other than cysteine;
• and n is an integer ranging from 1 to 20.

A method of producing a modified antibody-drug conjugate comprising:

• (a) reacting the nucleophilic group of a drug moiety with a linker reagent to form a drug-linker intermediate;
• and
• (b) reacting the intermediate with a parent antibody comprising the motif bound thereto and
• wherein the motif having a structure represented by the following formula 1:
• Xa-[(MCys)n-Xbn]n Formula (1)
• wherein (MCys)n represents a simple cysteine residue or a peptide motif that contains a cysteine residue and has a specific functionality or a secondary or tertiary structure;
• Xa and Xbn each independently represents a peptide comprising 0 to 20 amino acid residues other than cysteine;
• and n is an integer ranging from 1 to 20.

A method of producing a modified antibody comprising a motif bound to a parent antibody, the method comprising the steps of:

• (a) constructing an expression vector comprising a polynucleotide sequence in which a polynucleotide sequence encoding the motif and a polynucleotide sequence encoding the parent antibody are recombinantly linked to each other;
• (b) expressing the constructed expression vector in a culture using host cells;
• and
• (c) isolating and purifying the modified antibody from the culture,
• wherein the motif has a structure represented by the following formula 1:
• Xa-[(MCys)n-Xbn]n Formula (1)
• wherein (MCys)n represents a simple cysteine residue or a peptide motif that contains a cysteine residue and has a specific functionality or a secondary or tertiary structure;
• Xa and Xbn each independently represents a peptide comprising 0 to 20 amino acid residues other than cysteine;
• and n is an integer ranging from 1 to 20.