Validation and application of a liquid chromatography-tandem mass spectrometric method for the determination of GDC-0879 and its metabolite in dog plasma using solid phase extraction

被引：4

作者：

Chou, Bilin

Adler, Ryan S. ^{[2
]}

Meng, Min ^{[2
]}

Percey, Shaundel ^{[2
]}

Dean, Brian

Hop, Cornelis E. C. A.

Shin, Young G. ^{[1
]}

机构：

[1] Genentech Inc, Drug Metab & Pharmacokinet, Dept Drug Metab & Pharmacokinet, San Francisco, CA 94080 USA

[2] Tandem Labs, Salt Lake City, UT 84124 USA

来源：

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS | 2012年 / 70卷

关键词：

LC-MS/MS; Validation; Dog plasma; GDC-0879; B-RAF KINASE; INHIBITORS; CANCER; PATHWAY; EFFICACY; GROWTH; POTENT; TARGET;

D O I：

10.1016/j.jpba.2012.05.029

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

A liquid-chromatographic-tandem mass spectrometric (LC-MS/MS) method was developed and validated for the determination of GDC-0879 and its ketone metabolite (M1) in dog plasma to support preclinical toxicokinetic evaluation. The method consisted of solid phase extraction for sample preparation and LC-MS/MS analysis in positive ion mode using electrospray ionization for analysis. D-4-GDC-0879 and C-13(2)-D-2-M1 were used as internal standards. A quadratic regression (weighted 1/concentration(2)) was used to fit calibration curves over the concentration range of 1-1000 ng/ml for both GDC-0879 and M1. The accuracy (%bias) at the lower limit of quantitation (LLOQ) was 12.0% and 2.0% for GDC-0879 and M1, respectively. The precision (%CV) for samples at the LLOQ was 11.3% and 2.6% for GDC-0879 and M1, respectively. For quality control samples at 3.00, 400 and 800 ng/ml, the between run %CV was <= 3.9% for GDC-0879 and <= 2.4% for M1. Between run %bias ranged from 4.6 to 12.0% for GDC-0879 and from -0.8 to 2.7% for M1. GDC-0879 and M1 were stable in dog plasma for at least 44 days at -70 degrees C. (C) 2012 Elsevier B.V. All rights reserved.

引用

页码：354 / 361

页数：8

共 13 条

[1]

[Anonymous], 2001, BAM (Bacteriological Analytical Manual), Rapid Methods for Detection Foodborne Pathogens, P1

[2] Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species [J].

Choo, E. F. ;

Driscoll, J. P. ;

Feng, J. ;

Liederer, B. ;

Plise, E. ;

Randolph, N. ;

Shin, Y. ;

Wong, S. ;

Ran, Y. .

XENOBIOTICA, 2009, 39 (09) :700-709

[3] Mutations of the BRAF gene in human cancer [J].

Davies, H ;

Bignell, GR ;

Cox, C ;

Stephens, P ;

Edkins, S ;

Clegg, S ;

Teague, J ;

Woffendin, H ;

Garnett, MJ ;

Bottomley, W ;

Davis, N ;

Dicks, N ;

Ewing, R ;

Floyd, Y ;

Gray, K ;

Hall, S ;

Hawes, R ;

Hughes, J ;

Kosmidou, V ;

Menzies, A ;

Mould, C ;

Parker, A ;

Stevens, C ;

Watt, S ;

Hooper, S ;

Wilson, R ;

Jayatilake, H ;

Gusterson, BA ;

Cooper, C ;

Shipley, J ;

Hargrave, D ;

Pritchard-Jones, K ;

Maitland, N ;

Chenevix-Trench, G ;

Riggins, GJ ;

Bigner, DD ;

Palmieri, G ;

Cossu, A ;

Flanagan, A ;

Nicholson, A ;

Ho, JWC ;

Leung, SY ;

Yuen, ST ;

Weber, BL ;

Siegler, HF ;

Darrow, TL ;

Paterson, H ;

Marais, R ;

Marshall, CJ ;

Wooster, R .

NATURE, 2002, 417 (6892) :949-954

[4] Advances in targeting the Ras/Raf/MEK/Erk mitogen-activated protein kinase cascade with MEK inhibitors for cancer therapy [J].

Friday, Bret B. ;

Adjei, Alex A. .

CLINICAL CANCER RESEARCH, 2008, 14 (02) :342-346

[5] Potent and selective pyrazole-based inhibitors of B-Raf kinase [J].

Hansen, Joshua D. ;

Grina, Jonas ;

Newhouse, Brad ;

Welch, Mike ;

Topalov, George ;

Littman, Nicole ;

Callejo, Michele ;

Gloor, Susan ;

Martinson, Matthew ;

Laird, Ellen ;

Brandhuber, Barbara J. ;

Vigers, Guy ;

Morales, Tony ;

Woessner, Rich ;

Randolph, Nikole ;

Lyssikatos, Joseph ;

Olivero, Alan .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (16) :4692-4695

[6] RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth [J].

Hatzivassiliou, Georgia ;

Song, Kyung ;

Yen, Ivana ;

Brandhuber, Barbara J. ;

Anderson, Daniel J. ;

Alvarado, Ryan ;

Ludlam, Mary J. C. ;

Stokoe, David ;

Gloor, Susan L. ;

Vigers, Guy ;

Morales, Tony ;

Aliagas, Ignacio ;

Liu, Bonnie ;

Sideris, Steve ;

Hoeflich, Klaus P. ;

Jaiswal, Bijay S. ;

Seshagiri, Somasekar ;

Koeppen, Hartmut ;

Belvin, Marcia ;

Friedman, Lori S. ;

Malek, Shiva .

NATURE, 2010, 464 (7287) :431-U132

[7] Antitumor Efficacy of the Novel RAF Inhibitor GDC-0879 Is Predicted by BRAFV600E Mutational Status and Sustained Extracellular Signal-Regulated Kinase/Mitogen-Activated Protein Kinase Pathway Suppression [J].

Hoeflich, Klaus P. ;

Herter, Sylvia ;

Tien, Janet ;

Wong, Leo ;

Berry, Leanne ;

Chan, Jocelyn ;

O'Brien, Carol ;

Modrusan, Zora ;

Seshagiri, Somasekar ;

Lackner, Mark ;

Stern, Howard ;

Choo, Edna ;

Murray, Lesley ;

Friedman, Lori S. ;

Belvin, Marcia .

CANCER RESEARCH, 2009, 69 (07) :3042-3051

[8]

Li NX, 2007, CURR OPIN INVEST DR, V8, P452

[9] Is B-Raf a good therapeutic target for melanoma and other malignancies? [J].

Madhunapantula, SubbaRao V. ;

Robertson, Gavin P. .

CANCER RESEARCH, 2008, 68 (01) :5-8

[10] Roles of the Raf/MEK/ERK pathway in cell growth, malignant transformation and drug resistance [J].

McCubrey, James A. ;

Steelman, Linda S. ;

Chappell, William H. ;

Abrams, Stephen L. ;

Wong, Ellis W. T. ;

Chang, Fumin ;

Lehmann, Brian ;

Terrian, David M. ;

Milella, Michele ;

Tafuri, Agostino ;

Stivala, Franca ;

Libra, Massimo ;

Basecke, Jorg ;

Evangelisti, Camilla ;

Martelli, Alberto M. ;

Franklin, Richard A. .

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH, 2007, 1773 (08) :1263-1284

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