The 2nd International Conference on Drug Discovery & Therapy: Dubai, February 1 - 4, 2010


Session Speaker

New Platinum Drug Dicycloplatin Appears Effective in Treating Brain and Prostate Cancers
Xuqing Yang, Jing Jie Yu, Yi Guo and Michael D. Mueller
USA

Dicycloplatin (DCP) is a new platinum-based drug developed in China. Due to its chemical structure, DCP 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. DCP toxicity profile of 210 mg/kg of LD50 compares favourably to 14.27 mg/kg for cisplatin and 164 mg/kg for carboplatin. In vivo studies indicate that IV administration of 20 mg/kg DCP in rats is followed by drug distributions in the brain and prostate of 3.16 µg/g and 3.64 µg/g, respectively. Histoculture Drug Response Assay (HDRA) indicates clinical efficacy of chemotherapy for various cancer types, including brain and prostate cancers. 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. Five patients with prostate cancer were cured by DCP alone. Polar surface area (PSA) and LogP calculations for estimating solubility and ability to cross the blood-brain barrier (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, USA suggest that DCP induces gene signature profile in human ovarian cancer cells through mechanisms similar to other platinum drugs. In conclusion, dicycloplatin may be an effective chemotherapeutic agent for patients with brain or prostate cancer.

















[Webmaster]   Copyright © 2010 2nd International Conference on Drug Design & Therapy