rubitecan
rubitecan structure
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Common Name | rubitecan | ||
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| CAS Number | 91421-42-0 | Molecular Weight | 393.350 | |
| Density | 1.6±0.1 g/cm3 | Boiling Point | 816.3±65.0 °C at 760 mmHg | |
| Molecular Formula | C20H15N3O6 | Melting Point | 182-186ºC | |
| MSDS | USA | Flash Point | 447.5±34.3 °C | |
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Effect of injection routes on pharmacokinetics and lactone/carboxylate equilibrium of 9-Nitrocamptothecin in rats.
Int. J. Pharm. 340(1-2) , 29-33, (2007) Pharmacokinetics and lactone/carboxylate equilibrium of 9-Nitrocamptothecin (9-NC) were compared after intravenous (i.v.) and intramuscular (i.m.) injection at a dose of 1.5mg/kg 9-NC solution. The concentrations of three different forms of 9-NC, namely lacto... |
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Effect of phospholipid composition on characterization of liposomes containing 9-nitrocamptothecin.
Drug Dev. Ind. Pharm. 32(6) , 719-26, (2006) 9-Nitrocamptothecin (9-NC), a newly developed camptothecin derivative, had poor solubility in any pharmaceutically acceptable solvents. One way of improving the solubility is to formulate the drug into liposomes. However, 9-NC has low affinity to lipid membra... |
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Sequential oral 9-nitrocamptothecin and etoposide: a pharmacodynamic- and pharmacokinetic-based phase I trial.
Mol. Cancer Ther. 5(8) , 2130-7, (2006) Resistance to topoisomerase (topo) I inhibitors has been related to down-regulation of nuclear target enzyme, whereas sensitization to topo II inhibitors may result from induction of topo II by topo I inhibitors. Here, we evaluated a sequence-specific adminis... |
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9-nitrocamptothecin polymeric nanoparticles: cytotoxicity and pharmacokinetic studies of lactone and total forms of drug in rats.
Anticancer Drugs 19(8) , 805-11, (2008) The objective of this study was to evaluate the cytotoxicity and pharmacokinetics of total and lactone forms of 9-nitrocamptothecin (9-NC), an effective antineoplastic drug, after intravenous injection of drug incorporated into poly (DL-lactic-glycolic acid) ... |
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Anticancer activity of new haloalkyl camptothecin esters against human cancer cell lines and human tumor xenografts grown in nude mice.
Anticancer Agents Med. Chem. 12(7) , 818-28, (2012) All chemotherapeutic agents currently in use have a narrow window of therapeutic index of 1 to 1.2. Camptothecin ester compounds are reported to have a wider therapeutic index when being used to treat human xenografts in nude mice. As a continuous effort in s... |
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Key role of topoisomerase I inhibitors in the treatment of recurrent and refractory epithelial ovarian carcinoma.
Expert Rev. Anticancer Ther. 8(5) , 819-31, (2008) Ovarian cancer remains one of the most difficult gynecologic cancers to treat, owing to its aggressive biology and high relapse rate, as well as the toxic side effects of available chemotherapeutic agents used to treat recurrent disease. Topoisomerase I inhib... |
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Optimal modeling for phase I design of a two drug combination-results of a phase I study of cisplatin with 9-nitrocamptothecin.
Invest. New Drugs 26(6) , 541-51, (2008) Combination of platinum with topoisomerase-I inhibitors are synergistic. The objectives of this study were to determine MTD range and toxicity profile of combinations of oral 9-nitrocamptothecin (9NC) and intravenous cisplatin in patients with refractory soli... |
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A phase I pharmacokinetics study of 9-nitrocamptothecin in patients with advanced solid tumors.
Cancer Chemother. Pharmacol. 67(4) , 955-61, (2011) 9-Nitrocamptothecin (9-NC) is a novel orally administered camptothecin analog. The purpose of this study is to evaluate the pharmacokinetics and safety of 9-nitrocamptothecin in patients with advanced solid tumors.The 23 patients for a single-dose pharmacokin... |
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Phase II study of rubitecan in recurrent or metastatic head and neck cancer.
Cancer Chemother. Pharmacol. 62(2) , 209-14, (2008) Rubitecan is an oral camptothecin analogue that has shown activity against a broad spectrum of human tumor xenografts and has been tested in several diseases.In the present study, 19 patients with incurable, recurrent or metastatic head and neck cancer were t... |
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Lactone stability and tissue distribution of free and liposomal encapsulated 9-nitrocamptothecin in rats following intravenous injection.
Drug Dev. Ind. Pharm. 34(8) , 853-9, (2008) 9-Nitrocamptothecin (9-NC) is a newly developed but poorly soluble derivative of camptothecin (CPT), which has a wide spectrum of anticancer activity in preclinical evaluation. Lactone moiety is a key structural feature for the antitumor activity of CPT analo... |