Abstract 1294: Metabolism and excretion of eribulin in patients with advanced solid tumors
Autor: | Arturo Lopez-Anaya, Hilde Rosing, Margarita Lymboura, Marja Mergui-Roelvink, Barbara Koetz, Larisa Reyderman, Serena Marchetti, Jan H.M. Schellens, Jos H. Beijnen, A. C. Dubbelman |
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Rok vydání: | 2011 |
Předmět: | |
Zdroj: | Cancer Research. 71:1294-1294 |
ISSN: | 1538-7445 0008-5472 |
Popis: | This Phase I, open-label, mass-balance study investigated the metabolism and excretion of eribulin, a non-taxane microtubule dynamics inhibitor with a novel mechanism of action, in patients with advanced solid tumors. A single 14C-eribulin acetate (∼85 μCi) 2 mg dose was given on Day 1 (cycle 1) as a 2-5-min IV bolus injection to 6 patients ≥18 years with advanced solid tumors that progressed after standard therapy or for which no standard therapy existed. Patients received 1.4 mg/m2 unlabeled eribulin mesylate (E7389) on Day 8 (cycle 1), and Days 1 and 8 of each subsequent 21-day cycle. Blood, urine, and fecal samples were collected from Days 1-8 (cycle 1) at specified time points or until sample radioactivity was Mean plasma eribulin exposure (627 ng.hr/mL) was comparable to that of total radioactivity (568 ng equivalent.hr/mL). Time-matched concentration ratios of eribulin to total radioactivity approached unity in blood and plasma: unchanged parent compound constituted almost all eribulin-derived radioactivity. Few metabolites of eribulin were detected in plasma. Each metabolite represented Overall, no major metabolites of eribulin were detected in plasma. Eribulin is primarily eliminated unchanged in feces, while urine constitutes a minor route of elimination. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 102nd Annual Meeting of the American Association for Cancer Research; 2011 Apr 2-6; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2011;71(8 Suppl):Abstract nr 1294. doi:10.1158/1538-7445.AM2011-1294 |
Databáze: | OpenAIRE |
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