ANTIBODY-CONJUGATES FOR TARGETING OF TUMOURS EXPRESSING TROP-2

The present invention concerns antibody-conjugates which are especially suitable for the targeting of Trop-2-expressing cells, in particular tumour cells. The antibody-conjugates according to the invention have structure (1): Herein, AB is an antibody capable of targeting Trop-2-expressing tumours;...

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Bibliographische Detailangaben
Hauptverfasser:	LELIEVELDT, Lianne, WIJDEVEN, Maria Antonia, VAN DELFT, Floris Louis, VAN BERKEL, Sander Sebastiaan, VAN GEEL, Remon
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	The present invention concerns antibody-conjugates which are especially suitable for the targeting of Trop-2-expressing cells, in particular tumour cells. The antibody-conjugates according to the invention have structure (1): Herein, AB is an antibody capable of targeting Trop-2-expressing tumours; L is a linker that links Z to D; Z is a connecting group; L6 is -GlcNAc(Fuc)w-(G)j-S-(L7)w'-, wherein G is a monosaccharide, j is an integer in the range of 0 - 10, S is a sugar or a sugar derivative, GlcNAc is N- acetylglucosamine and Fuc is fucose, w is 0 or 1, w' is 0, 1 or 2 and L7 is -N(H)C(O)CH2-, -N(H)C(O)CF2- or -CH2-; D is exatecan; b is 0 or 1; x is 1 or 2; and y is 1, 2, 3 or 4. The invention further concerns a method for preparing the antibody-conjugates of structure (1) and application of the antibody-conjugates of structure (1).