High performance liquid chromatographic determination of 123-I labeled tamoxifen metabolites in human plasma

被引:4
作者
De Vos, F
Van de Wiele, C
Vandecapelle, M
Dierckx, RA
Slegers, G
机构
[1] Univ Hosp Gent, Div Nucl Med, B-9000 Ghent, Belgium
[2] State Univ Ghent, Dept Radiopharm, B-9000 Ghent, Belgium
关键词
tamoxifen; metabolites; I-123;
D O I
10.1016/S0969-8051(01)00195-0
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
A high-performance liquid chromatographic procedure for the quantitation of [I-123]Iodomethyl-N, N-diethyltamoxifen (ITX), a radioligand for human breast cancer imaging, in human plasma is described. Separation was effected on a RP-C18 column, using a mixture of acetonitrile-water-triethylamine (70/30/0.5, v/v). ITX was rapidly cleared from human plasma and metabolites appeared as early as 7.5 min p.i. Quantitative assessment of metabolites in plasma over time allowed recalculation of the ITX plasma time-activity curve. Implications of ITX metabolite formation for breast tumour imaging are discussed. (C) 2001 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:335 / 338
页数:4
相关论文
共 10 条
[1]  
CHERIF A, 1996, J LABELLED COMPD RAD, V60, P338
[2]  
Dickson Robert B., 1997, P1541
[3]   MECHANISMS OF HORMONE RESISTANCE IN BREAST-CANCER [J].
HORWITZ, KB .
BREAST CANCER RESEARCH AND TREATMENT, 1993, 26 (02) :119-130
[4]   IDENTIFICATION OF THE CYTOCHROME-P450 IIIA FAMILY AS THE ENZYMES INVOLVED IN THE N-DEMETHYLATION OF TAMOXIFEN IN HUMAN LIVER-MICROSOMES [J].
JACOLOT, F ;
SIMON, I ;
DREANO, Y ;
BEAUNE, P ;
RICHE, C ;
BERTHOU, F .
BIOCHEMICAL PHARMACOLOGY, 1991, 41 (12) :1911-1919
[5]  
PINK JJ, 1995, DRUGS HORMONAL RESIS, P115
[6]   Biodistribution and dosimetry of (iodine-123)-iodomethyl-N,N-diethyltamoxifen, an (anti)oestrogen receptor radioligand [J].
Van de Wiele, C ;
De Vos, F ;
De Sutter, J ;
Dumont, F ;
Slegers, G ;
Dierckx, RA ;
Thierens, H .
EUROPEAN JOURNAL OF NUCLEAR MEDICINE, 1999, 26 (10) :1259-1264
[7]  
VANDEWIELE C, 2000, UNPUB J NATL CANC I
[8]  
WIEBE VJ, 1995, DRUG HORMONAL RESIST, P115
[9]   IMAGING, BIODISTRIBUTION AND THERAPY POTENTIAL OF HALOGENATED TAMOXIFEN ANALOGS [J].
YANG, DJ ;
LI, C ;
KUANG, LR ;
PRICE, JE ;
BUZDAR, AU ;
TANSEY, W ;
CHERIF, A ;
GRETZER, M ;
KIM, EE ;
WALLACE, S .
LIFE SCIENCES, 1994, 55 (01) :53-67
[10]   HALOGENATED ANALOGS OF TAMOXIFEN - SYNTHESIS, RECEPTOR ASSAY, AND INHIBITION OF MCF7-CELLS [J].
YANG, DJ ;
TEWSON, T ;
TANSEY, W ;
KUANG, LR ;
REGER, G ;
CHERIF, A ;
WRIGHT, KC ;
MOULT, RG ;
TILBURY, RS ;
CHU, K ;
KIM, EE ;
WALLACE, S .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1992, 81 (07) :622-625