In vitro characterization of the biotransformation of thiocoraline, a novel marine anti-cancer drug.

作者: Esther F. A. Brandon , Rolf W. Sparidans , Irma Meijerman , Ignasio Manzanares , Jos H. Beijnen

DOI: 10.1023/B:DRUG.0000026250.34645.7F

关键词: BiochemistryIn vitroBiologyUridineThiocoralineCytochrome P450TransferasePharmacologyAnti cancer drugsBiotransformationDrug

摘要: Thiocoraline is a potent new marine anti-cancer drug in vitro, which will be tested phase I clinical studies shortly. To assess the biotransformation and potential implications for human pharmacology toxicology, vitro metabolism of thiocoraline was characterized using plasma, liver preparations, cytochrome P450 (CYP) uridine diphosphoglucuronosyl transferase (UGT) supersomes cell lines.

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