Effect of Tacrolimus Formulation (Prolonged-Release vs Immediate-Release) on Its Susceptibility to Drug-Drug Interactions with St. John's Wort.
St. John's Wort
drug formulation
drug-drug interaction
pharmacogenetics
tacrolimus
Journal
Clinical pharmacology in drug development
ISSN: 2160-7648
Titre abrégé: Clin Pharmacol Drug Dev
Pays: United States
ID NLM: 101572899
Informations de publication
Date de publication:
04 Jan 2024
04 Jan 2024
Historique:
received:
11
08
2023
accepted:
28
11
2023
medline:
5
1
2024
pubmed:
5
1
2024
entrez:
4
1
2024
Statut:
aheadofprint
Résumé
Tacrolimus is metabolized by cytochrome P450 3A (CYP3A) and is susceptible to interactions with the CYP3A and P-glycoprotein inducer St. John's Wort (SJW). CYP3A isozymes are predominantly expressed in the small intestine and liver. Prolonged-release tacrolimus (PR-Tac) is largely absorbed in distal intestinal segments and is less susceptible to CYP3A inhibition. The effect of induction by SJW is unknown. In this randomized, crossover trial, 18 healthy volunteers received single oral tacrolimus doses (immediate-release [IR]-Tac or PR-Tac, 5 mg each) alone and during induction by SJW. Concentrations were quantified using ultra-high performance liquid chromatography coupled with tandem mass spectrometry and non-compartmental pharmacokinetics were evaluated. SJW decreased IR-Tac exposure (area under the concentration-time curve) to 73% (95% confidence interval 60%-88%) and maximum concentration (C
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Informations de copyright
© 2024 The Authors. Clinical Pharmacology in Drug Development published by Wiley Periodicals LLC on behalf of American College of Clinical Pharmacology.
Références
Schiff J, Cole E, Cantarovich M. Therapeutic monitoring of calcineurin inhibitors for the nephrologist. Clin J Am Soc Nephrol. 2007;2(2):374-384.
Hebert MF. Contributions of hepatic and intestinal metabolism and P-glycoprotein to cyclosporine and tacrolimus oral drug delivery. Adv Drug Deliv Rev. 1997;27(2-3):201-214.
Vannaprasaht S, Reungjui S, Supanya D, et al. Personalized tacrolimus doses determined by CYP3A5 genotype for induction and maintenance phases of kidney transplantation. Clin Ther. 2013;35(11):1762-1769.
Tsuchiya N, Satoh S, Tada H, et al. Influence of CYP3A5 and MDR1 (ABCB1) polymorphisms on the pharmacokinetics of tacrolimus in renal transplant recipients. Transplantation. 2004;78(8):1182-1187.
Masuda S, Goto M, Okuda M, et al. Initial dosage adjustment for oral administration of tacrolimus using the intestinal MDR1 level in living-donor liver transplant recipients. Transplant Proc. 2005;37(4):1728-1729.
Choi JH, Lee YJ, Jang SB, Lee JE, Kim KH, Park K. Influence of the CYP3A5 and MDR1 genetic polymorphisms on the pharmacokinetics of tacrolimus in healthy Korean subjects. Br J Clin Pharmacol. 2007;64(2):185-191.
Kuypers DR, de Jonge H, Naesens M, Lerut E, Verbeke K, Vanrenterghem Y. CYP3A5 and CYP3A4 but not MDR1 single-nucleotide polymorphisms determine long-term tacrolimus disposition and drug-related nephrotoxicity in renal recipients. Clin Pharmacol Ther. 2007;82(6):711-725.
Garnock-Jones KP. Tacrolimus prolonged release (Envarsus®): a review of its use in kidney and liver transplant recipients. Drugs. 2015;75(3):309-320.
Mercuri A, Wu S, Stranzinger S, et al. In vitro and in silico characterisation of tacrolimus released under biorelevant conditions. Int J Pharm. 2016;515(1-2):271-280.
Nigro V, Glicklich A, Weinberg J. Improved bioavailability of MELTDOSE once-daily formulation of tacrolimus (LCP-Tacro) with controlled agglomeration allows for consistent absorption over 24 hrs: a scintigraphic and pharmacokinetic evaluation. Am J Transplant. 2013;13(suppl 5):339(abstract).
Drozdzik M, Busch D, Lapczuk J, et al. Protein abundance of clinically relevant drug-metabolizing enzymes in the human liver and intestine: a comparative analysis in paired tissue specimens. Clin Pharmacol Ther. 2018;104(3):515-524.
Bergheim I, Bode C, Parlesak A. Distribution of cytochrome P450 2C, 2E1, 3A4, and 3A5 in human colon mucosa. BMC Clin Pharmacol. 2005;5:4.
Zhang QY, Dunbar D, Ostrowska A, Zeisloft S, Yang J, Kaminsky LS. Characterization of human small intestinal cytochromes P-450. Drug Metab Dispos. 1999;27(7):804-809.
Huppertz A, Ott C, Bruckner T, et al. Prolonged-release tacrolimus is less susceptible to interaction with the strong CYP3A inhibitor voriconazole in healthy volunteers. Clin Pharmacol Ther. 2019;106(6):1290-1298.
Dresser GK, Schwarz UI, Wilkinson GR, Kim RB. Coordinate induction of both cytochrome P4503A and MDR1 by St John's wort in healthy subjects. Clin Pharmacol Ther. 2003;73(1):41-50.
Mueller SC, Majcher-Peszynska J, Uehleke B, et al. The extent of induction of CYP3A by St. John's wort varies among products and is linked to hyperforin dose. Eur J Clin Pharmacol. 2006;62(1):29-36.
Hebert MF, Park JM, Chen YL, Akhtar S, Larson AM. Effects of St. John's wort (Hypericum perforatum) on tacrolimus pharmacokinetics in healthy volunteers. J Clin Pharmacol. 2004;44(1):89-94.
Mai I, Störmer E, Bauer S, Krüger H, Budde K, Roots I. Impact of St John's wort treatment on the pharmacokinetics of tacrolimus and mycophenolic acid in renal transplant patients. Nephrol Dial Transplant. 2003;18(4):819-822.
Hebert MF, Fisher RM, Marsh CL, Dressler D, Bekersky I. Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers. J Clin Pharmacol. 1999;39(1):91-96.
Floren LC, Bekersky I, Benet LZ, et al. Tacrolimus oral bioavailability doubles with coadministration of ketoconazole. Clin Pharmacol Ther. 1997;62(1):41-49.
Tuteja S, Alloway RR, Johnson JA, Gaber AO. The effect of gut metabolism on tacrolimus bioavailability in renal transplant recipients. Transplantation. 2001;71(9):1303-1307.
van de Kerkhof EG, de Graaf IA, Ungell AL, Groothuis GM. Induction of metabolism and transport in human intestine: validation of precision-cut slices as a tool to study induction of drug metabolism in human intestine in vitro. Drug Metab Dispos. 2008;36(3):604-613.
Gervot L, Carrière V, Costet P, et al. CYP3A5 is the major cytochrome P450 3A expressed in human colon and colonic cell lines. Environ Toxicol Pharmacol. 1996;2(4):381-388.
Campagne O, Mager DE, Brazeau D, Venuto RC, Tornatore KM. Tacrolimus population pharmacokinetics and multiple CYP3A5 genotypes in black and white renal transplant recipients. J Clin Pharmacol. 2018;58(9):1184-1195.
Adiwidjaja J, Boddy AV, McLachlan AJ. Physiologically based pharmacokinetic modelling of hyperforin to predict drug interactions with St John's Wort. Clin Pharmacokinet. 2019;58(7):911-926.
Hohmann N, Kocheise F, Carls A, Burhenne J, Haefeli WE, Mikus G. Midazolam microdose to determine systemic and pre-systemic metabolic CYP3A activity in humans. Br J Clin Pharmacol. 2015;79(2):278-285.
Halama B, Hohmann N, Burhenne J, Weiss J, Mikus G, Haefeli WE. A nanogram dose of the CYP3A probe substrate midazolam to evaluate drug interactions. Clin Pharmacol Ther. 2013;93(6):564-571.
Katzenmaier S, Markert C, Riedel KD, Burhenne J, Haefeli WE, Mikus G. Determining the time course of CYP3A inhibition by potent reversible and irreversible CYP3A inhibitors using a limited sampling strategy. Clin Pharmacol Ther. 2011;90(5):666-673.
Katzenmaier S, Markert C, Mikus G. Proposal of a new limited sampling strategy to predict CYP3A activity using a partial AUC of midazolam. Eur J Clin Pharmacol. 2010;66(11):1137-1141.
Burhenne J, Halama B, Maurer M, et al. Quantification of femtomolar concentrations of the CYP3A substrate midazolam and its main metabolite 1'-hydroxymidazolam in human plasma using ultra performance liquid chromatography coupled to tandem mass spectrometry. Anal Bioanal Chem. 2012;402(7):2439-2450.
Fredericks S, Moreton M, MacPhee IA, et al. Genotyping cytochrome P450 3A5 using the Light Cycler. Ann Clin Biochem. 2005;42(pt 5):376-381.
Johne A, Brockmöller J, Bauer S, Maurer A, Langheinrich M, Roots I. Pharmacokinetic interaction of digoxin with an herbal extract from St John's wort (Hypericum perforatum). Clin Pharmacol Ther. 1999;66(4):338-345.
Drozdzik M, Busch D, Lapczuk J, et al. Protein abundance of clinically relevant drug transporters in the human liver and intestine: a comparative analysis in paired tissue specimens. Clin Pharmacol Ther. 2019;105(5):1204-1212.
Takayama K, Ito K, Matsui A, et al. In vivo gene expression profile of human intestinal epithelial cells: from the viewpoint of drug metabolism and pharmacokinetics. Drug Metab Dispos. 2021;49(3):221-232.
Thörn M, Finnström N, Lundgren S, Rane A, Lööf L. Cytochromes P450 and MDR1 mRNA expression along the human gastrointestinal tract. Br J Clin Pharmacol. 2005;60(1):54-60.
Guo Y, Crnkovic CM, Won KJ, et al. Commensal gut bacteria convert the immunosuppressant tacrolimus to less potent metabolites. Drug Metab Dispos. 2019;47(3):194-202.
Lee JY, Tsolis RM, Bäumler AJ. The microbiome and gut homeostasis. Science. 2022;377(6601):eabp9960.
Krusekopf S, Roots I, Kleeberg U. Differential drug-induced mRNA expression of human CYP3A4 compared to CYP3A5, CYP3A7 and CYP3A43. Eur J Pharmacol. 2003; 466(1-2):7-12.
Yamamoto Y, Nakase H, Matsuura M, Maruyama S, Masuda S. CYP3A5 genotype as a potential pharmacodynamic biomarker for tacrolimus therapy in ulcerative colitis in Japanese patients. Int J Mol Sci. 2020;21(12):4347.
Hokkanen J, Tolonen A, Mattila S, Turpeinen M. Metabolism of hyperforin, the active constituent of St. John's wort, in human liver microsomes. Eur J Pharm Sci. 2011;42(3):273-284.
Venkataramanan R, Jain A, Cadoff E, et al. Pharmacokinetics of FK 506: preclinical and clinical studies. Transplant Proc. 1990;22(1):52-56.
Marquet P, Albano L, Woillard JB, et al. Comparative clinical trial of the variability factors of the exposure indices used for the drug monitoring of two tacrolimus formulations in kidney transplant recipients. Pharmacol Res. 2018;129:84-94.