Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by the erythromycin breath test [published erratum appears in Drug Metab Dispos 1995 Mar;23(3):following table of contents]

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Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by the erythromycin breath test [published erratum appears in Drug Metab Dispos 1995 Mar;23(3):following table of contents]

KS Lown, JC Kolars, KE Thummel, JL Barnett, KL Kunze, SA Wrighton and PB Watkins

Department of Medicine, University of Michigan Medical Center, Ann Arbor 48109-0108.

The CYP3A subfamily of cytochromes P450 metabolize many medications and environmental contaminants. CYP3A4 and, in 25% of patients, CYP3A5 seem to be the major CYP3A genes expressed in adult liver. Hepatic levels of CYP3A4 can be estimated by the erythromycin breath test and vary at least 10-fold among patients. CYP3A4 has also been shown to be present in small bowel where it is responsible for significant "first-pass" metabolism of orally administered substrates. However, it is not known whether there is significant interindividual variability in the intestinal expression of CYP3A4, or whether the liver and intestinal catalytic activities of CYP3A4 correlate within an individual. It is also not known whether CYP3A5 is expressed in the small intestine. To address these questions, we administered the erythromycin breath test to 20 patients and obtained biopsies from their small bowel. There was a 6-fold variation in CYP3A catalytic activity (midazolam hydroxylation), an 11-fold variation in CYP3A4 protein content, and an 8-fold variation in CYP3A4 mRNA content in intestinal biopsies. There was an excellent correlation between intestinal CYP3A4 protein level and catalytic activity (r = 0.86; p = 0.0001); however, neither parameter significantly correlated with hepatic CYP3A4 activity as measured by the erythromycin breath test result (r = 0.27; p = 0.24 and r = 0.33; p = 0.15, respectively). We also found that CYP3A5 protein was readily detectable in biopsies from 14 (70%) of the patients, indicating that CYP3A5 is commonly expressed in human small intestine.(ABSTRACT TRUNCATED AT 250 WORDS)

Volume 22, Issue 6, pp. 947-955, 11/01/1994
Copyright © 1994 by American Society for Pharmacology and Experimental Therapeutics

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Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by the erythromycin breath test [published erratum appears in Drug Metab Dispos 1995 Mar;23(3):following table of contents]

Volume 22, Issue 6, pp. 947-955, 11/01/1994 Copyright © 1994 by American Society for Pharmacology and Experimental Therapeutics

Volume 22, Issue 6, pp. 947-955, 11/01/1994
Copyright © 1994 by American Society for Pharmacology and Experimental Therapeutics

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				K. E. Thummel, C. Brimer, K. Yasuda, J. Thottassery, T. Senn, Y. Lin, H. Ishizuka, E. Kharasch, J. Schuetz, and E. Schuetz Transcriptional Control of Intestinal Cytochrome P-4503A by 1alpha ,25-Dihydroxy Vitamin D3 Mol. Pharmacol., December 1, 2001; 60(6): 1399 - 1406. [Abstract] [Full Text] [PDF]

				P. Schmiedlin-Ren, K. E. Thummel, J. M. Fisher, M. F. Paine, and P. B. Watkins Induction of CYP3A4 by 1alpha ,25-Dihydroxyvitamin D3 Is Human Cell Line-Specific and Is Unlikely to Involve Pregnane X Receptor Drug Metab. Dispos., November 1, 2001; 29(11): 1446 - 1453. [Abstract] [Full Text] [PDF]

				E. Hustert, A. Zibat, E. Presecan-Siedel, R. Eiselt, R. Mueller, C. Fu{beta}, I. Brehm, U. Brinkmann, M. Eichelbaum, L. Wojnowski, et al. Natural Protein Variants of Pregnane X Receptor with Altered Transactivation Activity Toward CYP3A4 Drug Metab. Dispos., November 1, 2001; 29(11): 1454 - 1459. [Abstract] [Full Text] [PDF]

				X.-Y. Chu, G. P. Sanchez-Castano, K. Higaki, D.-M. Oh, C.-P. Hsu, and G. L. Amidon Correlation between Epithelial Cell Permeability of Cephalexin and Expression of Intestinal Oligopeptide Transporter J. Pharmacol. Exp. Ther., November 1, 2001; 299(2): 575 - 582. [Abstract] [Full Text] [PDF]

				L. Huang, S. A. Wring, J. L. Woolley, K. R. Brouwer, C. Serabjit-Singh, and J. W. Polli Induction of P-Glycoprotein and Cytochrome P450 3A by HIV Protease Inhibitors Drug Metab. Dispos., April 13, 2001; 29(5): 754 - 760. [Abstract] [Full Text]

				M. Kasahara, H. Suzuki, and I. Komiya Studies on the Cytochrome P450 (CYP)-Mediated Metabolic Properties of Miocamycin: Evaluation of the Possibility of a Metabolic Intermediate Complex Formation with CYP, and Identification of the Human CYP Isoforms Drug Metab. Dispos., April 1, 2000; 28(4): 409 - 417. [Abstract] [Full Text]

				J. P. Gibbs, C. A. Liacouras, R. N. Baldassano, and J. T. Slattery Up-Regulation of Glutathione S-Transferase Activity in Enterocytes of Young Children Drug Metab. Dispos., December 1, 1999; 27(12): 1466 - 1469. [Abstract] [Full Text]

				Q.-Y. Zhang, D. Dunbar, A. Ostrowska, S. Zeisloft, J. Yang, and L. S. Kaminsky Characterization of Human Small Intestinal Cytochromes P-450 Drug Metab. Dispos., July 1, 1999; 27(7): 804 - 809. [Abstract] [Full Text]

				M. F. Fromm, D. Darbar, S. Dell'Orto, and D. M. Roden Modulation of Effect of Dietary Salt on Prehepatic First-Pass Metabolism: Effects of beta -Blockade and Intravenous Salt Loading J. Pharmacol. Exp. Ther., July 1, 1999; 290(1): 253 - 258. [Abstract] [Full Text]