Antibody-drug conjugates and immunotoxins
AssigneeOncomatryx Biopharma, S.L.
InventorsRoland Kontermann, Klaus Pfizenmaier, Cristina Ferrer, Myriam Fabre, Laureano Simon
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Abstract
The present invention relates to conjugates, in particular antibody-drug conjugates and immunotoxins, having the formula I: A-(L-D)p (I) or a pharmaceutically acceptable salts or solvates thereof, wherein: A is an antibody that selectively binds FAP; L is a linker; D is a drug comprising a cytolysin or a Nigrin-b A-chain; and p is 1 to 10, and to use of such conjugates in the therapeutic treatment of tumors. Methods of producing such conjugates and components for use in such methods are disclosed.
Claims17
A conjugate having the formula I:
- A-(L-D)p (I)
- or a pharmaceutically acceptable salt or solvate thereof,
- wherein:
- A is an antibody that selectively binds FAP;
- L is a linker comprising a spacer;
- D is a drug comprising a cytolysin of formula IV:
- wherein:
- R2 is H or C1-C4 alkyl;
- R6 is C1-C6 alkyl;
- R7 is C1-C6 alkyl, CH2OR19 or CH2OCOR20, wherein R19 is alkyl, R20 is C2-C6-alkenyl, phenyl, or CH2-phenyl;
- R9 is C1-C6 alkyl;
- R10 is H, OH, O-alkyl or O-acetyl;
- f is 1 or 2;
- R11 has the following structure:
- R21
- wherein
- R21 is H, OH, halogen, NH2, alkyloxy, phenyl, alkyl amino or dialkyl amino;
- R16 is H or a C1-C6-alkyl group;
- n=2, 3 or 4;
- q is 0, 1, 2 or 3;
- and
- p is 1 to 10.
A conjugate having the formula I:
- A-(L-D)p (I)
- or a pharmaceutically acceptable salt or solvate thereof,
- wherein:
- A is an antibody that selectively binds FAP;
- L is a linker;
- D is a drug having the structure:
- wherein p is 1 to 10.
Dependencies are inferred from the claim text.