Depatuxizumab Mafodotin (Genetical Recombination)



Depatuxizumab Mafodotin is an antibody-drug-conjugate (molecular weight: ca. 151,000) consisting of Mafodotin (N-((2R,3R)-3-{(2S)-1-[(3R,4S,5S)-4-({N-[6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl]-N-methyl-L-valyl-L-valyl}methylamino)-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl}-3-methoxy-2-methylpropanoyl)-L-phenylalanine (C₄₉H₇₆N₆O₁₁: molecular weight: 925.16)), which is composed of monomethylauristatin F (N-[(2R,3R)-3-((2S)-1-{(3R,4S,5S)-4-[(N-methyl-L-valyl-L-valyl)methylamino]-3-methoxy-5-methylheptanoyl}pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl]-L-phenylalanine) and 6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl linker, attached to an average of 4 Cys residues of Depatuxizumab (a recombinant monoclonal antibody; molecular weight: ca. 147,000). Depatuxizumab is a humanized and chimeric anti-human epidermal growth factor receptor (EGFR) monoclonal antibody in which the H-chains are composed of complementarity-determining regions derived from mouse anti-human EGFR antibody, human framework regions and human IgG1 constant regions and the L-chains are composed of variable regions derived from mouse anti-human EGFR antibody and human IgG1 constant regions. Depatuxizumab is produced in Chinese hamster ovary cells. Depatuxizumab is a glycoprotein composed of 2 H-chains (γ1-chains) consisting of 446 amino acid residues each and 2 L-chains (κ-chains) consisting of 214 amino acid residues each.

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