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Phase i study, with pharmacokinetic analysis, of intravenous administration of 6-aminochrysene entrapped into sonicated liposomes in patients with advanced cancer

par Soulier, Jean Paul;Brassine, Christiane;Laduron, Chantal;Delcroix, Claude ;Hollaert, Cathy;Coune, André
Référence Journal of liposome research, 1, 2, page (177-193)
Publication Publié, 1989

Article révisé par les pairs

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Résumé :

A phase I study of the intravenous administration of a water-insoluble cytostatic agent, 6-aminochrysene, was performed by using as carriers sonicated liposomes made of egg yolk lecithin, cholesterol, and stearylamine in the molar ratio 4:3:1. Thirteen patients were included in this trial and 47 infusions of liposomes were given. Dosages of 6-aminochrysene per course were escalated from 30 mg/m2 to 200 mg/m2. Courses were repeated every 2 weeks. No limiting toxicity was reached. Tolerance was good. Only slight sedation, nausea and vomiting, venous irritation, and lumbar pain were observed in a few patients. the maximum volume of liposomes infused over 2 hr was 1,196 ml. An objective response with regression of brain and adrenal metastases was observed in a patient with non-small-cell lung cancer. Pharmacokinetic analysis showed that the 6-aminochrysene serum concentration profiles were best fitted by a linear bicompartmental model. This study confirms that sonicated liposomes made of egg yolk lecithin, cholesterol, and stearylamine in the molar ratio 4:3:1 are a safe carrier for the intravenous administration of water-insoluble drugs. © 1989 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.