Research ArticlesPharmacokinetics of Cisplatin and Its Monohydrated Complex in Humans
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Activity profile of the cisplatin analogue PN149 in different tumor cell lines
2018, Biochemical PharmacologyCitation Excerpt :For determination of cell number, A498 kidney cancer cells and RT112 bladder cancer cells were treated with the platinum drugs in the concentrations of 10 µM, 20 µM and 50 µM for 1 h and the amount of viable cells was determined 72 h later (Fig. 2A). The chosen concentrations are clinically relevant as plasma concentrations in the range of 10 to 50 µM CDDP have been observed in platinum-treated cancer patients [22–24]. Similar to CDDP, PN149 led to a concentration-dependent decrease of cell number reaching a reduction to about 35% in A498 cells and about 20% in RT112 cells in case of 50 µM (Fig. 2A).
Improving the safety of metal-based drugs by tuning their metabolism with chemoprotective agents
2018, Journal of Inorganic BiochemistryCitation Excerpt :In terms of developing a strategy to mitigate these severe toxic side-effects of CP it is critical to identify which platinum species play an important role. To this end, the MHC is likely to be a key player since a) we have detected this species in human blood plasma within 5 min after the addition of CP [19,20], b) ~ 15% of total platinum in plasma of patients was present as the MHC after a 1-h infusion of cisplatin [21] and c) the MHC is 8-times as toxic as CP [22,23]. Based on the established efficiency CP and the related platinum-based anticancer drugs carboplatin and oxaliplatin as well as their severe toxic-side effects, considerable research efforts are currently underway to enhance the tumor selectivity of Pt-based anticancer drugs to achieve actual benefits for cancer patients.
Apoptosis and Arabinoxylan Rice Bran
2014, Wheat and Rice in Disease Prevention and HealthQuantitative liquid chromatographic determination of intact cisplatin in blood with microwave-assisted post-column derivatization and UV detection
2011, Journal of Pharmaceutical and Biomedical AnalysisCitation Excerpt :Cisplatin-containing blood samples were prepared by adding working solutions of cisplatin (1:100, v/v) to whole blood (room temperature; hematocrit: 0.22–0.52). They were gently vortex-mixed for approximately 5 s, resulting in clinically relevant nominal cisplatin concentrations of 2.48 × 10−7, 4.95 × 10−7, 9.90 × 10−7, 2.48 × 10−6, 4.95 × 10−6, and 9.90 × 10−6 M [11,12]. They were then promptly transferred to cold centrifuge tubes (10 kDa cut-off filter; Centrisart 1, Sartorius, Goettingen, Germany) and kept on ice until subjected to centripetal ultrafiltration (4000 × g; 20 min: 4 °C) within 30 min.
Spectroscopic studies of interactions of chondroitin sulfates with cisplatin
2011, Carbohydrate ResearchCitation Excerpt :In aqueous solution (pH <7.0), it undergoes hydrolysis to form cis-[Pt(NH3)2Cl(H2O)]+ (monoaqua) and cis-[Pt(NH3)2(H2O)2]2+ (diaqua).18 The monoaqua product is generally thought to be the active structure, based on in vivo and in vitro studies.19,20 In order to investigate the contribution of hydrolysis of the chloro ligands to complex formation of CDDP with CS, a comparative study, which involved monitoring the hydrolysis of CDDP in the presence and absence of CSA and CSC in aqueous solution was performed.