Crossreactivity of isolated everolimus metabolites with the Innofluor Certican immunoassay for therapeutic drug monitoring of everolimus

Therapeutic Drug Monitoring

Volumn 29, Issue 6, 2007, Pages 743-749

  Strom, Tobin ^a   Haschke, Manuel ^a   Boyd, Jared ^b   Roberts, Mark ^b   Arabshahi, Lili ^b   Marbach, Peter ^c   Christians, Uwe ^a,d  

^a UNIVERSITY OF COLORADO   (United States)

^b Seradyn   (United States)

^c NOVARTIS PHARMA AG   (Switzerland)

^d Eurofins Medinet Inc   (Germany)

Author keywords

Certican; Crossreactivity; Drug metabolism; Everolimus; HPLC UV; Immunoassay; LC MS MS; SDZ RAD

Indexed keywords

11 HYDROXY EVEROLIMUS; 12 HYDROXY EVEROLIMUS; 14 HYDROXY EVEROLIMUS; 16 HYDROXY EVEROLIMUS; 24 HYDROXY EVEROLIMUS; 25 HYDROXY EVEROLIMUS; 46 HYDROXY EVEROLIMUS; DRUG METABOLITE; EVEROLIMUS; RAPAMYCIN; UNCLASSIFIED DRUG;

ARTICLE; BLOOD; BLOOD SAMPLING; CROSS REACTION; DRUG ISOLATION; DRUG MONITORING; DRUG STABILITY; DRUG STRUCTURE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; IMMUNOASSAY; INNOFLUOR CERTICAN IMMUNOASSAY; ION TRAP MASS SPECTROMETRY; KIDNEY GRAFT; LIVER MICROSOME; MASS SPECTROMETRY; NORMAL HUMAN; PRIORITY JOURNAL; ULTRAVIOLET SPECTROSCOPY;

CROSS REACTIONS; DRUG MONITORING; HUMANS; IMMUNOASSAY; IMMUNOSUPPRESSIVE AGENTS; MICROSOMES, LIVER; MOLECULAR STRUCTURE; SIROLIMUS;

EID: 34848860896     PISSN: 01634356     EISSN: None     Source Type: Journal    
DOI: 10.1097/FTD.0b013e31815b3cbf     Document Type: Article

References (33)

1. Kahan BD. Sirolimus: a comprehensive review. Exp Opin Pharmacother. 2001;2:1903-1917.
2. Nashan B. Review of the proliferation inhibitor everolimus. Exp Opin Investig Drugs. 2002;11:1845-1857.
3. Kovarik JM. Everolimus: a proliferation signal inhibitor targeting primary causes of allograft dysfunction. Drugs Today (Barc). 2004;40:101-109.
4. Dancey JE. Inhibitors of the mammalian target of rapamycin. Exp Opin Investig Drugs. 2005;14:313-328.
5. Augustine JJ, Hricik DE. Experience with everolimus. Transplant Proc. 2004;36:500S-503S.
6. Trepanier DJ, Gallant H, Legatt DF, et al. Rapamycin: distribution, pharmacokinetics and therapeutic range investigations: an update. Clin Biochem. 1998;31:345-351.
7. Schuler W, Sedrani R, Cottens S, et al. SDZ RAD, a new rapamycin derivative: pharmacological properties in vitro and in vivo. Transplantation. 1997;64:36-42.
8. Schuurman HJ, Cottens S, Fuchs S, et al. SDZ RAD, a new rapamycin derivative: synergism with cyclosporine. Transplantation. 1997;64:32-35.
9. Nashan B. Early clinical experience with a novel rapamycin derivative. Ther Drug Monit. 2002;24:53-58.
10. Kovarik JM, Tedesco H, Pascual J, et al. Everolimus therapeutic concentration range defined from a prospective trial with reduced-exposure cyclosporine in de novo kidney transplantation. Ther Drug Monit. 2004;26:499-505.
11. Kovarik JM, Kaplan B, Tedesco Silva H, et al. Exposure-response relationships for everolimus in de novo kidney transplantation: defining a therapeutic range. Transplantation. 2002;73:920-925.
12. Boyd J, Arabshahi L, Roberts M, et al. A New FPIA Immunoassay for the quantitative determination of everolimus in whole blood. Ther Drug Monit. 2005;27:213-214.
13. Jones K, Saadat-Lajevard S, Lee T, et al. An immunoassay for the measurement of sirolimus. Clin Ther. 2000;22:B49-B61.
14. Holt DW, McKeown DA, Lee TD, et al. The relative proportions of sirolimus metabolites in blood using HPLC with mass-spectrometric detection. Transplant Proc. 2004;36:3223-3225.
15. Christians U, Sattler M, Schiebel HM, et al. Isolation of two immunosuppressive metabolites after in vitro metabolism of rapamycin. Drug Metab Dispos. 1992;20:186-191.
16. Jacobsen W, Serkova N, Hausen B, et al. Comparison of the in vitro metabolism of the macrolide immunosuppressants sirolimus and RAD. Transplant Proc. 2001;33:514-515.
17. Kuhn B, Jacobsen W, Christians U, et al. Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem. 2001;44:2027-2034.
18. Streit F, Christians U, Schiebel HM, et al. Sensitive and specific quantification of sirolimus (rapamycin) and its metabolites in blood of kidney graft recipients by HPLC/electrospray-mass spectrometry. Clin Chem. 1996;42:1417-1425.
19. Christians U, Jacobsen W, Serkova N, et al. Automated, fast and sensitive quantification of drugs in blood by liquid chromatography-mass spectrometry with on-line extraction: immunosuppressants. J Chromatogr B Biomed Sci Appl. 2000;748:41-53.
20. Morris RE. Rapamycins: antifungal, antitumor, antiproliferative and immunosuppressive macrolides. Transplant Rev. 1992;6:39-81.
21. Wang PC, Chan KW, Schiksnis RA, et al. High-performance liquid chromatographic isolation, spectroscopic characterization, and immunosuppressive activities of two rapamycin degradation products. J Liquid Chromatogr. 1994;17:3383-3392.
22. Streit F, Christians U, Schiebel HM, et al. Structural identification of four metabolites of the macrolide immunosuppressant sirolimus after in vitro metabolism by electrospray-MS/MS. Drug Metab Dispos. 1996;24:1272-1278.
23. Hallensleben K, Raida M, Habermehl G. Identification of a new metabolite of macrolide immunosuppressants, like rapamycin and SDZ-RAD, using high-performance liquid chromatography and electrospray tandem mass spectrometry. J Am Soc Mass Spectrom. 2000;11:516-525.
24. Vidal C, Kirchner GI, Sewing KF. Structural elucidation by electrospray mass spectrometry: an approach to the in vitro metabolism of the macrolide immunosuppressant SDZ RAD. J Am Soc Mass Spectrom. 1998;9:1267-1274.
25. Boernsen KO, Egge-Jacobsen W, Inverardi B, et al. Assessment and validation of the MS/MS fragmentation patterns of the macrolide immunosuppressant everolimus. J Mass Spectrometr. 2007;42:793-802.
26. Yatscoff RW, Wang P, Chan K, et al. Rapamycin: distribution, pharmacokinetics, and therapeutic range investigations. Ther Drug Monit. 1995;17:666-671.
27. Holt DW. Therapeutic drug monitoring of immunosuppressive drugs in kidney transplantation. Curr Opin Nephrol Hypertens. 2002;11:657-663.
28. Kirchner GI, Winkler M, Mueller L, et al. Pharmacokinetics of SDZ RAD and cyclosporin including their metabolites in seven kidney graft patients after the first dose of SDZ RAD. Br J Clin Pharmacol. 2000;50:449-454.
29. Kirchner GI, Mueller L, Winkler M, et al. Long-term pharmacokinetics of the metabolites of everolimus and cyclosporine in renal transplant recipients. Transplant Proc. 2002;34:2233-2234.
30. Kirchner GI, Vidal C, Winkler M, et al. LC/ESI-MS allows simultaneous and specific quantification of SDZ RAD and cyclosporine, including groups of their metabolites in human blood. Ther Drug Monit. 1999;21:116-122.
31. Strom T, Haschke M, Zhang YL, et al. Identification of everolimus metabolite patterns in trough blood samples of kidney transplant patients. Ther Drug Monit. 2007;29:592-599.
32. Salm P, Warnholtz C, Boyd J, et al. Evaluation of a fluorescent polarization immunoassay for whole blood everolimus determination using samples from renal transplant recipients. Clin Biochem. 2006;39:732-738.
33. Engelmayer J, Engelmayer U, Streit F, et al. Comparison of the Seradyn Innofluor Certican assay on TDXFLX system with LC/MS-MS. Ther Drug Monit. 2005;27:217.