Cytotoxic cd44 antibody immunoconjugates

Details Cytotoxic cd44 antibody immunoconjugates Cytotoxic cd44 antibody immunoconjugates

A - Human Necessities

61

K

A61K 47/48 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2443438

The present in invention relates to novel conjugates of antibodies with cytotoxic compounds, pharmaceutical compositions containing such conjugates, and their use in cancer therapy. In particular, the present invention relates to conjugates of antibodies which are specific for CD44 with maytansinoids, preferably with N2'-deacetyl-N2' (3-mercapto-1-oxopropyl)-maytansine (DM1). In a particularly preferred embodiment, the antibody/maytansinoid conjugate may be prepared from a maytansinoid of formula (II) wherein R1 represents H or SR4, wherein R4 represents methyl, ethy, linear alkyl, branched alkyl, cyclic alkyl, simple or substituted aryl, or heterocyclic; R2 represents CI or H; R3 represents H or CH3; and m represents 1, 2, or 3. PLreferably, R1 is H or CH3, R2 is CI, R3 is CH3, and m=2. The compound with R1=H, R2=CI, R3=CH3, and m=2 is designated DM1 in the literature.

La présente invention concerne de nouveaux conjugués d'anticorps de composés cytotoxiques, des compositions pharmaceutiques contenant lesdits conjugués, et leur utilisation dans le cadre de la thérapie du cancer. En particulier, l'invention a pour objet des conjugués d'anticorps qui sont spécifiques de CD44 avec des maytansinoïdes, de préférence avec N?2¿-désacétyl-N?2¿-(3-mercapto-1-oxopropyl)-maytansine (DM1).

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