Targeted
tumor therapy is a perspective procedure to specifically destroy the
cancer tissues with eliminating or at least decreasing the side effects of anticancer drugs. For this purpose the
drug molecule is attached to a targeting moiety (e.g.
peptide hormones) that recognizes
tumor specific or overexpressed receptors on
cancer cells. The in vitro
cytostatic or cytotoxic assays do not give proper information whether the
tumor growth inhibitory effect of the conjugate is better than the activity of the free
drug. Only in vivo studies are adequate to answer this question. However, the selection of the appropriate
tumor model is important to eliminate the false positive results. In our studies a
gonadotropin-releasing hormone analog (
GnRH-III) was applied as targeting moiety in
drug conjugates. The in vivo antitumor activity of these conjugates was investigated on mice bearing subcutaneously or orthotopically szigdeveloped
tumors. The subcutaneously implanted
tumor model which is isolated from its surroundings may provide false results in
tumor growth inhibition. In contrast, the orthotopically developed
tumor is a better model representing appropriate anatomical and clinical status of
cancer. Therefore, the orthotopical
colon cancer developed in our laboratory is a suitable model for the study of the antitumor activity of the conjugates prepared for targeted
tumor therapy.