Overcoming bioanalytical challenges in an Onglyza® intravenous [ 14C]microdose absolute bioavailability study with accelerator MS

Bioanalysis

Volumn 4, Issue 15, 2012, Pages 1855-1870

  Xu, Xiaohui ^a   Dueker, Stephen R ^b   Christopher, Lisa J ^a   Lohstroh, Pete N ^b   Keung, Chi Fung ^a   Cao, Kai ^a   Bonacorsi, Samuel J ^a   Cojocaru, Laura ^c   Shen, Jim X ^a   Humphreys, W Griffith ^a   Stouffer, Bruce ^a   Arnold, Mark E ^a  

^a BRISTOL MYERS SQUIBB   (United States)

^b Vitalea Science Inc   (United States)

^c Tandem Labs   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CARBON 14; DRUG RECEPTOR; SAXAGLIPTIN;

ACCELERATOR MASS SPECTROMETRY; ACCURACY; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; DRUG ADSORPTION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG MICRODOSE; DRUG RELEASE; FRACTIONATION; HUMAN; HUMAN EXPERIMENT; ISOTOPE LABELING; MALE; MASS SPECTROMETRY; NON INSULIN DEPENDENT DIABETES MELLITUS; NORMAL HUMAN; PRECIPITATION; QUANTITATIVE ANALYSIS; ULTRA PERFORMANCE LIQUID CHROMATOGRAPHY; VALIDATION PROCESS;

ADAMANTANE; ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; CALIBRATION; CARBON RADIOISOTOPES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DIABETES MELLITUS, TYPE 2; DIPEPTIDES; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DRUG EVALUATION; HUMANS; INJECTIONS, INTRAVENOUS; MALE; MASS SPECTROMETRY; REPRODUCIBILITY OF RESULTS; SENSITIVITY AND SPECIFICITY;

EID: 84865794138     PISSN: 17576180     EISSN: 17576199     Source Type: Journal    
DOI: 10.4155/bio.12.171     Document Type: Article

References (22)

1. Boulton DW, Kasichayanula S, Keung CF et al. The absolute oral bioavailability of saxagliptin and dapagliflozin. Br. J. Clin. Pharmacol.doi:10.1111/j.1365-2125.2012.04391.x (Epub. ahead of print) (2012
2. Fifield LK. Accelerator mass spectrometry and its application. Rep. Prog. Phys. 62, 1223-1274 (1999
3. Arjomand A. Accelerator mass spectrometry-enabled studies: Current status and future prospects. Bioanalysis 2(3), 519-541 (2010
4. Christopher LJ, Hong H, Vakkalagadda BJ et al. Metabolism and disposition of [14C]BMS-690514 an ErbB/vascular endothelial growth factor receptor inhibitor, after oral administration to humans. Drug Metab. Dispos. 38, 2049-2059 (2010
5. ICH Topic M3(R2). Non-clinical safety studies for the conduct of human clinical trials and marketing authorization for pharmaceuticals. International conference on harmonisation of technical requirements for registration of pharmaceuticals for human use (2009
6. Sarapa N, Hsyu PH, Lappin G, Garner RC. The application of accelerator mass spectrometry to absolute bioavailability studies in humans: Simultaneous administration of an intravenous microdose of 14C-nelfinavir mesylate solution and oral nelfinavir to healthy volunteers. J. Clin. Pharmacol. 45, 1198-1205 (2005 (Pubitemid 41361920)
7. Gao L, Li J, Kasserra C et al. Precision and accuracy in the quantitative analysis of biological samples by accelerator mass spectrometry: Application in microdose absolute bioavailability studies. Anal. Chem. 83(14), 5607-5616 (2011
8. Ings R. Microdosing: A valuable tool for accelerating drug development and the role of bioanalytical methods in meeting the challenge. Bioanalysis 1(7), 1293-1305 (2009
9. Su H, Boulton DW, Barros A Jr et al. In vivo pharmacokinetics and disposition and in vitro metabolism, inhibition and induction potential of saxagliptin in human. Drug Metab. Dispos. 40(7), 1345-1356 (2012
10. Xu X, Dremers R, Gu H et al. Liquid chromatography and tandem mass spectrometry method for the quantitative determination of saxagliptin and its major pharmacologically active 5-monohydroxy metabolite in human plasma: Method validation and overcoming specific and non-specific binding at low concentrations. J. Chromatogr. B 889-890, 77-86 (2012
11. Kirby M, Yu DM, O'Connor S, Gorrell MD. Inhibitor selectivity in the clinical application of dipeptidyl peptidase-4 inhibition. Clin. Sci. (Lond.) 118, 31-41 (2010
12. Cao K, Bonacorsi Jr SJ, Balasubramanian B et al. Carbon-14 labeling of saxagliptin (BMS-477118). J. Label. Compd. Radiopharm. 50, 1224-1229 (2007 (Pubitemid 351211392)
13. Vogel JS, Giacomo JA, Schulze-König T, Keck BD, Lohstroh P, Dueker SR. Accelerator mass spectrometry best practices for accuracy and precision in bioanalytical 14C measurements. Bioanalysis 2(3), 455-468 (2010
14. Vogel JS, Lohstroh PN, Keck BD, Dueker SR. Quantitative drug metabolism with accelerator mass spectrometry. In: Mass Spectrometry in Drug Metabolism And Disposition: Basic Principles And Applications. Lee M, Zhu M (Eds). John Wiley & Sons, Inc., NJ, USA (2011
15. Schulze-König T, Dueker SR, Giacomo J, Suter M, Vogel JS, Synal HA. BioMICADAS: Compact next generation AMS system for pharmaceutical science. Nucl. Instrum. Meth. Phys. Res. B 268, 891-894 (2010
16. Vogel JS. Rapid production of graphite without contamination for biomedical AMS. Radiocarbon 34(3), 344-350 (1992
17. 2 obtained from biochemical samples to graphite in septa-sealed vials for quantification of 14C via accelerator mass spectrometry. Anal. Chem. 75, 2192-2196 (2003 (Pubitemid 36542364)
18. Keck BD, Ognibene T, Vogel JS. Analytical validation of accelerator mass spectrometry for pharmaceutical development. Bioanalysis 2(3), 469-485 (2010
19. Synal H, Stocker M, Suter M. MICADAS: A new compact radiocarbon AMS system. Nuc. Inst. Meth. Phys. Res. Section B 259(1), 7-13 (2007 (Pubitemid 46726719)
20. Zoppi U, Crye J, Song Q, Arjomand A. Performance evaluation of the new AMS system at accium biosciences. Radiocarbon 49(1), 171-180 (2007
21. Salehpour M, Possnert G, Bryhni H, Palminger-Hallen I, Stahle L. Biological accelerator mass spectrometry at Uppsala University. Appl. Radiat. Isot. 67(3), 495-499 (2007
22. Fura A, Khanna A, Vyas V et al. Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections. Drug Metab. Dispos. 37, 1164-1171 (2009).