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Clinical Chemistry, Vol 42, 1417-1425, Copyright © 1996 by American Association for Clinical Chemistry
F Streit, U Christians, HM Schiebel, KL Napoli, L Ernst, A Linck, BD Kahan and KF Sewing
Institut fur Allgemeine Pharmakologie, Medizinische Hochschule Hannover, Germany.
Sirolimus (rapamycin) has a macrolide structure and is under clinical investigation as an immunosuppressant after organ transplantation. An HPLC/mass spectrometry assay to quantify sirolimus in blood was developed. 28-O-Acetyl sirolimus was used as internal standard. Blood samples were extracted with C18 columns. The extracts were injected into an HPLC system and isocratically eluted with methanol/1% formic acid (90/10 by vol) from a 150 X 4 mm C18 analytical column. The HPLC system was connected to a triple-stage quadrupole mass spectrometer with an electrospray interface and positive ions were detected. The limit of quantification in 1 mL of blood was 0.25 microgram/L and the calibration curve in blood was linear up to 250 microgram/L. The recovery from blood was 88 +/- 26% and interassay variation at 1 microgram/L was 19% and at 15 microgram/L 9.3%. Hydroxy, dihydroxy, demethyl, and didemethyl sirolimus as well as sirolimus were detected in blood of kidney graft patients.
The following articles in journals at HighWire Press have cited this article:
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  N. Picard, N. Djebli, F.-L. Sauvage, and P. Marquet Metabolism of Sirolimus in the Presence or Absence of Cyclosporine by Genotyped Human Liver Microsomes and Recombinant Cytochromes P450 3A4 and 3A5 Drug Metab. Dispos., March 1, 2007; 35(3): 350 - 355. [Abstract] [Full Text] [PDF]
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 C. L. Cummins, W. Jacobsen, U. Christians, and L. Z. Benet CYP3A4-Transfected Caco-2 Cells as a Tool for Understanding Biochemical Absorption Barriers: Studies with Sirolimus and Midazolam J. Pharmacol. Exp. Ther., January 1, 2004; 308(1): 143 - 155. [Abstract] [Full Text] [PDF]
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 C. Dambrin, J. Klupp, T. Birsan, J. Luna, T. Suzuki, T. Lam, P. Stahr, B. Hausen, U. Christians, P. Fitzgerald, et al. Sirolimus (Rapamycin) Monotherapy Prevents Graft Vascular Disease in Nonhuman Primate Recipients of Orthotopic Aortic Allografts Circulation, May 13, 2003; 107(18): 2369 - 2374. [Abstract] [Full Text] [PDF]
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V. J. Wacher, J. A. Silverman, S. Wong, P. Tran-Tau, A. O. Chan, A. Chai, X.-Q. Yu, D. O'Mahony, and Z. Ramtoola Sirolimus Oral Absorption in Rats Is Increased by Ketoconazole but Is Not Affected by D-alpha -Tocopheryl Poly(Ethylene Glycol 1000) Succinate J. Pharmacol. Exp. Ther., October 1, 2002; 303(1): 308 - 313. [Abstract] [Full Text] [PDF]
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 H. PODDER, S. M. STEPKOWSKI, K. L. NAPOLI, J. CLARK, R. R. VERANI, T.-C. CHOU, and B. D. KAHAN Pharmacokinetic Interactions Augment Toxicities of Sirolimus/Cyclosporine Combinations J. Am. Soc. Nephrol., May 1, 2001; 12(5): 1059 - 1071. [Abstract] [Full Text]
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 D. W. Holt, T. Lee, K. Jones, and A. Johnston Validation of an Assay for Routine Monitoring of Sirolimus Using HPLC with Mass Spectrometric Detection Clin. Chem., August 1, 2000; 46(8): 1179 - 1183. [Full Text] [PDF]
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N. Serkova, B. Hausen, G. J. Berry, W. Jacobsen, L. Z. Benet, R. E. Morris, and U. Christians Tissue Distribution and Clinical Monitoring of the Novel Macrolide Immunosuppressant SDZ-RAD and Its Metabolites in Monkey Lung Transplant Recipients: Interaction with Cyclosporine J. Pharmacol. Exp. Ther., July 1, 2000; 294(1): 323 - 332. [Abstract] [Full Text]
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 B. Hausen, K. Boeke, G. J. Berry, U. Christians, W. Schuler, and R. E. Morris Successful treatment of acute, ongoing rat lung allograft rejection with the novel immunosuppressant SDZ-RAD Ann. Thorac. Surg., March 1, 2000; 69(3): 904 - 909. [Abstract] [Full Text] [PDF]
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P. Salm, P. J. Taylor, and P. I. Pillans Analytical Performance of Microparticle Enzyme Immunoassay and HPLC-Tandem Mass Spectrometry in the Determination of Sirolimus in Whole Blood Clin. Chem., December 1, 1999; 45(12): 2278 - 2280. [Full Text] [PDF]
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J. F. GUMMERT, T. IKONEN, and R. E. MORRIS Newer Immunosuppressive Drugs: A Review J. Am. Soc. Nephrol., June 1, 1999; 10(6): 1366 - 1380. [Abstract] [Full Text]
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N. Serkova, L. Litt, T. L. James, W. Sadée, D. Leibfritz, L. Z. Benet, and U. Christians Evaluation of Individual and Combined Neurotoxicity of the Immunosuppressants Cyclosporine and Sirolimus by In Vitro Multinuclear NMR Spectroscopy J. Pharmacol. Exp. Ther., May 1, 1999; 289(2): 800 - 806. [Abstract] [Full Text]
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A. Lampen, Y. Zhang, I. Hackbarth, L. Z. Benet, K.-Fr. Sewing, and U. Christians Metabolism and Transport of the Macrolide Immunosuppressant Sirolimus in the Small Intestine J. Pharmacol. Exp. Ther., June 1, 1998; 285(3): 1104 - 1112. [Abstract] [Full Text]
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C. Vidal, G. I. Kirchner, G. Wunsch, and K.-F. Sewing Automated simultaneous quantification of the immunosuppressants 40-O-(2-hydroxyethyl)rapamycin and cyclosporine in blood with electrospray-mass spectrometric detection Clin. Chem., June 1, 1998; 44(6): 1275 - 1282. [Abstract] [Full Text] [PDF]
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M. J. M. Nickmilder, D. Latinne, J.-P. De Houx, R. K. Verbeeck, and G. J. J. Lhoest Isolation and identification of a C39 demethylated metabolite of rapamycin from pig liver microsomes and evaluation of its immunosuppressive activity Clin. Chem., March 1, 1998; 44(3): 532 - 538. [Abstract] [Full Text] [PDF]
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