Abstract A172: Dicycloplatin in cancer

Abstract

Abstract Dicycloplatin (DCP) is a new platinum-based drug developed in China. It possesses superior stability and water-solubility compared to cisplatin and carboplatin. Experimental findings in China demonstrate in vitro cytotoxicity of dicycloplatin against a variety of human cancer cell lines and significant in vivo antitumor activity in mouse tumor models. DCP toxicity profile of 210 mg/kg of LD50 compares favourably to 14.27 mg/kg for cisplatin and 164 mg/kg for carboplatin. Histoculture Drug Response Assay (HDRA) indicates clinical efficacy of chemotherapy for various cancer types including brain cancer. Pre-clinical and clinical studies in China suggest that DCP produces fewer side effects with a maximum tolerated dose of 650 mg/m2. In one case, DCP with radiotherapy successfully treated a lung cancer patient with brain metastasis. Polar surface area (PSA) and LogP calculations for estimating solubility and ability to cross the BBB indicate that DCP possesses the largest PSA (132) and CLogP (1), compared to carboplatin (106.2; −0.34) and cisplatin (53.6; −2.5). Investigations of molecular mechanisms at WVU suggest that DCP induces gene signature profile in human ovarian cancer cells through mechanisms similar to other platinum drugs. Citation Information: Mol Cancer Ther 2009;8(12 Suppl):A172.