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AssigneesLaRegion Wallone, Université Catholique De Louvain
InventorsAndre Trouet, Roger Baurain
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The compound (W—Z—M) according to the invention comprises a component (M) chosen from the group consisting of markers and therapeutic agents possessing an intracellular active site (A.S.), linked to a ligand (W—Z) comprising an arm (Z) linked to a terminal group (W), characterized in that the linkage between the arm (Z) of the ligand (W—Z) and the component (M) prevents intracellular entry of the compound (W—Z—M) and/or inhibits expression of the marker (M), in that said linkage can be selectively cleaved by factors secreted by target cells so as to permit expression of the marker (M) or entry of the therapeutic agent (M) into said target cells, and in that the terminal group (W) provides for the stability of the compound (W—Z—M) in the serum and circulating blood.
Compound (W—Z—M) comprising a component (M) chosen from the group consisting of markers and therapeutic agents possessing an intracellular active site (A.S.), linked to a ligand (W—Z) comprising an arm (Z) linked to a terminal group (W), characterized in that the linkage between the arm (Z) of the ligand (W—Z) and the component (M) prevents intracellular entry of the compound (W—Z—M) and/or inhibits expression of the marker (M), in that said linkage can be selectively cleaved by factors secreted by target cells so as to permit expression of the marker (M) or entry of the therapeutic agent (M) into said target cells, and in that the group (W) provides for the stability of the compound (W—Z—M) in the serum and the circulating blood.
Compound according to any one of the preceding claims, characterized in that the linkage between the component (M) and the arm (Z) of the ligand (W—Z) is a peptide link.
Compound according to any one of the preceding claims, characterized in that the arm (Z) of the ligand (W—Z) is a peptide consisting of at least two optionally substituted amino acids.
Compound according to any one of the preceding claims, characterized in that the therapeutic agents are antitumor therapeutic agents and in that the target cells are tumor cells.
Compound according to any one of the preceding claims, characterized in that the therapeutic agent (M) is chosen from the group consisting of anthracyclines folic acid derivatives, vinca alkaloids, calicheamycin, mitoxantrone, cytosine arabinosides (ARA-C) or adenosine arabinosides (ARA-A), fludarabine phosphate, melphalan, bleomycin, mitomycin, L-canavanine, toxoids, camptothecin and their derivatives, especially TOPOTECAN® (9-dimethylaminomethyl-10-hydroxycamptothecin hydrochloride), and derivatives of fluorochromes, especially rhodamine 123, and their derivatives, optionally linked to a substituted or unsubstituted amino acid.
Dependencies are inferred from the claim text.