In view of findings that various tumors express receptors for somatostatin, a new targeted cytotoxic analog of somatostatin, AN-162 (AEZS-124), consisting of doxorubicin linked through glutaric acid to the somatostatin octapeptide RC-121 was developed in our laboratory. We studied the toxicity in vivo and the effect of AN-162 on growth of the MDA-MB-231 estrogen-independent human breast cancer cell line xenografted into nude mice. AN-162 induced significant tumor growth inhibition compared with the control and the group treated with doxorubicin in equimolar doses. We also evaluated the stability of AN-162 in various sera in vitro, as this conjugate is susceptible to hydrolysis by serum carboxylesterase enzymes in the circulation. This study shows for the first time that AN-162 is a safe and effective compound for the treatment of experimental breast cancer. Our findings support the concept of targeted chemotherapy based on cytotoxic peptide analog AN-162 for the treatment of breast cancers and other cancers expressing
Preclinical evaluation of properties of a new targeted cytotoxic somatostatinanalog, AN-162 (AEZS-124), and its effects on tumor growth inhibition. / Seitz S; Schally AV; Treszl A; Papadia A; Rick F; Szalontay L; Szepeshazi K; Ortmann O; Halmos G; Hohla F; Buchholz S.. - STAMPA. - 20(2009), pp. 553-558.