Synthesis of 2H- and 13C-labelled sunitinib and its primary metabolite

被引：5

作者：

Elsinghorst, Paul W. ^{[1
]}

Guetschow, Michael ^{[1
]}

机构：

[1] Univ Bonn, Inst Pharmaceut, D-53121 Bonn, Germany

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2009年 / 52卷 / 9-10期

关键词：

sunitinib; carbon-13; deuterium; SU11248; SU12662; TYROSINE KINASE; QUANTITATIVE BIOANALYSIS; SPECTROMETRY; INHIBITOR; DEUTERIUM; MS;

D O I：

10.1002/jlcr.1608

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Sunitinib (Sutent (R), Pfizer) was approved in 2006 for the treatment of gastrointestinal and renal cancer. Isotope-labelled derivatives have already been prepared for PET and ADME radiography. The preparation of C-13- and H-2-labelled internal standards of sunitinib (SU11248) and its primary metabolite (SU12662) for LC-MS analysis of human blood samples is presented.

引用

页码：360 / 365

页数：6

共 20 条

[1] Sunitinib maleate [J].

Atkins, M ;

Jones, CA ;

Kirkpatrick, P .

NATURE REVIEWS DRUG DISCOVERY, 2006, 5 (04) :279-280

[2] Quantitation of SU11248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction [J].

Barattè, S ;

Sarati, S ;

Frigerio, E ;

James, CA ;

Ye, C ;

Zhang, Q .

JOURNAL OF CHROMATOGRAPHY A, 2004, 1024 (1-2) :87-94

[3]

Buckstein R, 2007, Curr Oncol, V14, P154, DOI 10.3747/co.2007.132

[4] Molecular basis for sunitinib efficacy and future clinical development [J].

Faivre, Sandrine ;

Demetri, George ;

Sargent, William ;

Raymond, Eric .

NATURE REVIEWS DRUG DISCOVERY, 2007, 6 (09) :734-745

[5]

GIRIBONE D, 2004, Patent No. 2004012776

[6] LC-MS development strategies for quantitative bioanalysis [J].

Jemal, Mohammed ;

Xia, Yuan-Qing .

CURRENT DRUG METABOLISM, 2006, 7 (05) :491-502

[7] 6-SUBSTITUTED 5-CHLORO-1,3-DIHYDRO-2H-IMIDAZO[4,5-B]PYRAZIN-2-ONES WITH HYPOTENSIVE ACTIVITY [J].

JONES, JH ;

HOLTZ, WJ ;

CRAGOE, EJ .

JOURNAL OF MEDICINAL CHEMISTRY, 1973, 16 (05) :537-542

[8]

KADIN SB, Patent No. 4721712

[9] QUANTITATIVE-ANALYSIS OF EMEPRONIUM BROMIDE BY DEMETHYLATION AND SELECTED ION MONITORING GC-MS [J].

KENNE, L ;

NOREN, B ;

STROMBERG, S .

ACTA CHEMICA SCANDINAVICA SERIES B-ORGANIC CHEMISTRY AND BIOCHEMISTRY, 1988, 42 (01) :59-61

[10] Isotopically labeled analogues for drug quantitation [J].

Liu, RH ;

Lin, DL ;

Chang, WT ;

Liu, CR ;

Tsay, WI ;

Li, JH ;

Kuo, TL .

ANALYTICAL CHEMISTRY, 2002, 74 (23) :618A-626A

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