Dmd #3244r Hepatic Uptake of the Novel Antifungal Agent Caspofungin
نویسندگان
چکیده
Division of Clinical Pharmacology, Vanderbilt University School of Medicine, Nashville, TN, USA (W.L., B.F.L., R.B.K.) and Department of Drug Metabolism, Merck Research Laboratories, West Point, PA, USA (P.S., X.X., M.Y., J.A.S., J. H. L., P.G.P). *Current address: Department of Drug Safety and Metabolism, Wyeth Pharmaceuticals, 1 Burtt Road, Andover, MA 01810 **Current address: Department of Pharmacokinetics and Drug Metabolism, Amgen, Thousand Oaks, CA 91320 DMD Fast Forward. Published on February 16, 2005 as doi:10.1124/dmd.104.003244
منابع مشابه
Hepatic uptake of the novel antifungal agent caspofungin.
Caspofungin (CANCIDAS, a registered trademark of Merck & Co., Inc.) is a novel echinocandin antifungal agent used in the treatment of esophageal and invasive candidiases, invasive aspergillosis, and neutropenia. Available data suggest that the liver is a key organ responsible for caspofungin elimination in rodents and humans. Caspofungin is primarily eliminated by metabolic transformation; howe...
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Caspofungin acetate (Cancidas, MK-0991, L-743,872) is a parenteral antifungal agent indicated in the treatment of invasive aspergillosis in patients who are intolerant of or whose infection is refractory to other antifungal therapies. It is the first member of a novel class of antifungals, the echinocandins, to be made available in the USA. As a class, the echinocandins possess a mechanism of a...
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The metabolism, excretion, and pharmacokinetics of caspofungin (Cancidas; Merck & Co., Inc.) were investigated after administration of a single intravenous dose to mice, rats, rabbits, and monkeys. Caspofungin had a low plasma clearance (0.29 to 1.05 ml/min/kg) and a long terminal elimination half-life (11.7 h to 59.7 h) in all preclinical species. The elimination kinetics of caspofungin were m...
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Fungal infection has increased in the past 2 decades in China. There are three classes of antifungal drugs, polyenes, azoles, and echinocandins, that are applied frequently in China. Caspofungin, which disrupts the fungal cell wall glucan formation through inhibiting the enzyme 1,3-β-glucan synthase, is one of the echinocandins. According to the results of clinical practices applied in China, c...
متن کاملIn vitro investigation of the hepatobiliary disposition mechanisms of the antifungal agent micafungin in humans and rats.
The purpose of the present study was to elucidate the transport mechanisms responsible for elimination of micafungin, a new semisynthetic echinocandin antifungal agent, which is predominantly cleared by biliary excretion in humans and rats. In vitro studies using sandwich-cultured rat and human hepatocytes were conducted. Micafungin uptake occurred primarily (∼75%) by transporter-mediated mecha...
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تاریخ انتشار 2005