title: Determination of intoplicine, a new antitumour drug, in human whole blood and plasma by normal-phase high-performance liquid chromatography with fluorescence detection.
abstract: Intoplicine, a benzopyrido-indole derivative, is a novel anticancer agent currently under phase I clinical evaluation. A selective, sensitive normal-phase high-performance liquid chromatographic (HPLC) assay with fluorescence detection, suitable for the determination of intoplicine in human plasma and whole blood, is described. The sample pretreatment involves a protein precipitation step with 2-propanol. The reported assay was validated, and the stability of the analyte in plasma, in whole blood and in the extraction fluid was investigated. The method has been implemented in a pharmacokinetic phase I clinical trial with intoplicine given as a 24-h intravenous infusion.
authors.affiliation: Slotervaart Hospital, Amsterdam, Netherlands.
authors.forename: R
authors.initials: R
authors.lastname: van Gijn
authors.forename: H
authors.initials: H
authors.lastname: Rosing
authors.forename: W W
authors.initials: WW
authors.lastname: ten Bokkel Huinink
authors.forename: O
authors.initials: O
authors.lastname: van Tellingen
authors.forename: J B
authors.initials: JB
authors.lastname: Vermorken
authors.forename: A J
authors.initials: AJ
authors.lastname: Liefting
authors.forename: R
authors.initials: R
authors.lastname: Bruno
authors.forename: H M
authors.initials: HM
authors.lastname: Pinedo
authors.forename: J H
authors.initials: JH
authors.lastname: Beijnen
mesh_terms: D000433:1-Propanol; D000970:Antineoplastic Agents / Q000097:blood*; D011232:Chemical Precipitation; D002851:Chromatography, High Pressure Liquid / Q000379:methods* / Q000592:standards / Q000706:statistics & numerical data; D004355:Drug Stability; D004912:Erythrocytes / Q000378:metabolism; D006801:Humans; D007211:Indoles / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics; D007262:Infusions, Intravenous; D011725:Pyridines / Q000008:administration & dosage / Q000097:blood* / Q000493:pharmacokinetics
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D011725:Pyridines; D000433:1-Propanol; C081834:intoplicine