| 摘要 |
<p>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.</p> |
