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.
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