Coupling of an anti-tumor to an antibody using glutaraldehyde preactivated anti-tumor agent
AssigneeUniversite Laval
InventorsMichel Page, Denis Thibeault
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Abstract
The present invention relates to antitumor compounds of the formula I: ##STR1## wherein M is selected from the group consisting of an hydrogen atom, a peptide residue, and a protein residue linked to the carbon atom via the amino residue of .epsilon.-lysine present therein which can be an antibody used to target the anti-tumor agent to the malignant cells, and R can be an antitumor agent such as daunorubicin, doxorubicin, or an epirublicin derivative.
Claims6
A method of preparing compounds of formula I ##STR5## wherein M is selected from the group consisting of a peptide residue, and a protein residue linked to the carbon atom via an amino residue of .epsilon.-lysine present therein, and wherein R represents an anti-tumor agent residue, which comprises the steps of:
- a reacting said antitumor agent with glutaraldehyde;
- b purifying the activated product by extraction with dichloromethane;
- and
- c reacting the drug-glutaraldehyde complex of step a) with a peptide or a protein M.
The method according to claim 11, wherein M is a peptide selected from the group consisting of anti-carcinoembryonic monoclonal, anti-carcinoembryonic polyclonal antibody, anti-alphafetoprotein monoclonal, anti-alphafetoprotein polyclonal antibody, anti-embryonic pre-albumin monoclonal antibody, human transferrin and Lys3-bombesin.
Dependencies are inferred from the claim text.