Lobaplatin, one of the third-generation
platinum compounds, has shown encouraging anticancer activity in a variety of
tumor types. However, the efficacy of
lobaplatin in
ovarian cancer has not been systemically evaluated. In this study,
lobaplatin as a single agent and in combination with
taxanes was investigated in-vitro and in an in vitro model of ovarian
carcinoma. Using the
sulforhodamine B (SRB) assay, the cytotoxic effects of
lobaplatin alone and in combination with
taxanes were compared with
cisplatin and
carboplatin in seven
ovarian cancer cell lines. In addition, in-vitro antitumor activities were evaluated with
cisplatin-sensitive and
cisplatin-resistant human
ovarian cancer xenografts in nude mice. The cytotoxicity of
lobaplatin was similar to or higher than that of
cisplatin and
carboplatin, with IC50 values from 0.9 to 13.8 μmol/L in a variety of
ovarian cancer cells. The combination of
lobaplatin with
docetaxel yielded enhanced cytotoxic activity in vitro. In addition, in
platinum-sensitive
ovarian cancer xenografts,
lobaplatin alone showed similar antitumor activity to
cisplatin and
carboplatin. Furthermore,
lobaplatin alone or in combination with
docetaxel exhibited significant activity in
platinum-resistant
ovarian cancer xenografts. These results indicate that the use of
lobaplatin alone or in combination with
docetaxel might be a rational and novel therapeutic strategy for
ovarian cancer. Further clinical development of
lobaplatin is clearly warranted.